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

Phase 1 Completed 32 enrolled Daiichi Sankyo

NaSequentialOpen-labelTreatment

Summary

This study has two parts. Part 1 will evaluate how pexidartinib affects the way the body processes CYP3A4 and CYP2C9 substrates using midazolam and tolbutamide, respectively, as probe agents. Part 2 will test the efficacy and safety of pexidartinib treatment in various tumor types. In Part 2, the same participants will continue to receive pexidartinib twice daily. Participants will be allowed to continue using pexidartinib as long as the participant derives benefit.

Timeline

Start: 2018-02-26
Primary completion: 2018-09-26
Completion: 2021-04-16

Publications

Lewis JH, Gelderblom H, van de Sande M, Stacchiotti S, Healey JH, Tap WD, Wagner AJ, Pousa AL, Druta M, Lin CC, Baba HA, Choi Y, Wang Q, Shuster DE, Bauer S. Pexidartinib Long-Term Hepatic Safety Profile in Patients with Tenosynovial Giant Cell Tumors. Oncologist. 2021 May;26(5):e863-e873. doi: 10.1002/onco.13629. Epub 2020 Dec 24.

Drugs

Evaluation	Drug	Modality	Dose	Route
Subject	Midazolam	Small molecule	2 mg	Oral
Subject	Pexidartinib	Small molecule	400 mg	—
Subject	Tolbutamide	Small molecule	500 mg	Oral

Indications

No indication recorded.