Trial Outcomes & Findings for A Study in Healthy Adult Male Participants to Assess Absorption, Distribution, Metabolism and Excretion (ADME) of Radiolabeled PF-06865571. (NCT NCT04866225)
NCT ID: NCT04866225
Last Updated: 2024-07-31
Results Overview
The total recovery of radioactivity in urine was listed and summarized using descriptive statistics. In this outcome measure, the percentages of dose excreted in urine in Period 1 and Period 2 were reported.
COMPLETED
PHASE1
6 participants
Period 1: Day -1 to maximum Day 21; Period 2: Day 1 to maximum Day 3
2024-07-31
Participant Flow
Participant milestones
| Measure |
Period 1:[14C]PF-06865571 300 mg Oral; Period 2:PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
Six healthy male participants were enrolled and received 2 regimens (A and B) in Periods 1 and 2, respectively. For regimen A in Period 1, an oral dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered. For regimen B in Period 2, an oral dose of 300 mg unlabeled PF-06865571 followed by an intravenous (IV) dose of 300 nCi \[14C\] in 100 μg of PF-06865571 was administered.
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|---|---|
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Overall Study
STARTED
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6
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Overall Study
COMPLETED
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6
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Overall Study
NOT COMPLETED
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0
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Reasons for withdrawal
Withdrawal data not reported
Baseline Characteristics
A Study in Healthy Adult Male Participants to Assess Absorption, Distribution, Metabolism and Excretion (ADME) of Radiolabeled PF-06865571.
Baseline characteristics by cohort
| Measure |
Period 1:[14C]PF-06865571 300 mg Oral; Period 2:PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
n=6 Participants
Six healthy male participants were enrolled and received 2 regimens (A and B) in Periods 1 and 2, respectively. For regimen A in Period 1, an oral dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered. For regimen B in Period 2, an oral dose of 300 mg unlabeled PF-06865571 followed by an intravenous (IV) dose of 300 nCi \[14C\] in 100 μg of PF-06865571 was administered.
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|---|---|
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Age, Continuous
Mean
|
42.0 Years
STANDARD_DEVIATION 13.90 • n=5 Participants
|
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Age, Customized
<18 years
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0 Participants
n=5 Participants
|
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Age, Customized
18-25 years
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1 Participants
n=5 Participants
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Age, Customized
26-35 years
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1 Participants
n=5 Participants
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Age, Customized
36-45 years
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1 Participants
n=5 Participants
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Age, Customized
>45 years
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3 Participants
n=5 Participants
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Sex: Female, Male
Female
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0 Participants
n=5 Participants
|
|
Sex: Female, Male
Male
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6 Participants
n=5 Participants
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Ethnicity (NIH/OMB)
Hispanic or Latino
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2 Participants
n=5 Participants
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Ethnicity (NIH/OMB)
Not Hispanic or Latino
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4 Participants
n=5 Participants
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Ethnicity (NIH/OMB)
Unknown or Not Reported
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0 Participants
n=5 Participants
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Race/Ethnicity, Customized
White
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4 Participants
n=5 Participants
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Race/Ethnicity, Customized
Black or African American
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2 Participants
n=5 Participants
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PRIMARY outcome
Timeframe: Period 1: Day -1 to maximum Day 21; Period 2: Day 1 to maximum Day 3Population: Analysis population included all participants who received 1 dose of \[14C\]PF-06865571 and who have evaluable total radioactivity concentration (urinary and fecal) data and who had no protocol deviations or AEs (such as vomiting of the dose, diarrhoea or severe constipation) that may have affected the extent of excretion analysis.
The total recovery of radioactivity in urine was listed and summarized using descriptive statistics. In this outcome measure, the percentages of dose excreted in urine in Period 1 and Period 2 were reported.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
n=6 Participants
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
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|---|---|---|
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Total Recovery of Radioactivity in Urine as Percentage of Total Radioactive Dose of PF-06865571 Administered
|
48.9 Percentage of Dose
Standard Deviation 16.3
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51.5 Percentage of Dose
Standard Deviation 15.8
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PRIMARY outcome
Timeframe: Period 1: Day -1 to maximum Day 21; Period 2: Day 1 to maximum Day 3Population: Analysis population included all participants who received 1 dose of \[14C\]PF-06865571 and who have evaluable total radioactivity concentration (urinary and fecal) data and who had no protocol deviations or AEs (such as vomiting of the dose, diarrhoea or severe constipation) that may have affected the extent of excretion analysis.
The total recovery of radioactivity in feces was listed and summarized using descriptive statistics. In this outcome measure, the percentages of dose excreted in feces in Period 1 and Period 2 were reported.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
n=6 Participants
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
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|---|---|---|
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Total Recovery of Radioactivity in Feces as Percentage of Total Radioactive Dose of PF-06865571 Administered
|
30.1 Percentage of Dose
Standard Deviation 2.9
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18.8 Percentage of Dose
Standard Deviation 3.3
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PRIMARY outcome
Timeframe: Period 1: Day -1 to maximum Day 21; Period 2: Day 1 to maximum Day 3Population: Analysis population included all participants who received 1 dose of \[14C\]PF-06865571 and who have evaluable total radioactivity concentration (urinary and fecal) data and who had no protocol deviations or AEs (such as vomiting of the dose, diarrhoea or severe constipation) that may have affected the extent of excretion analysis.
The total recovery of radioactivity in the combination of urine and feces was listed and summarized using descriptive statistics. In this outcome measure, the percentages of dose excreted in total excreta (urine + feces) in Period 1 and Period 2 were reported.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
n=6 Participants
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
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|---|---|---|
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Total Recovery of Radioactivity in Total Excreta (Urine + Feces) as Percentage of Total Radioactive Dose of PF-06865571 Administered
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79.0 Percentage of Dose
Standard Deviation 16.7
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70.3 Percentage of Dose
Standard Deviation 15.1
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PRIMARY outcome
Timeframe: Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)Population: Analysis population included all participants assigned to study intervention and who took at least 1 dose of study intervention.
Plasma samples were analyzed for radiolabeled PF-06865571 and its metabolites. \[14C\]PF-06865571 and the major metabolites in plasma, after oral administration of 300 mg \[14C\]PF-06865571 were identified. In this outcome measure, relative abundance of radiolabeled PF-06865571 in plasma based on \[14C\] quantitation was reported. The measure type was the mean value based on pooled sampling, which means blood samples from the 6 participants were pooled together and then analyzed as 1 sample, thus the confidence interval could not be calculated. Therefore, "Number" is selected as the Measure Type.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
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|---|---|---|
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Relative Abundance (Mean Value) of Radiolabeled PF-06865571 in Plasma in Period 1
|
43.8 Percentage of Radioactivity in Plasma
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—
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PRIMARY outcome
Timeframe: Period 1: 0, 0.5, 3, 6, 12, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)Population: Analysis population included all participants assigned to study intervention and who took at least 1 dose of study intervention.
Plasma samples were analyzed for radiolabeled PF-06865571 and its metabolites. \[14C\]PF-06865571 and the major metabolites in plasma, after oral administration of 300 mg \[14C\]PF-06865571 were identified. In this outcome measure, relative abundance of the metabolites of \[14C\]PF-06865571 in plasma based on \[14C\] quantitation was reported. The metabolites included 487, 391, 412, 556, M6 (PF-07822633), M7 (PF-07911964), 584, M1 (PF-06878236), 426, M4 (PF-06887477), 600, M5 (PF-06885984) and M2 (PF-06868609). The measure type was the mean value based on pooled sampling, which means blood samples from the 6 participants were pooled together and then analyzed as 1 sample, thus the confidence interval could not be calculated. Therefore, "Number" is selected as the Measure Type.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
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|---|---|---|
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Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1
487
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0 Percentage of Radioactivity in Plasma
|
—
|
|
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1
391
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3.0 Percentage of Radioactivity in Plasma
|
—
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Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1
412
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0 Percentage of Radioactivity in Plasma
|
—
|
|
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1
556
|
2.7 Percentage of Radioactivity in Plasma
|
—
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Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1
M6 (PF-07822633)
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11.3 Percentage of Radioactivity in Plasma
|
—
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Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1
M7 (PF-07911964)
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0.01 Percentage of Radioactivity in Plasma
|
—
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Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1
584
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1.1 Percentage of Radioactivity in Plasma
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—
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Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1
M1 (PF-06878236)
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0 Percentage of Radioactivity in Plasma
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—
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Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1
426
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1.5 Percentage of Radioactivity in Plasma
|
—
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|
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1
M4 (PF-06887477)
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1.5 Percentage of Radioactivity in Plasma
|
—
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|
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1
600
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0 Percentage of Radioactivity in Plasma
|
—
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Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1
M5 (PF-06885984)
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0 Percentage of Radioactivity in Plasma
|
—
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Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1
M2 (PF-06868609)
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36.6 Percentage of Radioactivity in Plasma
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—
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PRIMARY outcome
Timeframe: Period 1: Day -1 to maximum Day 21Population: Analysis population included all participants assigned to study intervention and who took at least 1 dose of study intervention.
Urine samples were analyzed for radiolabeled PF-06865571 and its metabolites. \[14C\]PF-06865571 and the major metabolites in urine, after oral administration of 300 mg \[14C\]PF-06865571 were identified. In this outcome measure, relative abundance of radiolabeled PF-06865571 in urine based on \[14C\] quantitation was reported. The measure type was the mean value based on pooled sampling, which means blood samples from the 6 participants were pooled together and then analyzed as 1 sample, thus the confidence interval could not be calculated. Therefore, "Number" is selected as the Measure Type.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
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|---|---|---|
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Relative Abundance (Mean Value) of Radiolabeled PF-06865571 in Urine in Period 1
|
2.7 Percentage of Radioactivity in Urine
|
—
|
PRIMARY outcome
Timeframe: Period 1: Day -1 to maximum Day 21Population: Analysis population included all participants assigned to study intervention and who took at least 1 dose of study intervention.
Urine samples were analyzed for radiolabeled PF-06865571 and its metabolites. \[14C\]PF-06865571 and the major metabolites in urine, after oral administration of 300 mg \[14C\]PF-06865571 were identified. In this outcome measure, relative abundance of the metabolites of \[14C\]PF-06865571 in urine based on \[14C\] quantitation was reported. The metabolites included 487, 391, 412, 556, M6 (PF-07822633), M7 (PF-07911964), 584, M1 (PF-06878236), 426, M4 (PF-06887477), 600, M5 (PF-06885984) and M2 (PF-06868609). The measure type was the mean value based on pooled sampling, which means blood samples from the 6 participants were pooled together and then analyzed as 1 sample, thus the confidence interval could not be calculated. Therefore, "Number" is selected as the Measure Type.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
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|---|---|---|
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Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1
487
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2.0 Percentage of Radioactivity in Urine
|
—
|
|
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1
391
|
6.0 Percentage of Radioactivity in Urine
|
—
|
|
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1
412
|
0 Percentage of Radioactivity in Urine
|
—
|
|
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1
556
|
4.7 Percentage of Radioactivity in Urine
|
—
|
|
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1
M6 (PF-07822633)
|
23.3 Percentage of Radioactivity in Urine
|
—
|
|
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1
M7 (PF-07911964)
|
23.3 Percentage of Radioactivity in Urine
|
—
|
|
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1
584
|
23.3 Percentage of Radioactivity in Urine
|
—
|
|
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1
M1 (PF-06878236)
|
0.7 Percentage of Radioactivity in Urine
|
—
|
|
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1
426
|
4.2 Percentage of Radioactivity in Urine
|
—
|
|
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1
M4 (PF-06887477)
|
4.2 Percentage of Radioactivity in Urine
|
—
|
|
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1
600
|
1.4 Percentage of Radioactivity in Urine
|
—
|
|
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1
M5 (PF-06885984)
|
1.4 Percentage of Radioactivity in Urine
|
—
|
|
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1
M2 (PF-06868609)
|
50.9 Percentage of Radioactivity in Urine
|
—
|
PRIMARY outcome
Timeframe: Period 1: Day -1 to maximum Day 21Population: Analysis population included all participants assigned to study intervention and who took at least 1 dose of study intervention.
Fecal samples were analyzed for radiolabeled PF-06865571 and its metabolites. \[14C\]PF-06865571 and the major metabolites in feces, after oral administration of 300 mg \[14C\]PF-06865571 were identified. In this outcome measure, relative abundance of radiolabeled PF-06865571 in feces based on \[14C\] quantitation was reported. The measure type was the mean value based on pooled sampling, which means blood samples from the 6 participants were pooled together and then analyzed as 1 sample, thus the confidence interval could not be calculated. Therefore, "Number" is selected as the Measure Type.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
|
|---|---|---|
|
Relative Abundance (Mean Value) of Radiolabeled PF-06865571 in Feces in Period 1
|
4.1 Percentage of Radioactivity in Feces
|
—
|
PRIMARY outcome
Timeframe: Period 1: Day -1 to maximum Day 21Population: Analysis population included all participants assigned to study intervention and who took at least 1 dose of study intervention.
Fecal samples were analyzed for radiolabeled PF-06865571 and its metabolites. \[14C\]PF-06865571 and the major metabolites in feces, after oral administration of 300 mg \[14C\]PF-06865571 were identified. In this outcome measure, relative abundance of the metabolites of \[14C\]PF-06865571 in feces based on \[14C\] quantitation was reported. The metabolites included 487, 391, 412, 556, M6 (PF-07822633), M7 (PF-07911964), 584, M1 (PF-06878236), 426, M4 (PF-06887477), 600, M5 (PF-06885984) and M2 (PF-06868609). The measure type was the mean value based on pooled sampling, which means blood samples from the 6 participants were pooled together and then analyzed as 1 sample, thus the confidence interval could not be calculated. Therefore, "Number" is selected as the Measure Type.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
|
|---|---|---|
|
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1
487
|
0 Percentage of Radioactivity in Feces
|
—
|
|
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1
391
|
0 Percentage of Radioactivity in Feces
|
—
|
|
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1
412
|
1.1 Percentage of Radioactivity in Feces
|
—
|
|
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1
556
|
0 Percentage of Radioactivity in Feces
|
—
|
|
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1
M6 (PF-07822633)
|
0 Percentage of Radioactivity in Feces
|
—
|
|
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1
M7 (PF-07911964)
|
21.0 Percentage of Radioactivity in Feces
|
—
|
|
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1
584
|
0 Percentage of Radioactivity in Feces
|
—
|
|
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1
M1 (PF-06878236)
|
15.0 Percentage of Radioactivity in Feces
|
—
|
|
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1
426
|
33.2 Percentage of Radioactivity in Feces
|
—
|
|
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1
M4 (PF-06887477)
|
33.2 Percentage of Radioactivity in Feces
|
—
|
|
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1
600
|
0 Percentage of Radioactivity in Feces
|
—
|
|
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1
M5 (PF-06885984)
|
0 Percentage of Radioactivity in Feces
|
—
|
|
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1
M2 (PF-06868609)
|
23.1 Percentage of Radioactivity in Feces
|
—
|
SECONDARY outcome
Timeframe: Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.
AUClast is defined as area under the plasma concentration-time profile from time zero to time of the last quantifiable concentration (Clast). The determination method of AUClast was linear/log trapezoidal rule.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
|
|---|---|---|
|
Area Under the Plasma Concentration-time Profile From Time Zero to Time of The Last Quantifiable Concentration (AUClast) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1
|
20080 ngEq*hr/mL (ngEq = nanogram equivalent)
Geometric Coefficient of Variation 15
|
—
|
SECONDARY outcome
Timeframe: Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.
Cmax is defined as maximum plasma concentration. The determination method of Cmax was observing directly from data.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
|
|---|---|---|
|
Maximum Plasma Concentration (Cmax) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1
|
4417 ngEq/mL (nanogram-equivalent/milliliter)
Geometric Coefficient of Variation 10
|
—
|
SECONDARY outcome
Timeframe: Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.
Tmax is defined as time to reach maximum observed plasma concentration. The determination method of Tmax was observing directly from data as time of first occurrence.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
|
|---|---|---|
|
Time for Cmax (Tmax) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1
|
3.00 hr (hours)
Interval 3.0 to 4.0
|
—
|
SECONDARY outcome
Timeframe: Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.
AUCinf = Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0-inf). The determination method of AUCinf was AUClast + (Clast\*/ kel), where Clast\* was the predicted plasma concentration at the last quantifiable time point estimated from the log-linear regression analysis, kel was the terminal phase rate constant.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
|
|---|---|---|
|
Area Under the Plasma Concentration Time Profile From Time Zero Extrapolated to Infinite Time (AUCinf) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1
|
20400 ngEq*hr/mL
Geometric Coefficient of Variation 15
|
—
|
SECONDARY outcome
Timeframe: Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.
Terminal elimination half-life (t1/2) was the time measured for the plasma concentration to decrease by one half. The determination method of t1/2 was loge(2)/kel, where kel was the terminal phase rate constant calculated by a linear regression of the log-linear concentration-time curve.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
|
|---|---|---|
|
Terminal Elimination Half-life (t1/2) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1
|
3.622 hr
Standard Deviation 1.9605
|
—
|
SECONDARY outcome
Timeframe: Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)Population: Analysis population included all participants treated who had at least one of the PF-06895571 PK parameters of interest.
AUClast is defined as area under the plasma concentration-time profile from time zero to time of the last quantifiable concentration (Clast). The determination method of AUClast was linear/log trapezoidal rule.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
|
|---|---|---|
|
AUClast of Oral PF-06865571 in Plasma in Period 1
|
7962 ng*hr/mL (nanogram*hour per milliliter)
Geometric Coefficient of Variation 19
|
—
|
SECONDARY outcome
Timeframe: Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)Population: Analysis population included all participants treated who had at least one of the PF-06895571 PK parameters of interest.
Cmax is defined as maximum plasma concentration. The determination method of Cmax was observing directly from data.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
|
|---|---|---|
|
Cmax of Oral PF-06865571 in Plasma in Period 1
|
2096 ng/mL (nanogram per milliliter)
Geometric Coefficient of Variation 15
|
—
|
SECONDARY outcome
Timeframe: Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)Population: Analysis population included all participants treated who had at least one of the PF-06895571 PK parameters of interest.
Tmax is defined as time to reach maximum observed plasma concentration. The determination method of Tmax was observing directly from data as time of first occurrence.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
|
|---|---|---|
|
Tmax of Oral PF-06865571 in Plasma in Period 1
|
3.00 hr
Interval 2.0 to 4.0
|
—
|
SECONDARY outcome
Timeframe: Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)Population: Analysis population included all participants treated who had at least one of the PF-06895571 PK parameters of interest.
AUCinf = Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0-inf). The determination method of AUCinf was AUClast + (Clast\*/ kel), where Clast\* was the predicted plasma concentration at the last quantifiable time point estimated from the log-linear regression analysis, kel was the terminal phase rate constant.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
|
|---|---|---|
|
AUCinf of Oral PF-06865571 in Plasma in Period 1
|
7964 ng*hr/mL
Geometric Coefficient of Variation 19
|
—
|
SECONDARY outcome
Timeframe: Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)Population: Analysis population included all participants treated who had at least one of the PF-06895571 PK parameters of interest.
Terminal elimination half-life (t1/2) was the time measured for the plasma concentration to decrease by one half. The determination method of t1/2 was loge(2)/kel, where kel was the terminal phase rate constant calculated by a linear regression of the log-linear concentration-time curve.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
|
|---|---|---|
|
t1/2 of Oral PF-06865571 in Plasma in Period 1
|
6.275 hr
Standard Deviation 2.9246
|
—
|
SECONDARY outcome
Timeframe: Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.
AUClast is defined as area under the plasma concentration-time profile from time zero to time of the last quantifiable concentration (Clast). The determination method of AUClast was linear/log trapezoidal rule.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
|
|---|---|---|
|
AUClast of Intravenous (IV) Radiolabeled PF-06865571 in Plasma in Period 2
|
4.145 ng*hr/mL
Geometric Coefficient of Variation 20
|
—
|
SECONDARY outcome
Timeframe: Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.
Cmax is defined as maximum plasma concentration. The determination method of Cmax was observing directly from data.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
|
|---|---|---|
|
Cmax of IV Radiolabeled PF-06865571 in Plasma in Period 2
|
2.893 ng/mL
Geometric Coefficient of Variation 13
|
—
|
SECONDARY outcome
Timeframe: Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.
Tmax is defined as time to reach maximum observed plasma concentration. The determination method of Tmax was observing directly from data as time of first occurrence.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
|
|---|---|---|
|
Tmax of IV Radiolabeled PF-06865571 in Plasma in Period 2
|
0.250 hr
Interval 0.167 to 0.25
|
—
|
SECONDARY outcome
Timeframe: Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.
Terminal elimination half-life (t1/2) was the time measured for the plasma concentration to decrease by one half. The determination method of t1/2 was loge(2)/kel, where kel was the terminal phase rate constant calculated by a linear regression of the log-linear concentration-time curve.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
|
|---|---|---|
|
t1/2 of IV Radiolabeled PF-06865571 in Plasma in Period 2
|
1.232 hr
Standard Deviation 0.25664
|
—
|
SECONDARY outcome
Timeframe: Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.
AUCinf = Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0-inf). The determination method of AUCinf was AUClast + (Clast\*/ kel), where Clast\* was the predicted plasma concentration at the last quantifiable time point estimated from the log-linear regression analysis, kel was the terminal phase rate constant.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
|
|---|---|---|
|
AUCinf of IV Radiolabeled PF-06865571 in Plasma in Period 2
|
4.209 ng*hr/mL
Geometric Coefficient of Variation 19
|
—
|
SECONDARY outcome
Timeframe: Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.
CL is a quantitative measure of the rate at which a drug substance is removed from the body. The determination method of CL was dose/AUCinf.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
|
|---|---|---|
|
Systemic Clearance (CL) of IV Radiolabeled PF-06865571 in Plasma in Period 2
|
23.88 L/hr (liter per hour)
Geometric Coefficient of Variation 20
|
—
|
SECONDARY outcome
Timeframe: Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.
Volume of distribution is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired blood concentration of a drug. Vss is the apparent volume of distribution at steady-state.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
|
|---|---|---|
|
Steady State Volume of Distribution (Vss) of IV Radiolabeled PF-06865571 in Plasma in Period 2
|
38.83 L (Liters)
Geometric Coefficient of Variation 16
|
—
|
SECONDARY outcome
Timeframe: Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)Population: Analysis population included all participants treated who had at least one of the PF-06895571 PK parameters of interest.
AUCinf = Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0-inf). It is obtained from AUC (0-t) plus AUC (t-inf). AUCinf(dn) is defined as dose normalized (to 1 mg equivalent) AUCinf, which equals to AUCinf/Dose.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
|
|---|---|---|
|
Dose-Normalized AUCinf (AUCinf[dn]) of Oral Unlabeled PF-06865571 in Plasma in Period 2
|
31.46 ng*hr/mL/mg
Geometric Coefficient of Variation 21
|
—
|
SECONDARY outcome
Timeframe: Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.
AUCinf = Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0-inf). It is obtained from AUC (0-t) plus AUC (t-inf). AUCinf(dn) is defined as dose normalized (to 1 mg equivalent) AUCinf, which equals to AUCinf/Dose.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
|
|---|---|---|
|
AUCinf(dn) of IV Microtracer of Radiolabeled PF-06865571 in Plasma in Period 2
|
41.92 ng*hr/mL/mg
Geometric Coefficient of Variation 20
|
—
|
SECONDARY outcome
Timeframe: Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)Population: Analysis population included all participants treated who had at least one of the PF-06895571 PK parameters of interest and at least one of the 14C parameters of interest.
Absolute Oral Bioavailability (F) provided information on the amount of PF-06865571 reaching the systemic circulation. F was estimated as the ratio of adjusted geometric means of dose-normalized AUCinf for oral unlabeled PF-06865571 and IV labeled 14C PF-06865571 in plasma (from Period 2 only) which was equivalent to the following equation: F = \[PF-06865571\_AUCpo/\[14C\]PF-06865571\_AUCiv\]×\[ \[14C\]PF-06865571\_Doseiv/ PF-06865571\_Dosepo\], where PF-06865571\_AUCpo = AUCinf(dn) of oral unlabeled PF-06865571, \[14C\]PF-06865571\_AUCiv = AUCinf(dn) of intravenous radiolabeled PF-06865571, \[14C\]PF-06865571\_Doseiv = dose of intravenous radiolabeled PF-06865571, PF-06865571\_Dosepo = dose of oral unlabeled PF-06865571.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
|
|---|---|---|
|
Absolute Oral Bioavailability (F) of Oral Unlabeled and IV Radiolabeled PF-06865571 for Plasma AUCinf(dn) in Period 2
|
75.06 Percent
Interval 71.06 to 79.29
|
—
|
SECONDARY outcome
Timeframe: Period 1: up to 48 hours post-dose (Day 1 to Day 3)Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.
%14C\_Urine\_PO is defined as percentage of the radioactive dose administered that is excreted in the urine following oral administration. %14C\_Urine\_PO = Total 14C\_Urine\_PO/14C Dosepo × 100, where PO = orally, Total 14C\_Urine\_PO = total radioactivity excreted into the urine post-dose following oral administration of \[14C\]PF-06865571, 14C Dosepo = dose of 14C following oral administration of \[14C\]PF-06865571.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
|
|---|---|---|
|
Percentage of Total 14C in Urine Following Oral Administration (%14C_Urine_PO) of Radiolabeled PF-06865571 in Period 1
|
45.92 Percentage of Total 14C
Geometric Coefficient of Variation 44
|
—
|
SECONDARY outcome
Timeframe: Period 2: up to 48 hours post-dose (Day 1 to Day 3)Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.
%14C\_Urine\_IV is defined as percentage of the radioactive dose administered that is excreted in the urine following IV administration. %14C\_Urine\_IV = Total 14C \_Urine\_IV/14C Doseiv × 100, where IV = intravenous, Total 14C\_Urine\_IV = total radioactivity excreted into the urine following IV administration of \[14C\]PF 06865571, 14C Doseiv = dose of 14C following IV administration of \[14C\]PF 06865571.
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
|
|---|---|---|
|
Percentage of Total 14C in Urine Following IV Microtracer Administration (%14C_Urine_IV) of Radiolabeled PF-06865571 in Period 2
|
49.50 Percentage of Total 14C
Geometric Coefficient of Variation 44
|
—
|
SECONDARY outcome
Timeframe: Period 1 and Period 2: up to 48 hours post-dose (Day 1 to Day 3)Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.
Determination of the Fraction Absorbed (Fa) (obtained from Periods 1 and 2) provided information on the fraction of the total PF-06865571 dose absorbed, regardless of the fate of that dose after absorption (ie, metabolism, degradation, etc). Fa was estimated as the ratio of the adjusted geometric means of % of administered radioactive dose excreted into the urine following oral and IV administration of \[14C\]PF-06865571 microtracer dose over the same collection time (up to 48 hours post dose) in Periods 1 and 2, respectively: Fa = \[% 14C\_Urine\_PO/% 14C\_Urine\_IV\].
Outcome measures
| Measure |
[14C]PF-06865571 300 mg Oral
n=6 Participants
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
|
|---|---|---|
|
Fraction Absorbed (Fa) for Percentage of Excretion of Total 14C in Urine for Oral and IV Radiolabeled PF-06865571
|
92.78 Percent
Interval 62.07 to 138.68
|
—
|
Adverse Events
[14C] PF-06865571 300 mg Oral
PF-06865571 300 mg Oral & [14C] PF-06865571 100 μg IV
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
[14C] PF-06865571 300 mg Oral
n=6 participants at risk
An oral single-dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered on Day 1 in Period 1.
|
PF-06865571 300 mg Oral & [14C] PF-06865571 100 μg IV
n=6 participants at risk
An oral single-dose of 300 mg unlabeled PF-06865571 followed by an IV dose of 300 nCi \[14C\] in 100 μg of PF-06865571 (at around 3 hours post oral dose) was administered on Day 1 in Period 2. The \[14C\] IV dose was administered as an infusion over approximately 15 minutes.
|
|---|---|---|
|
Eye disorders
Conjunctivitis allergic
|
16.7%
1/6 • For Period 1, adverse events were assessed from Baseline up to Day 21. For Period 2, adverse events were assessed from Baseline up to Day 21, followed by one follow-up phone call for each participant which occurred at least 28 days and up to 35 days after the last dose of PF-06865571.
The same event may appear as both an AE and an SAE. An event may be categorized as serious in one participant and as non-serious in another participant, or one participant may have experienced both a serious and nonserious event during the study. Total number at risk below refers to the number of participants evaluable for SAEs or AEs.
|
0.00%
0/6 • For Period 1, adverse events were assessed from Baseline up to Day 21. For Period 2, adverse events were assessed from Baseline up to Day 21, followed by one follow-up phone call for each participant which occurred at least 28 days and up to 35 days after the last dose of PF-06865571.
The same event may appear as both an AE and an SAE. An event may be categorized as serious in one participant and as non-serious in another participant, or one participant may have experienced both a serious and nonserious event during the study. Total number at risk below refers to the number of participants evaluable for SAEs or AEs.
|
|
Gastrointestinal disorders
Diarrhoea
|
33.3%
2/6 • For Period 1, adverse events were assessed from Baseline up to Day 21. For Period 2, adverse events were assessed from Baseline up to Day 21, followed by one follow-up phone call for each participant which occurred at least 28 days and up to 35 days after the last dose of PF-06865571.
The same event may appear as both an AE and an SAE. An event may be categorized as serious in one participant and as non-serious in another participant, or one participant may have experienced both a serious and nonserious event during the study. Total number at risk below refers to the number of participants evaluable for SAEs or AEs.
|
0.00%
0/6 • For Period 1, adverse events were assessed from Baseline up to Day 21. For Period 2, adverse events were assessed from Baseline up to Day 21, followed by one follow-up phone call for each participant which occurred at least 28 days and up to 35 days after the last dose of PF-06865571.
The same event may appear as both an AE and an SAE. An event may be categorized as serious in one participant and as non-serious in another participant, or one participant may have experienced both a serious and nonserious event during the study. Total number at risk below refers to the number of participants evaluable for SAEs or AEs.
|
|
Renal and urinary disorders
Urine abnormality
|
16.7%
1/6 • For Period 1, adverse events were assessed from Baseline up to Day 21. For Period 2, adverse events were assessed from Baseline up to Day 21, followed by one follow-up phone call for each participant which occurred at least 28 days and up to 35 days after the last dose of PF-06865571.
The same event may appear as both an AE and an SAE. An event may be categorized as serious in one participant and as non-serious in another participant, or one participant may have experienced both a serious and nonserious event during the study. Total number at risk below refers to the number of participants evaluable for SAEs or AEs.
|
0.00%
0/6 • For Period 1, adverse events were assessed from Baseline up to Day 21. For Period 2, adverse events were assessed from Baseline up to Day 21, followed by one follow-up phone call for each participant which occurred at least 28 days and up to 35 days after the last dose of PF-06865571.
The same event may appear as both an AE and an SAE. An event may be categorized as serious in one participant and as non-serious in another participant, or one participant may have experienced both a serious and nonserious event during the study. Total number at risk below refers to the number of participants evaluable for SAEs or AEs.
|
|
Respiratory, thoracic and mediastinal disorders
Throat irritation
|
16.7%
1/6 • For Period 1, adverse events were assessed from Baseline up to Day 21. For Period 2, adverse events were assessed from Baseline up to Day 21, followed by one follow-up phone call for each participant which occurred at least 28 days and up to 35 days after the last dose of PF-06865571.
The same event may appear as both an AE and an SAE. An event may be categorized as serious in one participant and as non-serious in another participant, or one participant may have experienced both a serious and nonserious event during the study. Total number at risk below refers to the number of participants evaluable for SAEs or AEs.
|
0.00%
0/6 • For Period 1, adverse events were assessed from Baseline up to Day 21. For Period 2, adverse events were assessed from Baseline up to Day 21, followed by one follow-up phone call for each participant which occurred at least 28 days and up to 35 days after the last dose of PF-06865571.
The same event may appear as both an AE and an SAE. An event may be categorized as serious in one participant and as non-serious in another participant, or one participant may have experienced both a serious and nonserious event during the study. Total number at risk below refers to the number of participants evaluable for SAEs or AEs.
|
|
Respiratory, thoracic and mediastinal disorders
Upper-airway cough syndrome
|
16.7%
1/6 • For Period 1, adverse events were assessed from Baseline up to Day 21. For Period 2, adverse events were assessed from Baseline up to Day 21, followed by one follow-up phone call for each participant which occurred at least 28 days and up to 35 days after the last dose of PF-06865571.
The same event may appear as both an AE and an SAE. An event may be categorized as serious in one participant and as non-serious in another participant, or one participant may have experienced both a serious and nonserious event during the study. Total number at risk below refers to the number of participants evaluable for SAEs or AEs.
|
0.00%
0/6 • For Period 1, adverse events were assessed from Baseline up to Day 21. For Period 2, adverse events were assessed from Baseline up to Day 21, followed by one follow-up phone call for each participant which occurred at least 28 days and up to 35 days after the last dose of PF-06865571.
The same event may appear as both an AE and an SAE. An event may be categorized as serious in one participant and as non-serious in another participant, or one participant may have experienced both a serious and nonserious event during the study. Total number at risk below refers to the number of participants evaluable for SAEs or AEs.
|
|
Skin and subcutaneous tissue disorders
Dermatitis contact
|
16.7%
1/6 • For Period 1, adverse events were assessed from Baseline up to Day 21. For Period 2, adverse events were assessed from Baseline up to Day 21, followed by one follow-up phone call for each participant which occurred at least 28 days and up to 35 days after the last dose of PF-06865571.
The same event may appear as both an AE and an SAE. An event may be categorized as serious in one participant and as non-serious in another participant, or one participant may have experienced both a serious and nonserious event during the study. Total number at risk below refers to the number of participants evaluable for SAEs or AEs.
|
0.00%
0/6 • For Period 1, adverse events were assessed from Baseline up to Day 21. For Period 2, adverse events were assessed from Baseline up to Day 21, followed by one follow-up phone call for each participant which occurred at least 28 days and up to 35 days after the last dose of PF-06865571.
The same event may appear as both an AE and an SAE. An event may be categorized as serious in one participant and as non-serious in another participant, or one participant may have experienced both a serious and nonserious event during the study. Total number at risk below refers to the number of participants evaluable for SAEs or AEs.
|
|
Skin and subcutaneous tissue disorders
Pruritus
|
16.7%
1/6 • For Period 1, adverse events were assessed from Baseline up to Day 21. For Period 2, adverse events were assessed from Baseline up to Day 21, followed by one follow-up phone call for each participant which occurred at least 28 days and up to 35 days after the last dose of PF-06865571.
The same event may appear as both an AE and an SAE. An event may be categorized as serious in one participant and as non-serious in another participant, or one participant may have experienced both a serious and nonserious event during the study. Total number at risk below refers to the number of participants evaluable for SAEs or AEs.
|
0.00%
0/6 • For Period 1, adverse events were assessed from Baseline up to Day 21. For Period 2, adverse events were assessed from Baseline up to Day 21, followed by one follow-up phone call for each participant which occurred at least 28 days and up to 35 days after the last dose of PF-06865571.
The same event may appear as both an AE and an SAE. An event may be categorized as serious in one participant and as non-serious in another participant, or one participant may have experienced both a serious and nonserious event during the study. Total number at risk below refers to the number of participants evaluable for SAEs or AEs.
|
|
Vascular disorders
Flushing
|
16.7%
1/6 • For Period 1, adverse events were assessed from Baseline up to Day 21. For Period 2, adverse events were assessed from Baseline up to Day 21, followed by one follow-up phone call for each participant which occurred at least 28 days and up to 35 days after the last dose of PF-06865571.
The same event may appear as both an AE and an SAE. An event may be categorized as serious in one participant and as non-serious in another participant, or one participant may have experienced both a serious and nonserious event during the study. Total number at risk below refers to the number of participants evaluable for SAEs or AEs.
|
0.00%
0/6 • For Period 1, adverse events were assessed from Baseline up to Day 21. For Period 2, adverse events were assessed from Baseline up to Day 21, followed by one follow-up phone call for each participant which occurred at least 28 days and up to 35 days after the last dose of PF-06865571.
The same event may appear as both an AE and an SAE. An event may be categorized as serious in one participant and as non-serious in another participant, or one participant may have experienced both a serious and nonserious event during the study. Total number at risk below refers to the number of participants evaluable for SAEs or AEs.
|
Additional Information
Results disclosure agreements
- Principal investigator is a sponsor employee Pfizer has the right to review disclosures, requesting a delay of less than 60 days. Investigator will postpone single center publications until after disclosure of pooled data (all sites), less than 12 months from study completion/termination at all participating sites. Investigator may not disclose previously undisclosed confidential information other than study results.
- Publication restrictions are in place
Restriction type: OTHER