Effect of Tepotinib on PK of CYP3A Substrate Midazolam

Phase 1 Completed 12 enrolled Merck KGaA, Darmstadt, Germany

NaSequentialOpen-labelOther

Summary

The study investigated the effect of tepotinib on the pharmacokinetics (PK) of the Cytochrome P450 (CYP) 3A substrate midazolam determined from concentrations of midazolam and its main metabolite 1-hydroxymidazolam in healthy participants.

Timeline

Start: 2018-08-20
Primary completion: 2018-10-25
Completion: 2018-10-30

Outcome

Met primary endpoint

paper In clinical studies, tepotinib had no effect on the pharmacokinetics of midazolam or its metabolite 1'-hydroxymidazolam. PMID 37415001 ↗

Publications

Yalkinoglu O, Becker A, Krebs-Brown A, Vetter C, Lupfert C, Perrin D, Heuer J, Biedert H, Hirt S, Bytyqi A, Bachmann A, Strotmann R. Assessment of the potential of the MET inhibitor tepotinib to affect the pharmacokinetics of CYP3A4 and P-gp substrates. Invest New Drugs. 2023 Aug;41(4):596-605. doi: 10.1007/s10637-023-01378-z. Epub 2023 Jul 6.

Drugs

Evaluation	Drug	Modality	Dose	Route
Subject	Midazolam	Small molecule	7.5 mg	Oral
Subject	Tepotinib	Small molecule	500 mg	Oral

Indications

No indication recorded.