Binimetinib

Binimetinib

Systematic (IUPAC) name
5-((4-bromo-2-fluorophenyl)amino)-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzo[d]imidazole-6-carboxamide
Clinical data
Trade names	Binimetinib
Legal status
Legal status	Investigational
Identifiers
CAS Number	606143-89-9
ATC code	none
PubChem	CID 10288191
ChemSpider	8463660
ChEMBL	CHEMBL3187723
Chemical data
Formula	C17H15BrF2N4O3
Molar mass	441.23 g/mol
SMILES CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)F)C(=O)NOCCO
InChI InChI=1S/C17H15BrF2N4O3/c1-24-8-21-16-13(24)7-10(17(26)23-27-5-4-25)15(14(16)20)22-12-3-2-9(18)6-11(12)19/h2-3,6-8,22,25H,4-5H2,1H3,(H,23,26) Key:ACWZRVQXLIRSDF-UHFFFAOYSA-N

Binimetinib (MEK162, ARRY-162) is a MEK inhibitor being developed by Array Biopharma^[1] to treat various cancers.

In 2015 it was in phase 3 clinical trials for ovarian cancer,^[2] BRAF mutant melanoma,^[3] and NRAS mutant melanoma.^[4]

In Dec 2015 the company announced that the mutant-NRAS melanoma trial was successful.^[5] In the trial, those receiving binimetinib had a median progression-free survival of 2.8 months versus 1.5 months for those on the standard dacarbazine treatment.^[6]

In April 2016 it was reported that the phase III trial for low-grade ovarian cancer was terminated due to lack of efficacy.^[7]

References

1. "Array biopharma:: Binimetinib"
2. A Study of MEK162 vs. Physician's Choice Chemotherapy in Patients With Low-grade Serous Ovarian, Fallopian Tube or Peritoneal Cancer
3. Study Comparing Combination of LGX818 Plus MEK162 Versus Vemurafenib and LGX818 Monotherapy in BRAF Mutant Melanoma (COLUMBUS)
4. Study Comparing the Efficacy of MEK162 Versus Dacarbazine in Unresectable or Metastatic NRAS Mutation-positive Melanoma
5. Array BioPharma Has Successful Trial for Cancer Drug Binimetinib. Dec 2015
6. Array BioPharma announces Phase 3 binimetinib trial meets primary endpoint for NRAS-mutant melanoma. Dec 2015
7. Array bags Phase 3 study of binimetinib in ovarian cancer; shares down 4%