Trial · NCT03291288

Effect of Pexidartinib on the Way the Body Processes CYP3A4 and CYP2C9 Substrates (Pharmacokinetics)

NCT03291288, Phase 1, Completed, Daiichi Sankyo; results first posted 2020-03-19

3 sourcestrials-2026-11-12-0.5.0

Cite this record

ConductScience Library. Effect of Pexidartinib on the Way the Body Processes CYP3A4 and CYP2C9 Substrates (Pharmacokinetics). Trials, record NCT03291288. Release trials-2026-11-12-0.5.0, 12 Nov 2026. https://conductscience.org/library/trials/NCT03291288

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Trial

As registered on ClinicalTrials.gov, in the graph's capture of the registry.

Title: Effect of Pexidartinib on the Way the Body Processes CYP3A4 and CYP2C9 Substrates (Pharmacokinetics)
NCT number: NCT03291288
Status: Completed
Phases: Phase 1
Enrollment: 32 participants, actual
Lead sponsor: Daiichi Sankyo
Conditions: Drug Interaction Potential
Interventions: Tolbutamide, Midazolam, Pexidartinib
First posted: 2017-09-25
Last updated: 2021-05-14
Results first posted: 2020-03-19

Source ClinicalTrials.gov

Registered outcomes14

Each outcome the trial registered, primary first, in ClinicalTrials.gov's words.

List	Outcome	Time frame	Description
Primary	Pharmacokinetic Analysis: Maximum Concentration (Cmax) for Midazolam	Baseline to 15 days post treatment	Plasma samples for midazolam were collected at predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 24, and 48 hours (h) (±10 minutes up to 1 h, ±10% thereafter) on Days 1 to 3, and also when co-administered with pexidartinib on Days 3 (to 5) and Days 13 (to 15).
Primary	Pharmacokinetic Analysis: Maximum Concentration (Cmax) for Tolbutamide	Baseline to 15 days post treatment	Plasma samples for tolbutamide were collected at predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 24, and 48 h (±10 min up to 1 h, ±10% thereafter) on Days 1 to 3, and also when co-administered with pexidartinib on Days 3 (to 5) and Days 13 (to 15).
Primary	Pharmacokinetic Analysis: Time to Maximum Concentration (Tmax) for Midazolam	Baseline to 15 days post treatment	Plasma samples for midazolam were collected at predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 24, and 48 hours (h) (±10 minutes up to 1 h, ±10% thereafter) on Days 1 to 3, and also when co-administered with pexidartinib on Days 3 (to 5) and Days 13 (to 15).
Primary	Pharmacokinetic Analysis: Time to Maximum Concentration (Tmax) for Tolbutamide	Baseline to 15 days post treatment	Plasma samples for tolbutamide were collected at predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 24, and 48 h (±10 min up to 1 h, ±10% thereafter) on Days 1 to 3, and also when co-administered with pexidartinib on Days 3 (to 5) and Days 13 (to 15).
Primary	Pharmacokinetic Analysis: Area Under the Curve to the Last Observable Concentration (AUClast) for Midazolam	Baseline to 15 days post treatment	Plasma samples for midazolam were collected at predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 24, and 48 hours (h) (±10 minutes up to 1 h, ±10% thereafter) on Days 1 to 3, and also when co-administered with pexidartinib on Days 3 (to 5) and Days 13 (to 15).
Primary	Pharmacokinetic Analysis: Area Under the Curve to the Last Observable Concentration (AUClast) for Tolbutamide	Baseline to 15 days post treatment	Plasma samples for tolbutamide were collected at predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 24, and 48 h (±10 min up to 1 h, ±10% thereafter) on Days 1 to 3, and also when co-administered with pexidartinib on Days 3 (to 5) and Days 13 (to 15).
Primary	Overall Summary of Treatment-emergent Adverse Events	Baseline to 1 year post treatment	Adverse events that emerge during treatment, having been absent pre-treatment, or worsens relative to the pre-treatment state.
Secondary	Pharmacokinetic Analysis: Maximum Concentration (Cmax) for Pexidartinib and ZAAD-1006a Metabolite	Baseline to 13 days post treatment	Plasma samples for pexidartinib and its metabolite were collected at predose, 0.5, 1, 2, 2.5, 3, 4, 6, 8, and 10 (±1) h after the first dose on Day 3, and at steady state when co-administered with midazolam and tolbutamide on Day 13.
Secondary	Pharmacokinetic Analysis: Time to Maximum Concentration (Tmax) for Pexidartinib and ZAAD-1006a Metabolite	Baseline to 13 days post treatment	Plasma samples for pexidartinib and its metabolite were collected at predose, 0.5, 1, 2, 2.5, 3, 4, 6, 8, and 10 (±1) h after the first dose on Day 3, and at steady state when co-administered with midazolam and tolbutamide on Day 13.
Secondary	Pharmacokinetic Analysis: Area Under the Curve to the Last Observable Concentration (AUClast) for Pexidartinib and ZAAD-1006a Metabolite	Baseline to 13 days post treatment	Plasma samples for pexidartinib and its metabolite were collected at predose, 0.5, 1, 2, 2.5, 3, 4, 6, 8, and 10 (±1) h after the first dose on Day 3, and at steady state when co-administered with midazolam and tolbutamide on Day 13.

1 to 10 of 14Source ClinicalTrials.gov

See all 14 registered outcomes

Outcomes14

Each outcome the trial posted results for, in ClinicalTrials.gov's words.

Type	Outcome	Time frame	Population	Units	Measured as
PRIMARY	Pharmacokinetic Analysis: Maximum Concentration (Cmax) for Midazolam	Baseline to 15 days post treatment	Pharmacokinetic parameters were assessed in the Pharmacokinetic Evaluable population.	ng/mL	MEAN
PRIMARY	Pharmacokinetic Analysis: Maximum Concentration (Cmax) for Tolbutamide	Baseline to 15 days post treatment	Pharmacokinetic parameters were assessed in the Pharmacokinetic Evaluable population.	ng/mL	MEAN
PRIMARY	Pharmacokinetic Analysis: Time to Maximum Concentration (Tmax) for Midazolam	Baseline to 15 days post treatment	Pharmacokinetic parameters were assessed in the Pharmacokinetic Evaluable population.	hours	MEDIAN
PRIMARY	Pharmacokinetic Analysis: Time to Maximum Concentration (Tmax) for Tolbutamide	Baseline to 15 days post treatment	Pharmacokinetic parameters were assessed in the Pharmacokinetic Evaluable population.	hours	MEDIAN
PRIMARY	Pharmacokinetic Analysis: Area Under the Curve to the Last Observable Concentration (AUClast) for Midazolam	Baseline to 15 days post treatment	Pharmacokinetic parameters were assessed in the Pharmacokinetic Evaluable population.	ng*hour/mL	MEAN
PRIMARY	Pharmacokinetic Analysis: Area Under the Curve to the Last Observable Concentration (AUClast) for Tolbutamide	Baseline to 15 days post treatment	Pharmacokinetic parameters were assessed in the Pharmacokinetic Evaluable population.	ng*hour/mL	MEAN
PRIMARY	Overall Summary of Treatment-emergent Adverse Events	Baseline to 1 year post treatment	Treatment-emergent adverse events (TEAEs) were assessed in the Safety Analysis population.	Participants	COUNT_OF_PARTICIPANTS
SECONDARY	Pharmacokinetic Analysis: Maximum Concentration (Cmax) for Pexidartinib and ZAAD-1006a Metabolite	Baseline to 13 days post treatment	Pharmacokinetic parameters were assessed in the Pharmacokinetic Evaluable population.	ng/mL	MEAN
SECONDARY	Pharmacokinetic Analysis: Time to Maximum Concentration (Tmax) for Pexidartinib and ZAAD-1006a Metabolite	Baseline to 13 days post treatment	Pharmacokinetic parameters were assessed in the Pharmacokinetic Evaluable population.	hours	MEDIAN
SECONDARY	Pharmacokinetic Analysis: Area Under the Curve to the Last Observable Concentration (AUClast) for Pexidartinib and ZAAD-1006a Metabolite	Baseline to 13 days post treatment	Pharmacokinetic parameters were assessed in the Pharmacokinetic Evaluable population.	ng*hour/mL	MEAN

1 to 10 of 14Source ClinicalTrials.gov

See all 14 outcomes

Results by group50

Each measurement the trial posted, group by group, in the words and numbers it posted.

Outcome	Group	Value	Spread	Units
Pharmacokinetic Analysis: Maximum Concentration (Cmax) for Midazolam	Part 1: Midazolam Only	13.6	Standard Deviation 6.8	ng/mL
Pharmacokinetic Analysis: Maximum Concentration (Cmax) for Midazolam	Part 1: Pexidartinib + Midazolam (Cycle 1, Day 1)	12.0	Standard Deviation 4.9	ng/mL
Pharmacokinetic Analysis: Maximum Concentration (Cmax) for Midazolam	Part 1: Pexidartinib + Midazolam (Cycle 1, Day 11)	9.7	Standard Deviation 4.1	ng/mL
Pharmacokinetic Analysis: Maximum Concentration (Cmax) for Tolbutamide	Part 1: Tolbutamide Only	44400	Standard Deviation 13100	ng/mL
Pharmacokinetic Analysis: Maximum Concentration (Cmax) for Tolbutamide	Part 1: Pexidartinib + Tolbutamide (Cycle 1, Day 1)	46700	Standard Deviation 16300	ng/mL
Pharmacokinetic Analysis: Maximum Concentration (Cmax) for Tolbutamide	Part 1: Pexidartinib + Tolbutamide (Cycle 1, Day 11)	44400	Standard Deviation 12200	ng/mL
Pharmacokinetic Analysis: Time to Maximum Concentration (Tmax) for Midazolam	Part 1: Midazolam Only	0.525	Full Range 0.333 to 1.37	hours
Pharmacokinetic Analysis: Time to Maximum Concentration (Tmax) for Midazolam	Part 1: Pexidartinib + Midazolam (Cycle 1, Day 1)	0.5	Full Range 0.417 to 1.42	hours
Pharmacokinetic Analysis: Time to Maximum Concentration (Tmax) for Midazolam	Part 1: Pexidartinib + Midazolam (Cycle 1, Day 11)	0.5	Full Range 0.333 to 0.917	hours
Pharmacokinetic Analysis: Time to Maximum Concentration (Tmax) for Tolbutamide	Part 1: Tolbutamide Only	2.90	Full Range 1 to 8.2	hours

1 to 10 of 50Source ClinicalTrials.gov

See all 50 results by group

Participant flow12

How many started, completed or left each group, period by period.

Period	Milestone	Group	Participants
Drug-drug Interaction Phase	STARTED	Part 1: Drug-drug Interaction Phase	32
Drug-drug Interaction Phase	STARTED	Part 2: Pexidartinib Only	0
Drug-drug Interaction Phase	COMPLETED	Part 1: Drug-drug Interaction Phase	26
Drug-drug Interaction Phase	COMPLETED	Part 2: Pexidartinib Only	0
Drug-drug Interaction Phase	NOT COMPLETED	Part 1: Drug-drug Interaction Phase	6
Drug-drug Interaction Phase	NOT COMPLETED	Part 2: Pexidartinib Only	0
Pexidartinib Only	STARTED	Part 1: Drug-drug Interaction Phase	0
Pexidartinib Only	STARTED	Part 2: Pexidartinib Only	26
Pexidartinib Only	COMPLETED	Part 1: Drug-drug Interaction Phase	0
Pexidartinib Only	COMPLETED	Part 2: Pexidartinib Only	24

1 to 10 of 12Source ClinicalTrials.gov

See all 12 participant flow

Adverse events88

Each adverse event the trial posted, group by group: the participants affected out of those at risk.

Type	Event	Organ system	Group	Affected	At risk
other	Anemia	Blood and lymphatic system disorders	Part 1: Drug-drug Interaction Phase	5	30
other	Anemia	Blood and lymphatic system disorders	Part 2: Pexidartinib Only	4	25
other	Eye swelling	Eye disorders	Part 1: Drug-drug Interaction Phase	0	30
other	Eye swelling	Eye disorders	Part 2: Pexidartinib Only	2	25
other	Nausea	Gastrointestinal disorders	Part 1: Drug-drug Interaction Phase	3	30
other	Nausea	Gastrointestinal disorders	Part 2: Pexidartinib Only	3	25
other	Diarrhea	Gastrointestinal disorders	Part 1: Drug-drug Interaction Phase	4	30
other	Diarrhea	Gastrointestinal disorders	Part 2: Pexidartinib Only	0	25
other	Dysphagia	Gastrointestinal disorders	Part 1: Drug-drug Interaction Phase	2	30
other	Dysphagia	Gastrointestinal disorders	Part 2: Pexidartinib Only	1	25

1 to 10 of 88Source ClinicalTrials.gov

See all 88 adverse events

Adverse event totals6

The totals the trial posted for each group.

Total	Group	Affected	At risk
Total, all-cause mortality	Part 1: Drug-drug Interaction Phase	1	30
Total, all-cause mortality	Part 2: Pexidartinib Only	0	25
Total, other adverse events	Part 1: Drug-drug Interaction Phase	24	30
Total, other adverse events	Part 2: Pexidartinib Only	23	25
Total, serious adverse events	Part 1: Drug-drug Interaction Phase	5	30
Total, serious adverse events	Part 2: Pexidartinib Only	5	25

Source ClinicalTrials.gov

Papers1

The papers the trial lists on ClinicalTrials.gov.

PMID	Listed as
33289960	DERIVED

Source PubMed

Grants0

The grants NIH RePORTER links to the trial, newest funded first: NIH's, and some of AHRQ's, CDC's, FDA's and VA's. Each shows its title, principal investigators, organization and funder in its newest year.

None in this release.

Trial comparisons2

Comparisons of the trial's two groups, calculated by ConductScience from the counts it posted.

Comparison	Source
Part 1: Drug-drug Interaction Phase vs Part 2: Pexidartinib Only: deaths from any cause	Trial comparisons
Part 1: Drug-drug Interaction Phase vs Part 2: Pexidartinib Only: serious adverse events	Trial comparisons

Tests0

The ConductCognition tests this trial's registered outcomes name, as ScienceGraph matched them in trial-tests-2026-11-12-0.2.1.

None in this release.

Data dates

The day each source was copied for this release.

ClinicalTrials.gov: 2026-11-12; ClinicalTrials.gov
Results, from AACT: 2026-03-23; AACT
NIH grant links: 2026-11-13; NIH RePORTER

Sources 3

ClinicalTrials.gov's posted results, through CTTI's AACTFreely available. Acknowledgement requested
ClinicalTrials.govNo license stated
NIH RePORTER's clinical studies and project filesPublic domain

Each source's terms

ClinicalTrials.gov's posted results, through CTTI's AACTClinicalTrials.gov data via Aggregate Analysis of ClinicalTrials.gov (AACT), CTTI. CTTI makes its materials freely available and requests acknowledgement. https://aact.ctti-clinicaltrials.org/documentation/299
ClinicalTrials.govnone stated
NIH RePORTER's clinical studies and project filesPublic domain (NIH RePORTER)

ClinicalTrials.gov's data carry an international copyright outside the United States: https://clinicaltrials.gov/about-site/terms-conditions.

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