Cobimetinib
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.
Identifiers |
|
---|---|
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) |