Oral Bioavailability and Mass Balance Trial With Pimasertib

Phase 1 Completed 6 enrolled Merck KGaA, Darmstadt, Germany

NaSingle-groupOpen-labelTreatment

Summary

This is a Phase 1, open-label, single centered trial to evaluate the mass balance, bioavailability and metabolism of pimasertib in cancer subjects with locally advanced or metastatic solid tumors.

Timeline

Start: 2012-11-30
Primary completion: 2014-07-31
Completion: 2014-07-31

Publications

Results Scheible H, Kraetzer F, Marx A, Johne A, Wimmer E. Metabolism of the MEK1/2 Inhibitor Pimasertib Involves a Novel Conjugation with Phosphoethanolamine in Patients with Solid Tumors. Drug Metab Dispos. 2017 Feb;45(2):174-182. doi: 10.1124/dmd.116.072934. Epub 2016 Dec 1.
von Richter O, Massimini G, Scheible H, Udvaros I, Johne A. Pimasertib, a selective oral MEK1/2 inhibitor: absolute bioavailability, mass balance, elimination route, and metabolite profile in cancer patients. Br J Clin Pharmacol. 2016 Dec;82(6):1498-1508. doi: 10.1111/bcp.13078. Epub 2016 Sep 19.

Drugs

Evaluation	Drug	Modality	Dose	Route
Subject	Pimasertib	Small molecule	60 mg	Oral

Indications

No indication recorded.