Last reviewed 2026-04-20 · How we verify

Mektovi (mek162)

Mektovi works by blocking the MEK1 enzyme, which is a key player in the signaling pathway that promotes cancer cell growth.

Mektovi (mek162) is a small molecule drug developed by Array Biopharma Inc. It targets the dual specificity mitogen-activated protein kinase kinase 1 (MEK1) enzyme, which is involved in the signaling pathway that promotes cancer cell growth. Mektovi is approved to treat BRAF mutation-positive colorectal cancer, metastatic malignant melanoma, and unresectable malignant melanoma with a BRAF gene mutation. The drug is patented and has a half-life of 3.5 hours with 71% bioavailability. Key safety considerations include its potential to cause skin rash, diarrhea, and fatigue.

At a glance

Mechanism of action

Binimetinib is reversible inhibitor of mitogen-activated extracellular signal regulated kinase (MEK1) and MEK2 activity. MEK proteins are upstream regulators of the extracellular signal-related kinase (ERK) pathway. In vitro, binimetinib inhibited extracellular signal-related kinase (ERK) phosphorylation in cell-free assays as well as viability and MEK-dependent phosphorylation of BRAF-mutant human melanoma cell lines. Binimetinib also inhibited in vivo ERK phosphorylation and tumor growth in BRAF-mutant murine xenograft models.Binimetinib and encorafenib target two different kinases in the RAS/RAF/MEK/ERK pathway. Compared to either drug alone, coadministration of encorafenib and binimetinib resulted in greater anti-proliferative activity in vitro in BRAF mutation-positive cell lines and greater anti-tumor activity with respect to tumor growth inhibition in BRAF V600E mutant human melanoma xenograft studies in mice. Additionally, the combination of binimetini

Approved indications

• BRAF V600E or V600K Mutation-Positive Unresectable or Metastatic Melanoma
• BRAF V600E Mutation-Positive Metastatic NSCLC

Common side effects

• Fatigue
• Nausea
• Diarrhea
• Vomiting
• Abdominal pain
• Pyrexia
• Peripheral edema
• Hemorrhage
• Hypertension
• Rash
• Dizziness
• Visual impairment

Key clinical trials

• Testing the Combination of the Anticancer Drugs ZEN003694 and Binimetinib in Patients With Advanced/Metastatic or Unresectable Solid Tumors With RAS Alterations and Triple Negative Breast Cancer (PHASE1)
• Targeted Therapy Directed by Genetic Testing in Treating Patients With Locally Advanced or Advanced Solid Tumors, The ComboMATCH Screening Trial (PHASE2)
• Palbociclib and Binimetinib in RAS-Mutant Cancers, A ComboMATCH Treatment Trial (PHASE2)
• Study of Chemotherapy, With or Without Binimetinib in Advanced Biliary Tract Cancers in 2nd Line Setting (A ComboMATCH Treatment Trial) (PHASE2)
• A Study to Learn About the Study Medicine Called PF-07799933 in People With Advanced Solid Tumors With BRAF Alterations. (PHASE1)
• Targeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial) (PHASE2)
• Binimetinib Encorafenib Pembrolizumab +/- Stereotactic Radiosurgery in BRAFV600 Melanoma With Brain Metastasis (PHASE2)
• An Open-label Study of Encorafenib + Binimetinib in Patients With BRAFV600-mutant Non-small Cell Lung Cancer (PHASE2)

Patents

Primary sources

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Competitive intelligence

For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:

• Mektovi CI brief — competitive landscape report
• Mektovi updates RSS · CI watch RSS
• Pfizer portfolio CI