Friday, April 3, 2015

Drugs in Clinical Pipeline: Binimetinib

Binimetinib [5-((4-bromo-2-fluorophenyl)amino)-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzo[d]imidazole-6-carboxamide] is an oral small-molecule MEK inhibitor. MEK is a key protein kinase in the RAS/RAF/MEK/ERK pathway, which regulates several key cellular activities including proliferation, differentiation, migration, survival and angiogenesis. Inappropriate activation of this pathway has been shown to occur in many cancers, in particular through mutations in BRAF, KRAS and NRAS.

Common Name: Binimetinib
Synonyms: MEK-162; MEK162; ARRY-162; ARRY162; ARRY 162; ARRY-438162
IUPAC Name: 5-((4-bromo-2-fluorophenyl)amino)-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzo[d]imidazole-6-carboxamide
CAS Number: 606143-89-9
Mechanism of Action: Kinase Inhibitior; MEK Inhibitor
Indication: NRAS-mutant Melanoma; Melanoma
Development Stage: Phase III
Company: Array Biopharm/Novartis

Melanoma is the fifth most common cancer among men and the seventh most common cancer among women in the United States, with 76,000 new cases and over 9,700 deaths from the disease projected in 2014. Novel therapies that target the RAS/RAF/MEK/ERK pathway have a strong scientific rationale for activity in this disease, as melanoma is often characterized by activating mutations in BRAF (approximately 40% to 60%of patients) and NRAS (15% to 20% of patients). There are presently no approved therapies specifically targeting NRAS-mutant melanoma.