Binimetinib is a medication used to treat metastatic melanoma with specific mutations. Binimetinib, also known as Mektovi, is a potent and selective oral mitogen-activated protein kinase 1/2 (MEK 1/2) inhibitor which is combined with Encorafenib.
- Mechanism
- Curator reviewed · 2 references
Binimetinib, noncompetitive with ATP, binds reversibly to and inhibits the activity of mitogen-activated extracellular signal-regulated kinase (MEK) 1 and 2. The inhibition of MEK1/2 prevents the activation of MEK1/2-dependent effector proteins and transcription factors, resulting in the inhibition of growth factor-mediated cell signaling such as the downstream extracellular signal-related kinase (ERK) pathway. This may lead to the inhibition of tumor cell proliferation and an inhibition in the production of various inflammatory cytokines including interleukin-1, -6, and tumor necrosis factor. MEK1/2 are themselves threonine and tyrosine kinases that possess a dual specificity. They subsequently contribute critically to the activation of the RAS/RAF/MEK/ERK pathway and are typically upregulated in a number of different tumor cell types.
- Primary indication
- Binimetinib, in conjunction with encorafenib, is indicated for the treatment of unresectable or metastatic melanoma with BRAF V600E or V600K mutation and metastatic non-small cell lung cancer (NSCLC) with a BRAF V600E mutation.Curator reviewed · 5 structured indications
- Formula / weight
- C17H15BrF2N4O3 · 441.233 g/mol (avg)
- First approval
- Canada, 2021 · United States, 2018 · European Union, 2020
- Code names
- ARRY-162 · ARRY-438162 · MEK-162 · NVP-MEK162 · PF-06811462
- Brand names
Resolves to
ACWZRVQXLIRSDF-UHFFFAOYSA-NSMILESCN1C=NC2=C(F)C(NC3=CC=C(Br)C=C3F)=C(C=C12)C(=O)NOCCOWhat you can answer from here — as of May 26, 2026
Which drugs share a target with Binimetinib, and which of those have an active Phase 3 trial?
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