Trial Outcomes & Findings for A Study To Evaluate The Pharmacokinetics, Excretion, Mass Balance and Metabolism of PF-07265803 (NCT NCT05286281)
NCT ID: NCT05286281
Last Updated: 2024-03-29
Results Overview
Radioactivity excreted in urine was reported as the percentage of the administered radioactivity excreted at each time interval, cumulatively through that interval and the total percent of dose recovered in urine.
COMPLETED
PHASE1
6 participants
Predose, in intervals of 0-6, 6-12, 12-24, 24-48, 48-72, 72-96 hours postdose on Day 1, and each subsequent 24 hours interval up to discharge (maximum 14 days)
2024-03-29
Participant Flow
Participant milestones
| Measure |
[14C]PF-07265803 400 mg
Participants received a single oral dose of PF-07265803 400 mg (containing 100 μCi 14C) on Day 1. μCi = microcurie.
|
|---|---|
|
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 To Evaluate The Pharmacokinetics, Excretion, Mass Balance and Metabolism of PF-07265803
Baseline characteristics by cohort
| Measure |
[14C]PF-07265803 400 mg
n=6 Participants
Participants received a single oral dose of PF-07265803 400 mg (containing 100 μCi 14C) on Day 1.
|
|---|---|
|
Age, Continuous
|
55.3 Years
STANDARD_DEVIATION 11.74 • n=5 Participants
|
|
Age, Customized
<18
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0 Participants
n=5 Participants
|
|
Age, Customized
18-25
|
0 Participants
n=5 Participants
|
|
Age, Customized
26-35
|
0 Participants
n=5 Participants
|
|
Age, Customized
36-45
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2 Participants
n=5 Participants
|
|
Age, Customized
>45
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4 Participants
n=5 Participants
|
|
Sex/Gender, Customized
Male
|
6 Participants
n=5 Participants
|
|
Sex/Gender, Customized
Female
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0 Participants
n=5 Participants
|
|
Ethnicity (NIH/OMB)
Hispanic or Latino
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0 Participants
n=5 Participants
|
|
Ethnicity (NIH/OMB)
Not Hispanic or Latino
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6 Participants
n=5 Participants
|
|
Ethnicity (NIH/OMB)
Unknown or Not Reported
|
0 Participants
n=5 Participants
|
|
Race (NIH/OMB)
American Indian or Alaska Native
|
0 Participants
n=5 Participants
|
|
Race (NIH/OMB)
Asian
|
0 Participants
n=5 Participants
|
|
Race (NIH/OMB)
Native Hawaiian or Other Pacific Islander
|
0 Participants
n=5 Participants
|
|
Race (NIH/OMB)
Black or African American
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0 Participants
n=5 Participants
|
|
Race (NIH/OMB)
White
|
6 Participants
n=5 Participants
|
|
Race (NIH/OMB)
More than one race
|
0 Participants
n=5 Participants
|
|
Race (NIH/OMB)
Unknown or Not Reported
|
0 Participants
n=5 Participants
|
PRIMARY outcome
Timeframe: Predose, in intervals of 0-6, 6-12, 12-24, 24-48, 48-72, 72-96 hours postdose on Day 1, and each subsequent 24 hours interval up to discharge (maximum 14 days)Population: Extent of excretion population is defined as all participants who received 1 dose of \[14C\]PF-07265803 and who had evaluable total radioactivity concentration (urinary and fecal) data and who had no protocol deviations or adverse events (such as vomiting of the dose, diarrhoea or severe constipation) that might have affected the extent of excretion analysis.
Radioactivity excreted in urine was reported as the percentage of the administered radioactivity excreted at each time interval, cumulatively through that interval and the total percent of dose recovered in urine.
Outcome measures
| Measure |
[14C]PF-07265803 400 mg
n=6 Participants
Participants received a single oral dose of PF-07265803 400 mg (containing 100 μCi 14C) on Day 1.
|
|---|---|
|
Total Recovery of Radioactivity in Urine, Expressed as Percentage of Total Radioactive Dose Administered
|
13.98 Percentage of total radioactive dose
Standard Deviation 2.3111
|
PRIMARY outcome
Timeframe: Predose, in intervals of each 24 hours post dose on Day 1 up to discharge (maximum 14 days)Population: Extent of excretion population is defined as all participants who received 1 dose of \[14C\]PF-07265803 and who had evaluable total radioactivity concentration (urinary and fecal) data and who had no protocol deviations or adverse events (such as vomiting of the dose, diarrhoea or severe constipation) that might have affected the extent of excretion analysis.
Radioactivity excreted in feces was reported as the percentage of the administered radioactivity excreted at each time interval, cumulatively through that interval and the total percent of dose recovered in feces.
Outcome measures
| Measure |
[14C]PF-07265803 400 mg
n=6 Participants
Participants received a single oral dose of PF-07265803 400 mg (containing 100 μCi 14C) on Day 1.
|
|---|---|
|
Total Recovery of Radioactivity in Feces, Expressed as Percentage of Total Radioactive Dose Administered
|
74.65 Percentage of total radioactive dose
Standard Deviation 3.0842
|
PRIMARY outcome
Timeframe: Predose, in intervals of each 24 hours post dose on Day 1 up to discharge (maximum 14 days)Population: Extent of excretion population is defined as all participants who received 1 dose of \[14C\]PF-07265803 and who had evaluable total radioactivity concentration (urinary and fecal) data and who had no protocol deviations or adverse events (such as vomiting of the dose, diarrhoea or severe constipation) that might have affected the extent of excretion analysis.
Radioactivity excreted in urine and feces was reported as the percentage of the administered radioactivity excreted at each time interval, cumulatively through that interval and the total percent of dose recovered in urine and feces.
Outcome measures
| Measure |
[14C]PF-07265803 400 mg
n=6 Participants
Participants received a single oral dose of PF-07265803 400 mg (containing 100 μCi 14C) on Day 1.
|
|---|---|
|
Total Recovery of Radioactivity in Total Excretion (Urine + Feces), Expressed as Percentage of Total Radioactive Dose Administered
|
88.64 Percentage of total radioactive dose
Standard Deviation 5.0887
|
PRIMARY outcome
Timeframe: Predose, 0.5, 1, 2, 3, 4, 6, 9, 12, 24, 36, 48, 72, 96, 120 hours post dose on Day 1Population: All participants who received 1 dose of \[14C\]PF-07265803 and who had evaluable total radioactivity concentration (urinary and fecal) data and who had no protocol deviations or adverse events (such as vomiting of the dose, diarrhoea or severe constipation) that might have affected the extent of excretion analysis.
Plasma homogenates were extracted for total radioactivity, and processed samples were analyzed by HPLC with radiochemical detection for quantitation of \[14C\]PF-07265803-derived components and by HRMS for identification of PF-07265803 and metabolites after a single 400-mg (100 μCi) oral dose of \[14C\]PF-07265803. Relative abundance of the metabolites of \[14C\]PF-07265803 in plasma based on \[14C\] quantitation was reported, expressed as percentage of radioactivity. PF-07265803 and four metabolites identified/characterized in human plasma including PF-07327859, PF-07327890, PF -07327860, and des(dimethylamino)-dioxy-PF-07265803 (m/z 461) were presented below. The plasma analysis was done with a single master pool sample (individual participants pooled based on time and from these a single master pool of all participants in one tube) due to the low amount of radioactivity in the plasma, hence there would be no mean or standard deviation.
Outcome measures
| Measure |
[14C]PF-07265803 400 mg
n=6 Participants
Participants received a single oral dose of PF-07265803 400 mg (containing 100 μCi 14C) on Day 1.
|
|---|---|
|
Relative Abundance of PF-07265803 and Its Metabolites in Plasma, Expressed as Percentage of Radioactivity
PF-07265803
|
8.49 Percentage of radioactivity
|
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Relative Abundance of PF-07265803 and Its Metabolites in Plasma, Expressed as Percentage of Radioactivity
PF-07327859
|
68.27 Percentage of radioactivity
|
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Relative Abundance of PF-07265803 and Its Metabolites in Plasma, Expressed as Percentage of Radioactivity
PF-07327890
|
12.73 Percentage of radioactivity
|
|
Relative Abundance of PF-07265803 and Its Metabolites in Plasma, Expressed as Percentage of Radioactivity
PF -07327860
|
2.58 Percentage of radioactivity
|
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Relative Abundance of PF-07265803 and Its Metabolites in Plasma, Expressed as Percentage of Radioactivity
m/z 461
|
2.58 Percentage of radioactivity
|
PRIMARY outcome
Timeframe: Predose, in intervals of 0-6, 6-12, 12-24, 24-48, 48-72, 72-96 hours postdose on Day 1, and each subsequent 24 hours interval up to discharge (maximum 14 days)Population: All participants who received 1 dose of \[14C\]PF-07265803 and who had evaluable total radioactivity concentration (urinary and fecal) data and who had no protocol deviations or adverse events (such as vomiting of the dose, diarrhoea or severe constipation) that might have affected the extent of excretion analysis.
Urine homogenates were extracted for total radioactivity, and processed samples were analyzed by HPLC with radiochemical detection for quantitation of \[14C\]PF-07265803-derived components and by HRMS for identification of PF-07265803 and metabolites after a single 400-mg (100 μCi) oral dose of \[14C\]PF-07265803. In this outcome measure, relative abundance of the metabolites of \[14C\]PF-07265803 in urine based on \[14C\] quantitation was reported, expressed as percentage of radioactivity. PF-07265803 and four metabolites identified/characterized in human urine including PF-07327859, PF-07327890, PF-07327891, and des(dimethylamino)-dioxy-PF-07265803 (m/z 461) were presented below.
Outcome measures
| Measure |
[14C]PF-07265803 400 mg
n=6 Participants
Participants received a single oral dose of PF-07265803 400 mg (containing 100 μCi 14C) on Day 1.
|
|---|---|
|
Relative Abundance of PF-07265803 and Its Metabolites in Urine, Expressed as Percentage of Radioactivity
PF-07265803
|
6.86 Percentage of radioactivity
Standard Deviation 1.33
|
|
Relative Abundance of PF-07265803 and Its Metabolites in Urine, Expressed as Percentage of Radioactivity
PF-07327891
|
0.888 Percentage of radioactivity
Standard Deviation 0.754
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|
Relative Abundance of PF-07265803 and Its Metabolites in Urine, Expressed as Percentage of Radioactivity
PF-07327859
|
63.9 Percentage of radioactivity
Standard Deviation 4.89
|
|
Relative Abundance of PF-07265803 and Its Metabolites in Urine, Expressed as Percentage of Radioactivity
PF-07327890
|
11.9 Percentage of radioactivity
Standard Deviation 2.85
|
|
Relative Abundance of PF-07265803 and Its Metabolites in Urine, Expressed as Percentage of Radioactivity
m/z 461
|
1.61 Percentage of radioactivity
Standard Deviation 0.455
|
PRIMARY outcome
Timeframe: Predose, in intervals of each 24 hours post dose on Day 1 up to discharge (maximum 14 days)Population: All participants who received 1 dose of \[14C\]PF-07265803 and who had evaluable total radioactivity concentration (urinary and fecal) data and who had no protocol deviations or adverse events (such as vomiting of the dose, diarrhoea or severe constipation) that might have affected the extent of excretion analysis.
Fecal homogenates were extracted for total radioactivity, and processed samples were analyzed by HPLC with radiochemical detection for quantitation of \[14C\]PF-07265803-derived components and by HRMS for identification of PF-07265803 and metabolites after a single 400-mg (100 μCi) oral dose of \[14C\]PF-07265803. In this outcome measure, relative abundance of the metabolites of \[14C\]PF-07265803 in feces based on \[14C\] quantitation was reported, expressed as percentage of radioactivity. PF-07265803 and four metabolites identified/characterized in human urine including PF-07327859, PF-07327890, PF-07327891, and PF-07327860 were presented below.
Outcome measures
| Measure |
[14C]PF-07265803 400 mg
n=6 Participants
Participants received a single oral dose of PF-07265803 400 mg (containing 100 μCi 14C) on Day 1.
|
|---|---|
|
Relative Abundance of PF-07265803 and Its Metabolites in Feces, Expressed as Percentage of Radioactivity
PF-07265803
|
1.53 Percentage of radioactivity
Standard Deviation 1.48
|
|
Relative Abundance of PF-07265803 and Its Metabolites in Feces, Expressed as Percentage of Radioactivity
PF-07327859
|
78.1 Percentage of radioactivity
Standard Deviation 3.53
|
|
Relative Abundance of PF-07265803 and Its Metabolites in Feces, Expressed as Percentage of Radioactivity
PF-07327890
|
6.79 Percentage of radioactivity
Standard Deviation 1.94
|
|
Relative Abundance of PF-07265803 and Its Metabolites in Feces, Expressed as Percentage of Radioactivity
PF-07327891
|
6.45 Percentage of radioactivity
Standard Deviation 1.12
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|
Relative Abundance of PF-07265803 and Its Metabolites in Feces, Expressed as Percentage of Radioactivity
PF-07327860
|
1.90 Percentage of radioactivity
Standard Deviation 1.46
|
SECONDARY outcome
Timeframe: Predose, 0.5, 1, 2, 3, 4, 6, 9, 12, 24, 36, 48, 72, 96, 120 hours post dose on Day 1Population: 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 0 to time of the last quantifiable concentration (Clast). The determination method of AUClast was linear/log trapezoidal rule.
Outcome measures
| Measure |
[14C]PF-07265803 400 mg
n=6 Participants
Participants received a single oral dose of PF-07265803 400 mg (containing 100 μCi 14C) on Day 1.
|
|---|---|
|
Area Under the Plasma Concentration-Time Profile From Time 0 to Time of the Last Quantifiable Concentration (AUClast) of Total Radioactivity of [14C]PF-07265803 in Plasma
|
5345 ngEq (nanogram equivalent)*hr/mL
Geometric Coefficient of Variation 34
|
SECONDARY outcome
Timeframe: Predose, 0.5, 1, 2, 3, 4, 6, 9, 12, 24, 36, 48, 72, 96, 120 hours post dose on Day 1Population: All participants treated who had at least one of the 14C parameters of interest. Only 1 participant contributed data for this parameter of interest.
AUCinf is defined as area under the plasma concentration time profile from time zero extrapolated to infinite time.
Outcome measures
| Measure |
[14C]PF-07265803 400 mg
n=1 Participants
Participants received a single oral dose of PF-07265803 400 mg (containing 100 μCi 14C) on Day 1.
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|---|---|
|
Area Under the Plasma Concentration-Time Profile From Time 0 Extrapolated to Infinite Time (AUCinf) of Total Radioactivity of [14C]PF-07265803 in Plasma
|
6430 ngEq*hr/mL
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SECONDARY outcome
Timeframe: Predose, 0.5, 1, 2, 3, 4, 6, 9, 12, 24, 36, 48, 72, 96, 120 hours post dose on Day 1Population: All participants treated who had at least one of the 14C parameters of interest.
Cmax is defined as maximum plasma concentration. Cmax was observed directly from data.
Outcome measures
| Measure |
[14C]PF-07265803 400 mg
n=6 Participants
Participants received a single oral dose of PF-07265803 400 mg (containing 100 μCi 14C) on Day 1.
|
|---|---|
|
Maximum Plasma Concentration (Cmax) of Total Radioactivity of [14C]PF-07265803 in Plasma
|
1183 ngEq/mL (nanogram-equivalent/milliliter)
Geometric Coefficient of Variation 13
|
SECONDARY outcome
Timeframe: Predose, 0.5, 1, 2, 3, 4, 6, 9, 12, 24, 36, 48, 72, 96, 120 hours post dose on Day 1Population: All participants treated who had at least one of the 14C parameters of interest.
Tmax is defined as time for Cmax. Tmax was observed directly from data as time of first occurrence.
Outcome measures
| Measure |
[14C]PF-07265803 400 mg
n=6 Participants
Participants received a single oral dose of PF-07265803 400 mg (containing 100 μCi 14C) on Day 1.
|
|---|---|
|
Time for Cmax (Tmax) of Total Radioactivity of [14C]PF-07265803 in Plasma
|
1.000 hours
Interval 0.5 to 3.0
|
SECONDARY outcome
Timeframe: Predose, 0.5, 1, 2, 3, 4, 6, 9, 12, 24, 36, 48, 72, 96, 120 hours post dose on Day 1Population: All participants treated who had at least one of the 14C parameters of interest contributing to the summary statistics for t1/2. Only 1 participant contributed data for this parameter 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-07265803 400 mg
n=1 Participants
Participants received a single oral dose of PF-07265803 400 mg (containing 100 μCi 14C) on Day 1.
|
|---|---|
|
Terminal Elimination Half-life (t1/2) of Total Radioactivity of [14C]PF-07265803 in Plasma
|
3.24 hours
|
SECONDARY outcome
Timeframe: Predose, 0.5, 1, 2, 3, 4, 6, 9, 12, 24, 36, 48, 72, 96, 120 hours post dose on Day 1Population: All participants treated who had at least 1 of the PF- 07265803 (or its known circulating metabolites PF-07327859, PF-07327860, PF-07327890) PK parameters of interest contributing to the summary statistics for AUClast.
AUClast is defined as area under the plasma concentration-time profile from time 0 to time of the last quantifiable concentration (Clast). The determination method of AUClast was linear/log trapezoidal rule.
Outcome measures
| Measure |
[14C]PF-07265803 400 mg
n=6 Participants
Participants received a single oral dose of PF-07265803 400 mg (containing 100 μCi 14C) on Day 1.
|
|---|---|
|
AUClast of PF-07265803, PF-07327859, PF-07327860 and PF-07327890 in Plasma
PF-07265803
|
313.2 ng*hr/mL (nanogram*hour per milliliter)
Geometric Coefficient of Variation 21
|
|
AUClast of PF-07265803, PF-07327859, PF-07327860 and PF-07327890 in Plasma
PF-07327859
|
3661 ng*hr/mL (nanogram*hour per milliliter)
Geometric Coefficient of Variation 17
|
|
AUClast of PF-07265803, PF-07327859, PF-07327860 and PF-07327890 in Plasma
PF-07327860
|
828.3 ng*hr/mL (nanogram*hour per milliliter)
Geometric Coefficient of Variation 109
|
|
AUClast of PF-07265803, PF-07327859, PF-07327860 and PF-07327890 in Plasma
PF-07327890
|
855.5 ng*hr/mL (nanogram*hour per milliliter)
Geometric Coefficient of Variation 27
|
SECONDARY outcome
Timeframe: Predose, 0.5, 1, 2, 3, 4, 6, 9, 12, 24, 36, 48, 72, 96, 120 hours post dose on Day 1Population: All participants treated who had at least 1 of the PF-07265803 (or its known circulating metabolites PF-07327859, PF-07327860, PF-07327890) PK parameters of interest contributing to the summary statistics for AUCinf.
AUCinf is defined as area under the plasma concentration time profile from time zero extrapolated to infinite time. 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-07265803 400 mg
n=6 Participants
Participants received a single oral dose of PF-07265803 400 mg (containing 100 μCi 14C) on Day 1.
|
|---|---|
|
AUCinf of PF-07265803, PF-07327859, PF-07327860 and PF-07327890 in Plasma
PF-07265803
|
315.1 ng*hr/mL
Geometric Coefficient of Variation 21
|
|
AUCinf of PF-07265803, PF-07327859, PF-07327860 and PF-07327890 in Plasma
PF-07327859
|
3451 ng*hr/mL
Geometric Coefficient of Variation 16
|
|
AUCinf of PF-07265803, PF-07327859, PF-07327860 and PF-07327890 in Plasma
PF-07327860
|
1018 ng*hr/mL
Geometric Coefficient of Variation 110
|
|
AUCinf of PF-07265803, PF-07327859, PF-07327860 and PF-07327890 in Plasma
PF-07327890
|
871.7 ng*hr/mL
Geometric Coefficient of Variation 27
|
SECONDARY outcome
Timeframe: Predose, 0.5, 1, 2, 3, 4, 6, 9, 12, 24, 36, 48, 72, 96, 120 hours post dose on Day 1Population: All participants treated who had at least 1 of the PF-07265803 (or its known circulating metabolites PF-07327859, PF-07327860, PF-07327890) PK parameters of interest contributing to the summary statistics for CL/F.
CL/F is apparent clearance of PF-07265803 from plasma, for extravascular routes of administration. CL/F was calculated with dose/AUCinf.
Outcome measures
| Measure |
[14C]PF-07265803 400 mg
n=6 Participants
Participants received a single oral dose of PF-07265803 400 mg (containing 100 μCi 14C) on Day 1.
|
|---|---|
|
Apparent Clearance (CL/F) of PF-07265803 in Plasma
|
1280 L/hr (liter per hour)
Geometric Coefficient of Variation 21
|
SECONDARY outcome
Timeframe: Predose, 0.5, 1, 2, 3, 4, 6, 9, 12, 24, 36, 48, 72, 96, 120 hours post dose on Day 1Population: All participants treated who had at least 1 of the PF-07265803 (or its known circulating metabolites PF-07327859, PF-07327860, PF-07327890) PK parameters of interest contributing to the summary statistics for Vz/F.
Vz/F is apparent volume of distribution, estimated from terminal phase, for extravascular dosing. Vz/F was calculated with dose /(AUCinf\*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-07265803 400 mg
n=6 Participants
Participants received a single oral dose of PF-07265803 400 mg (containing 100 μCi 14C) on Day 1.
|
|---|---|
|
Apparent Volume (Vz/F) of PF-07265803 in Plasma
|
3158 L (liter)
Geometric Coefficient of Variation 29
|
SECONDARY outcome
Timeframe: Predose, 0.5, 1, 2, 3, 4, 6, 9, 12, 24, 36, 48, 72, 96, 120 hours post dose on Day 1Population: All participants treated who had at least 1 of the PF-07265803 (or its known circulating metabolites PF-07327859, PF-07327860, PF-07327890) PK parameters of interest contributing to the summary statistics for Cmax.
Cmax is defined as maximum plasma concentration. Cmax was observed directly from data.
Outcome measures
| Measure |
[14C]PF-07265803 400 mg
n=6 Participants
Participants received a single oral dose of PF-07265803 400 mg (containing 100 μCi 14C) on Day 1.
|
|---|---|
|
Cmax of PF-07265803, PF-07327859, PF-07327860 and PF-07327890 in Plasma
PF-07265803
|
258.6 ng/mL
Geometric Coefficient of Variation 11
|
|
Cmax of PF-07265803, PF-07327859, PF-07327860 and PF-07327890 in Plasma
PF-07327859
|
741.2 ng/mL
Geometric Coefficient of Variation 16
|
|
Cmax of PF-07265803, PF-07327859, PF-07327860 and PF-07327890 in Plasma
PF-07327860
|
22.38 ng/mL
Geometric Coefficient of Variation 58
|
|
Cmax of PF-07265803, PF-07327859, PF-07327860 and PF-07327890 in Plasma
PF-07327890
|
117.3 ng/mL
Geometric Coefficient of Variation 30
|
SECONDARY outcome
Timeframe: Predose, 0.5, 1, 2, 3, 4, 6, 9, 12, 24, 36, 48, 72, 96, 120 hours post dose on Day 1Population: All participants treated who had at least 1 of the PF-07265803 (or its known circulating metabolites PF-07327859, PF-07327860, PF-07327890) PK parameters of interest contributing to the summary statistics for Tmax.
Tmax is defined as time for maximum plasma concentration (Cmax). Tmax was observed directly from data as time of first occurrence.
Outcome measures
| Measure |
[14C]PF-07265803 400 mg
n=6 Participants
Participants received a single oral dose of PF-07265803 400 mg (containing 100 μCi 14C) on Day 1.
|
|---|---|
|
Tmax of PF-07265803, PF-07327859, PF-07327860 and PF-07327890 in Plasma
PF-07265803
|
0.5000 hr (hour)
Interval 0.5 to 0.5
|
|
Tmax of PF-07265803, PF-07327859, PF-07327860 and PF-07327890 in Plasma
PF-07327859
|
1.000 hr (hour)
Interval 1.0 to 3.0
|
|
Tmax of PF-07265803, PF-07327859, PF-07327860 and PF-07327890 in Plasma
PF-07327860
|
24.00 hr (hour)
Interval 9.0 to 24.0
|
|
Tmax of PF-07265803, PF-07327859, PF-07327860 and PF-07327890 in Plasma
PF-07327890
|
2.500 hr (hour)
Interval 2.0 to 4.0
|
SECONDARY outcome
Timeframe: Predose, 0.5, 1, 2, 3, 4, 6, 9, 12, 24, 36, 48, 72, 96, 120 hours post dose on Day 1Population: All participants treated who had at least 1 of the PF-07265803 (or its known circulating metabolites PF-07327859, PF-07327860, PF-07327890) PK parameters of interest contributing to the summary statistics for t1/2.
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-07265803 400 mg
n=6 Participants
Participants received a single oral dose of PF-07265803 400 mg (containing 100 μCi 14C) on Day 1.
|
|---|---|
|
t1/2 of PF-07265803, PF-07327859, PF-07327860 and PF-07327890 in Plasma
PF-07265803
|
1.713 hr
Standard Deviation 0.14278
|
|
t1/2 of PF-07265803, PF-07327859, PF-07327860 and PF-07327890 in Plasma
PF-07327859
|
4.985 hr
Standard Deviation 1.5148
|
|
t1/2 of PF-07265803, PF-07327859, PF-07327860 and PF-07327890 in Plasma
PF-07327860
|
14.79 hr
Standard Deviation 7.3121
|
|
t1/2 of PF-07265803, PF-07327859, PF-07327860 and PF-07327890 in Plasma
PF-07327890
|
11.97 hr
Standard Deviation 6.5779
|
SECONDARY outcome
Timeframe: From the first dose of study treatment up to 35 daysPopulation: All participants assigned to study treatment and who took at least 1 dose of study treatment.
An AE was any untoward medical occurrence in a participant who received study treatment without regard to possibility of causal relationship. Treatment-related AE was any untoward medical occurrence attributed to study treatment in a participant who received study treatment. Relatedness to study treatment was assessed by the investigator. A serious adverse event (SAE) was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. Treatment-emergent were events between first dose of study treatment and up to 35 days that were absent before treatment or that worsened relative to pretreatment state.
Outcome measures
| Measure |
[14C]PF-07265803 400 mg
n=6 Participants
Participants received a single oral dose of PF-07265803 400 mg (containing 100 μCi 14C) on Day 1.
|
|---|---|
|
Number of Participants With All-Causality and Treatment-Related Treatment-Emergent Adverse Events (TEAEs)
Number of Participants with all-causality TEAEs
|
0 Participants
|
|
Number of Participants With All-Causality and Treatment-Related Treatment-Emergent Adverse Events (TEAEs)
Number of Participants with all-causality SAEs
|
0 Participants
|
|
Number of Participants With All-Causality and Treatment-Related Treatment-Emergent Adverse Events (TEAEs)
Number of Participants with treatment-related TEAEs
|
0 Participants
|
|
Number of Participants With All-Causality and Treatment-Related Treatment-Emergent Adverse Events (TEAEs)
Number of Participants with treatment-related SAEs
|
0 Participants
|
SECONDARY outcome
Timeframe: From the first dose of study treatment up to 35 daysPopulation: All participants assigned to study treatment and who took at least 1 dose of study treatment.
Laboratory abnormalities included: Hemoglobin (HGB), hematocrit, erythrocytes (ery.) \<0.8\*lower limit of normal (LLN); ery. mean corpuscular (EMC) volume, EMC HGB, EMC HGB concentration, potassium, chloride, calcium, bicarbonate\<0.9\*LLN,\>1.1\*ULN; platelets\<0.5\*LLN,\>1.75\*upper limit of normal (ULN); leukocytes, glucose\<0.6\*LLN,\>1.5\* ULN; lymphocytes, neutrophils, protein, albumin \<0.8\*LLN,\>1.2\*ULN; basophils, eosinophils, monocytes, urate \>1.2\*ULN; bilirubin (total, direct, indirect)\>1.5\*ULN; aspartate/alanine aminotransferase, alkaline phosphatase\>3.0\*ULN; sodium \<0.95\*LLN,\>1.05\*ULN; blood urea nitrogen, creatinine \>1.3\*ULN; Urine: pH\<4.5,\>8; glucose, ketones, protein, HGB, nitrite, leukocyte esterase\>=1. Only those categories in which at least 1 participant had data were reported.
Outcome measures
| Measure |
[14C]PF-07265803 400 mg
n=6 Participants
Participants received a single oral dose of PF-07265803 400 mg (containing 100 μCi 14C) on Day 1.
|
|---|---|
|
Number of Participants With Laboratory Abnormalities Without Regard to Baseline Abnormality
EMC HGB (pg/cell) <0.9*LLN
|
1 Participants
|
|
Number of Participants With Laboratory Abnormalities Without Regard to Baseline Abnormality
Urinalysis: pH (scalar) >8
|
1 Participants
|
SECONDARY outcome
Timeframe: From the first dose of study treatment up to 35 daysPopulation: All participants assigned to study treatment and who took at least 1 dose of study treatment.
Vital signs (pulse rate, systolic and diastolic blood pressure) were obtained with participant in the supine position, after having approximately 5 minutes of rest. Clinical significance of vital signs was determined at the investigator's discretion.
Outcome measures
| Measure |
[14C]PF-07265803 400 mg
n=6 Participants
Participants received a single oral dose of PF-07265803 400 mg (containing 100 μCi 14C) on Day 1.
|
|---|---|
|
Number of Participants With Clinically Significant Vital Signs Values
|
0 Participants
|
SECONDARY outcome
Timeframe: From the first dose of study treatment up to 35 daysPopulation: All participants assigned to study treatment and who took at least 1 dose of study treatment.
Standard 12-lead ECGs utilizing limb leads were collected using an ECG machine that automatically calculated the heart rate and measures PR, QT, and QTc intervals and QRS complex. Clinical significance of vital signs was determined at the investigator's discretion.
Outcome measures
| Measure |
[14C]PF-07265803 400 mg
n=6 Participants
Participants received a single oral dose of PF-07265803 400 mg (containing 100 μCi 14C) on Day 1.
|
|---|---|
|
Number of Participants With Clinically Significant Electrocardiogram (ECG) Values
|
0 Participants
|
Adverse Events
[14C]PF-07265803 400 mg
Serious adverse events
Adverse event data not reported
Other adverse events
Adverse event data not reported
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