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Systematic (IUPAC) name

(S)-[3,4-Difluoro-2-(2-fluoro-4-iodophenylamino)phenyl][3-hydroxy-3-(piperidin-2-yl)azetidin-1-yl] methanone


Cobimetinib (trade name Cotellic) is a MEK inhibitor developed by Exelixis and Genentech. It is used in combination with vemurafenib, a BRAF inhibitor, to treat melanoma. In November 2015, the U.S. Food and Drug Administration approved cobimetinib for unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, in combination with vemurafenib(Zelboraf). Cobimetinib is not indicated for treatment of patients with wild-type BRAF melanoma.[4]

Cobimetinib in combination with vemurafenib is reportedly priced at $17,600 per month, or about $211,000 per year.[5] A competing dual therapy, using dabrafenib along with trametinib, is also approved by the FDA,[6] and is reported to cost $15,300 monthly, or $183,600 per year.


CAS Number 934660-93-2

Chemical data

Formula C21H21F3IN3O2
Molar mass 531.3 g/mol

Clinical data

Pronunciation koe-bi-me-ti-nib
Trade names Cotellic

Pharmacokinetic data

Bioavailability reported from 28%to 46%
Protein binding 95%
Metabolism Intestinal and lowhepatic clearance (mostlyCYP3A4 oxidation andUGT2B7glucuronidation)
Biological half-life 44 hours (mean)



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