Trial Outcomes & Findings for Effect of Low-Fat Food on Pexidartinib Pharmacokinetics in Healthy Volunteers (NCT NCT03901313)
NCT ID: NCT03901313
Last Updated: 2020-05-11
Results Overview
Mean Cmax of pexidartinib is calculated for each treatment period
Recruitment status
COMPLETED
Study phase
PHASE1
Target enrollment
24 participants
Primary outcome timeframe
Baseline, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 14, 22, 24, 28, 32, 36, 48, 54, 60, 72, 84, 96, 108, 120, 132, and 144 hours postdose
Results posted on
2020-05-11
Participant Flow
A total of 24 participants who met all inclusion criteria and no exclusion criteria were enrolled in the study.
Participant milestones
| Measure |
Sequence ABC
Healthy volunteers will receive Treatments A, then B, and then C, with a 6-day washout between treatments, during a stay at the clinic of 20 days
Treatment A - 400 mg Fasting: Single oral 400 mg (2 × 200 mg capsules) dose of pexidartinib in the morning under fasting conditions
Treatment B - 400 mg Fed: Single oral 400 mg (2 × 200 mg capsules) dose of pexidartinib in the morning within 30 minutes (min) after a low-fat standard breakfast meal
Treatment C - 200 mg Fed: Single oral 200 mg (1 × 200 mg capsule) dose of pexidartinib in the morning within 30 min after a low-fat standard breakfast meal
|
Sequence ACB
Healthy volunteers will receive Treatments A, then C, and then B, with a 6-day washout between treatments, during a stay at the clinic of 20 days
Treatment A - 400 mg Fasting: Single oral 400 mg (2 × 200 mg capsules) dose of pexidartinib in the morning under fasting conditions
Treatment B - 400 mg Fed: Single oral 400 mg (2 × 200 mg capsules) dose of pexidartinib in the morning within 30 minutes (min) after a low-fat standard breakfast meal
Treatment C - 200 mg Fed: Single oral 200 mg (1 × 200 mg capsule) dose of pexidartinib in the morning within 30 min after a low-fat standard breakfast meal
|
Sequence BAC
Healthy volunteers will receive Treatments B, then A, and then C, with a 6-day washout between treatments, during a stay at the clinic of 20 days
Treatment A - 400 mg Fasting: Single oral 400 mg (2 × 200 mg capsules) dose of pexidartinib in the morning under fasting conditions
Treatment B - 400 mg Fed: Single oral 400 mg (2 × 200 mg capsules) dose of pexidartinib in the morning within 30 minutes (min) after a low-fat standard breakfast meal
Treatment C - 200 mg Fed: Single oral 200 mg (1 × 200 mg capsule) dose of pexidartinib in the morning within 30 min after a low-fat standard breakfast meal
|
Sequence BCA
Healthy volunteers will receive Treatments B, then C, and then A, with a 6-day washout between treatments, during a stay at the clinic of 20 days
Treatment A - 400 mg Fasting: Single oral 400 mg (2 × 200 mg capsules) dose of pexidartinib in the morning under fasting conditions
Treatment B - 400 mg Fed: Single oral 400 mg (2 × 200 mg capsules) dose of pexidartinib in the morning within 30 minutes (min) after a low-fat standard breakfast meal
Treatment C - 200 mg Fed: Single oral 200 mg (1 × 200 mg capsule) dose of pexidartinib in the morning within 30 min after a low-fat standard breakfast meal
|
Sequence CAB
Healthy volunteers will receive Treatments C, then A, and then B, with a 6-day washout between treatments, during a stay at the clinic of 20 days
Treatment A - 400 mg Fasting: Single oral 400 mg (2 × 200 mg capsules) dose of pexidartinib in the morning under fasting conditions
Treatment B - 400 mg Fed: Single oral 400 mg (2 × 200 mg capsules) dose of pexidartinib in the morning within 30 minutes (min) after a low-fat standard breakfast meal
Treatment C - 200 mg Fed: Single oral 200 mg (1 × 200 mg capsule) dose of pexidartinib in the morning within 30 min after a low-fat standard breakfast meal
|
Sequence CBA
Healthy volunteers will receive Treatments C, then B, and then A, with a 6-day washout between treatments, during a stay at the clinic of 20 days
Treatment A - 400 mg Fasting: Single oral 400 mg (2 × 200 mg capsules) dose of pexidartinib in the morning under fasting conditions
Treatment B - 400 mg Fed: Single oral 400 mg (2 × 200 mg capsules) dose of pexidartinib in the morning within 30 minutes (min) after a low-fat standard breakfast meal
Treatment C - 200 mg Fed: Single oral 200 mg (1 × 200 mg capsule) dose of pexidartinib in the morning within 30 min after a low-fat standard breakfast meal
|
|---|---|---|---|---|---|---|
|
Overall Study
STARTED
|
4
|
4
|
4
|
4
|
4
|
4
|
|
Overall Study
COMPLETED
|
4
|
4
|
4
|
4
|
4
|
4
|
|
Overall Study
NOT COMPLETED
|
0
|
0
|
0
|
0
|
0
|
0
|
Reasons for withdrawal
Withdrawal data not reported
Baseline Characteristics
Effect of Low-Fat Food on Pexidartinib Pharmacokinetics in Healthy Volunteers
Baseline characteristics by cohort
| Measure |
All Participants
n=24 Participants
Healthy volunteers randomized to receive 1 of 6 sequences of Treatment A, B, and C, with a 6-day washout between treatments, during a stay at the clinic of 20 days
Treatment A - 400 mg Fasting: Single oral 400 mg (2 × 200 mg capsules) dose of pexidartinib in the morning under fasting conditions
Treatment B - 400 mg Fed: Single oral 400 mg (2 × 200 mg capsules) dose of pexidartinib in the morning within 30 minutes (min) after a low-fat standard breakfast meal
Treatment C - 200 mg Fed: Single oral 200 mg (1 × 200 mg capsule) dose of pexidartinib in the morning within 30 min after a low-fat standard breakfast meal
|
|---|---|
|
Age, Categorical
<=18 years
|
0 Participants
n=5 Participants
|
|
Age, Categorical
Between 18 and 65 years
|
24 Participants
n=5 Participants
|
|
Age, Categorical
>=65 years
|
0 Participants
n=5 Participants
|
|
Age, Continuous
|
36.6 years
STANDARD_DEVIATION 8.06 • n=5 Participants
|
|
Sex: Female, Male
Female
|
3 Participants
n=5 Participants
|
|
Sex: Female, Male
Male
|
21 Participants
n=5 Participants
|
|
Race (NIH/OMB)
American Indian or Alaska Native
|
0 Participants
n=5 Participants
|
|
Race (NIH/OMB)
Asian
|
2 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
|
12 Participants
n=5 Participants
|
|
Race (NIH/OMB)
White
|
10 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
|
|
Region of Enrollment
United States
|
24 participants
n=5 Participants
|
PRIMARY outcome
Timeframe: Baseline, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 14, 22, 24, 28, 32, 36, 48, 54, 60, 72, 84, 96, 108, 120, 132, and 144 hours postdosePopulation: Pharmacokinetic parameters were assessed in the Pharmacokinetic Analysis Set.
Mean Cmax of pexidartinib is calculated for each treatment period
Outcome measures
| Measure |
Treatment A
n=24 Participants
All healthy volunteers who received Treatment A - 400 mg Fasting: Single oral 400 mg (2 × 200 mg capsules) dose of pexidartinib in the morning under fasting conditions
|
Treatment B
n=24 Participants
All healthy volunteers who received Treatment B - 400 mg Fed: Single oral 400 mg (2 × 200 mg capsules) dose of pexidartinib in the morning within 30 minutes (min) after a low-fat standard breakfast meal
|
Treatment C
n=24 Participants
All healthy volunteers who received Treatment C - 200 mg Fed: Single oral 200 mg (1 × 200 mg capsule) dose of pexidartinib in the morning within 30 min after a low-fat standard breakfast meal
|
|---|---|---|---|
|
Maximum Observed Concentration in Plasma (Cmax) of Pexidartinib
|
4580 ng/mL
Standard Deviation 1240
|
7090 ng/mL
Standard Deviation 1590
|
3870 ng/mL
Standard Deviation 729
|
PRIMARY outcome
Timeframe: Baseline, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 14, 22, 24, 28, 32, 36, 48, 54, 60, 72, 84, 96, 108, 120, 132, and 144 hours postdosePopulation: Pharmacokinetic parameters were assessed in the Pharmacokinetic Analysis Set.
Median Tmax of pexidartinib is calculated for each treatment period
Outcome measures
| Measure |
Treatment A
n=24 Participants
All healthy volunteers who received Treatment A - 400 mg Fasting: Single oral 400 mg (2 × 200 mg capsules) dose of pexidartinib in the morning under fasting conditions
|
Treatment B
n=24 Participants
All healthy volunteers who received Treatment B - 400 mg Fed: Single oral 400 mg (2 × 200 mg capsules) dose of pexidartinib in the morning within 30 minutes (min) after a low-fat standard breakfast meal
|
Treatment C
n=24 Participants
All healthy volunteers who received Treatment C - 200 mg Fed: Single oral 200 mg (1 × 200 mg capsule) dose of pexidartinib in the morning within 30 min after a low-fat standard breakfast meal
|
|---|---|---|---|
|
Time to Cmax (Tmax)
|
2.00 hours
Interval 1.0 to 3.52
|
3.50 hours
Interval 2.5 to 10.0
|
3.30 hours
Interval 2.5 to 4.5
|
PRIMARY outcome
Timeframe: Baseline, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 14, 22, 24, 28, 32, 36, 48, 54, 60, 72, 84, 96, 108, 120, 132, and 144 hours postdosePopulation: Pharmacokinetic parameters were assessed in the Pharmacokinetic Analysis Set.
Mean AUClast and AUCinf for pexidartinib are calculated for each treatment period
Outcome measures
| Measure |
Treatment A
n=24 Participants
All healthy volunteers who received Treatment A - 400 mg Fasting: Single oral 400 mg (2 × 200 mg capsules) dose of pexidartinib in the morning under fasting conditions
|
Treatment B
n=24 Participants
All healthy volunteers who received Treatment B - 400 mg Fed: Single oral 400 mg (2 × 200 mg capsules) dose of pexidartinib in the morning within 30 minutes (min) after a low-fat standard breakfast meal
|
Treatment C
n=24 Participants
All healthy volunteers who received Treatment C - 200 mg Fed: Single oral 200 mg (1 × 200 mg capsule) dose of pexidartinib in the morning within 30 min after a low-fat standard breakfast meal
|
|---|---|---|---|
|
Area Under the Concentration-time Curve From Time of Dosing to Last Measurable Concentration (AUClast) and to Infinity (AUCinf)
AUClast
|
64800 ng*hour/mL
Standard Deviation 19300
|
102000 ng*hour/mL
Standard Deviation 26300
|
53600 ng*hour/mL
Standard Deviation 14200
|
|
Area Under the Concentration-time Curve From Time of Dosing to Last Measurable Concentration (AUClast) and to Infinity (AUCinf)
AUCinf
|
66100 ng*hour/mL
Standard Deviation 19900
|
104000 ng*hour/mL
Standard Deviation 27400
|
54600 ng*hour/mL
Standard Deviation 15000
|
PRIMARY outcome
Timeframe: Baseline, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 14, 22, 24, 28, 32, 36, 48, 54, 60, 72, 84, 96, 108, 120, 132, and 144 hours postdosePopulation: Pharmacokinetic parameters were assessed in the Pharmacokinetic Analysis Set.
Mean t1/2 for pexidartinib is calculated for each treatment period
Outcome measures
| Measure |
Treatment A
n=24 Participants
All healthy volunteers who received Treatment A - 400 mg Fasting: Single oral 400 mg (2 × 200 mg capsules) dose of pexidartinib in the morning under fasting conditions
|
Treatment B
n=24 Participants
All healthy volunteers who received Treatment B - 400 mg Fed: Single oral 400 mg (2 × 200 mg capsules) dose of pexidartinib in the morning within 30 minutes (min) after a low-fat standard breakfast meal
|
Treatment C
n=24 Participants
All healthy volunteers who received Treatment C - 200 mg Fed: Single oral 200 mg (1 × 200 mg capsule) dose of pexidartinib in the morning within 30 min after a low-fat standard breakfast meal
|
|---|---|---|---|
|
Terminal Half-life (t1/2)
|
24.2 hours
Standard Deviation 5.28
|
23.1 hours
Standard Deviation 4.68
|
23.6 hours
Standard Deviation 5.04
|
Adverse Events
Treatment A
Serious events: 0 serious events
Other events: 1 other events
Deaths: 0 deaths
Treatment B
Serious events: 0 serious events
Other events: 0 other events
Deaths: 0 deaths
Treatment C
Serious events: 0 serious events
Other events: 2 other events
Deaths: 0 deaths
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
Treatment A
n=24 participants at risk
All healthy volunteers who received Treatment A - 400 mg Fasting: Single oral 400 mg (2 × 200 mg capsules) dose of pexidartinib in the morning under fasting conditions
|
Treatment B
n=24 participants at risk
All healthy volunteers who received Treatment B - 400 mg Fed: Single oral 400 mg (2 × 200 mg capsules) dose of pexidartinib in the morning within 30 minutes (min) after a low-fat standard breakfast meal
|
Treatment C
n=24 participants at risk
All healthy volunteers who received Treatment C - 200 mg Fed: Single oral 200 mg (1 × 200 mg capsule) dose of pexidartinib in the morning within 30 min after a low-fat standard breakfast meal
|
|---|---|---|---|
|
Blood and lymphatic system disorders
Neutropenia
|
0.00%
0/24 • Adverse events were collected from study enrollment up to 28 days of administration of the last dose of study treatment.
A treatment-emergent adverse event (TEAE) was defined as an adverse event that emerged during treatment, having been absent pre-treatment, or worsened relative to the pre-treatment state.
|
0.00%
0/24 • Adverse events were collected from study enrollment up to 28 days of administration of the last dose of study treatment.
A treatment-emergent adverse event (TEAE) was defined as an adverse event that emerged during treatment, having been absent pre-treatment, or worsened relative to the pre-treatment state.
|
4.2%
1/24 • Adverse events were collected from study enrollment up to 28 days of administration of the last dose of study treatment.
A treatment-emergent adverse event (TEAE) was defined as an adverse event that emerged during treatment, having been absent pre-treatment, or worsened relative to the pre-treatment state.
|
|
Skin and subcutaneous tissue disorders
Dermatitis contact
|
0.00%
0/24 • Adverse events were collected from study enrollment up to 28 days of administration of the last dose of study treatment.
A treatment-emergent adverse event (TEAE) was defined as an adverse event that emerged during treatment, having been absent pre-treatment, or worsened relative to the pre-treatment state.
|
0.00%
0/24 • Adverse events were collected from study enrollment up to 28 days of administration of the last dose of study treatment.
A treatment-emergent adverse event (TEAE) was defined as an adverse event that emerged during treatment, having been absent pre-treatment, or worsened relative to the pre-treatment state.
|
4.2%
1/24 • Adverse events were collected from study enrollment up to 28 days of administration of the last dose of study treatment.
A treatment-emergent adverse event (TEAE) was defined as an adverse event that emerged during treatment, having been absent pre-treatment, or worsened relative to the pre-treatment state.
|
|
Skin and subcutaneous tissue disorders
Dry skin
|
4.2%
1/24 • Adverse events were collected from study enrollment up to 28 days of administration of the last dose of study treatment.
A treatment-emergent adverse event (TEAE) was defined as an adverse event that emerged during treatment, having been absent pre-treatment, or worsened relative to the pre-treatment state.
|
0.00%
0/24 • Adverse events were collected from study enrollment up to 28 days of administration of the last dose of study treatment.
A treatment-emergent adverse event (TEAE) was defined as an adverse event that emerged during treatment, having been absent pre-treatment, or worsened relative to the pre-treatment state.
|
0.00%
0/24 • Adverse events were collected from study enrollment up to 28 days of administration of the last dose of study treatment.
A treatment-emergent adverse event (TEAE) was defined as an adverse event that emerged during treatment, having been absent pre-treatment, or worsened relative to the pre-treatment state.
|
Additional Information
Contact for Clinical Trial Information
Daiichi Sankyo, Inc.
Phone: 908-992-6400
Email: [email protected]
Results disclosure agreements
- Principal investigator is a sponsor employee
- Publication restrictions are in place