Cobimetinib

Cobimetinib
Clinical data
Pronunciation	/ˌkoʊbɪˈmɛtɪnɪb/ KOH-bim-ET-i-nib
Trade names	Cotellic
Other names	GDC-0973, XL-518
AHFS/Drugs.com	Monograph
MedlinePlus	a615057
License data	US DailyMed: Cobimetinib;
Pregnancy; category	AU: D;
Routes of; administration	By mouth
ATC code	L01EE02 (WHO) ;
Legal status
Legal status	AU: S4 (Prescription only); CA: ℞-only; UK: POM (Prescription only); US: ℞-only; EU: Rx-only; In general: ℞ (Prescription only);
Pharmacokinetic data
Bioavailability	reported from 28% to 46%
Protein binding	95%
Metabolism	Intestinal and low Liver clearance (mostly CYP3A4 oxidation and UGT2B7 glucuronidation)
Elimination half-life	44 hours (mean)
Excretion	Feces (76–77%), urine (17.9–18%) (after oral and IV administration)
Identifiers
	IUPAC name (S)-[3,4-Difluoro-2-(2-fluoro-4-iodophenylamino)phenyl] [3-hydroxy-3-(piperidin-2-yl)azetidin-1-yl] methanone;
CAS Number	934660-93-2;
PubChem CID	16222096;
IUPHAR/BPS	7626;
DrugBank	DB05239 ;
ChemSpider	17349374;
UNII	ER29L26N1X;
KEGG	D10405; D10615;
ChEBI	CHEBI:90851 ;
ChEMBL	ChEMBL2146883;
CompTox Dashboard (EPA)	DTXSID60239435 ;
Chemical and physical data
Formula	C21H21F3IN3O2
Molar mass	531.318 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1CCN[C@@H](C1)C2(CN(C2)C(=O)C3=C(C(=C(C=C3)F)F)NC4=C(C=C(C=C4)I)F)O;
	InChI InChI=1S/C21H21F3IN3O2/c22-14-6-5-13(19(18(14)24)27-16-7-4-12(25)9-15(16)23)20(29)28-10-21(30,11-28)17-3-1-2-8-26-17/h4-7,9,17,26-27,30H,1-3,8,10-11H2/t17-/m0/s1; Key:BSMCAPRUBJMWDF-KRWDZBQOSA-N;

Cobimetinib, sold under the brand name Cotellic, is an anti-cancer medication used in combination with vemurafenib (Zelboraf) alone or with both vemurafenib and atezolizumab (Tecentriq) to treat melanoma. Cobimetinib is a MEK inhibitor. Cotellic, Zelboraf, and Tecentriq are all marketed by Genentech.

The most common side effects include diarrhea, rash, nausea (feeling sick), vomiting, pyrexia (fever), photosensitivity (light sensitivity) reaction, abnormal results for certain liver function tests (increased levels of alanine aminotransferase, aspartate aminotransferase) and abnormal results for an enzyme related to muscle breakdown (creatine phosphokinase).

Cobimetinib was approved for medical use in the United States in November 2015.

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