Binimetinib

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File:Binimetinib.png
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
  • Investigational
Identifiers
CAS Number 606143-89-9
ATC code none
PubChem CID: 10288191
ChemSpider 8463660
ChEMBL CHEMBL3187723
Chemical data
Formula C17H15BrF2N4O3
Molecular mass 441.23 g/mol
  • CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)F)C(=O)NOCCO
  • 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" [1]
  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%

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