binimetinib   Click here for help

GtoPdb Ligand ID: 7921

Synonyms: ARRY 162 | ARRY-162 | ARRY-438162 | MEK-162 | MEK162 | Mektovi®
Approved drug PDB Ligand
binimetinib is an approved drug (FDA and EMA (2018))
Compound class: Synthetic organic
Comment: Binimetinib is a potent non-ATP competitive inhibitor of MEK1/2 kinase activity [3] (link directly to abstract 794 online here).
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 4
Hydrogen bond donors 3
Rotatable bonds 7
Topological polar surface area 88.41
Molecular weight 440.03
XLogP 3.23
No. Lipinski's rules broken 0
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Canonical SMILES OCCONC(=O)c1cc2n(C)cnc2c(c1Nc1ccc(cc1F)Br)F
Isomeric SMILES OCCONC(=O)c1cc2n(C)cnc2c(c1Nc1ccc(cc1F)Br)F
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)
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Summary of Clinical Use Click here for help
Binimetinib received FDA approval as a treatment for advanced BRAF-mutant melanoma in June 2018. The approval is for a combination binimetinib plus the BRAF mutant kinase inhibitor, encorafenib. Results from Phase 3 clinical trial NCT01909453 which compared the combination of encorafenib plus binimetinib and encorafenib monotherapy to vemurafenib monotherapy in BRAF mutant melanoma were published in May 2018 [2]. Phase 2 trial results for melanoma are available in [1].
Clinical studies in other solid tumour types and in hematological cancers are underway. Click here to link to's full list of binimetinib (MEK162) trials.