Last reviewed 2026-04-20 · How we verify

Mektovi (binimetinib)

Mektovi works by blocking a specific enzyme called MEK1, which is involved in sending signals that promote cancer cell growth.

Mektovi (binimetinib) is a small molecule drug developed by Array Biopharma Inc, targeting the dual specificity mitogen-activated protein kinase kinase 1. It is FDA-approved for treating BRAF mutation-positive colorectal cancer, metastatic malignant melanoma, and unresectable malignant melanoma with BRAF gene mutation. Mektovi is a patented medication with no generic manufacturers available. Key safety considerations include its short half-life of 3.5 hours and moderate bioavailability of 71%. The commercial status of Mektovi is patented, with Array Biopharma Inc being the current owner.

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 mutation-positive colorectal cancer
• Metastatic malignant melanoma
• Unresectable malignant melanoma with BRAF gene mutation

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

Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.

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