Dose selection, pharmacokinetics, and pharmacodynamics of BRAF inhibitor dabrafenib (GSK2118436).

doi:10.1158/1078-0432.CCR-14-0887

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Article

Dose selection, pharmacokinetics, and pharmacodynamics of BRAF inhibitor dabrafenib (GSK2118436).

Clinical cancer research : an official journal of the American Association for Cancer Research - 1 Sept 2014

Falchook Gerald S, Long Georgina V, Kurzrock Razelle, Kim Kevin B, Arkenau H-Tobias, Brown Michael P, Hamid Omid, Infante Jeffrey R, Millward Michael, Pavlick Anna, Chin Melvin T, O'Day Steven J, Blackman Samuel C, Curtis C Martin, Lebowitz Peter, Ma Bo, Ouellet Daniele, Kefford Richard F

Abstract excerpt

PURPOSE: Dabrafenib is a selective, potent ATP-competitive inhibitor of the BRAFV600-mutant kinase that has demonstrated efficacy in clinical trials. We report the rationale for dose selection in the first-in-human study of dabrafenib, including pharmacokinetics, tissue pharmacodynamics, 2[18F]fluoro-2-deoxy-D-glucose-positron emission tomography (FDG-PET) pharmacodynamics, and dose-response relationship....

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PMID: 24958809
DOI: 10.1158/1078-0432.CCR-14-0887

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BID
BRAF

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