Binimetinib

Binimetinib is a reversible inhibitor of mitogen-activated extracellular signal regulated kinase 1 (MEK1) and MEK2 activity. MEK proteins are upstream regulators of the extracellular signal-related kinase (ERK) pathway.

• MEKTOVI is a kinase inhibitor indicated: • in combination with encorafenib, for the treatment of patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, as detected by an FDA-approved test. ( 1.1 , 2.1 ) • in combination with encorafenib, for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) with a BRAF V600E mutation, as detected by an FDA-approved test.ICD-10: C34.90, C43.9

• None. None.contraindicated

Melanoma • Confirm the presence of BRAF V600E or V600K mutation in tumor specimens prior to the initiation of MEKTOVI. ( 2.1 ) • The recommended dose is 45 mg orally twice daily in combination with encorafenib. Take MEKTOVI with or without food. ( 2.2 ) • For patients with moderate or severe hepatic impairment the recommended dose is 30 mg orally twice daily. ( 2.4 , 8.6 ) NSCLC • Confirm the presence of BRAF V600E mutation in tumor or plasma specimens prior to initiating MEKTOVI. ( 2.1 ) • The recommended dose is 45 mg orally twice daily in combination with encorafenib. Take MEKTOVI with or without food. ( 2.2 ) 2.1 Patient Selection BRAF V600E or V600K Mutation-Positive Unresectable or Metastatic Melanoma Confirm the presence of a BRAF V600E or V600K mutation in tumor specimens prior to initiating MEKTOVI [see Clinical Studies (14) ] . Information on FDA-approved tests for the detection of BRAF V600E and V600K mutations in melanoma is available at: http://www.fda.gov/CompanionDiagnostics . BRAF V600E Mutation-Positive Metastatic Non-Small Cell Lung Cancer (NSCLC) Confirm the presence of a BRAF V600E mutation in tumor or plasma specimens prior to initiating MEKTOVI [see Clinical Studies (14.2) ] . If no mutation is detected in a plasma specimen, test tumor tissue. Information on FDA-approved tests for the detection of BRAF V600E mutations in NSCLC is available at: http://www.fda.gov/CompanionDiagnostics .

• New Primary Malignancies, Cutaneous and Non-cutaneous: Can occur when MEKTOVI is used in combination with encorafenib. Monitor patients for new malignancies prior to initiation of treatment, during treatment, and after discontinuation of treatment. ( 5.1 ) • Cardiomyopathy: Assess left ventricular ejection fraction (LVEF) before initiating treatment, after one month of treatment, then every 2 to 3 months thereafter. The safety of MEKTOVI has not been established in patients with LVEF below 50%. ( 5.2 ) • Venous Thromboembolism: Deep vein thrombosis and pulmonary embolism can occur. ( 5.3 ) • Ocular Toxicities: Serous retinopathy, retinal vein occlusion (RVO) and uveitis have occurred. Perform an ophthalmologic evaluation at regular intervals and for any visual disturbances. ( 5.4 ) • Interstitial Lung Disease (ILD): Assess new or progressive unexplained pulmonary symptoms or findings for possible ILD. ( 5.5 ) • Hepatotoxicity: Monitor liver function tests before and during treatment with MEKTOVI and encorafenib and as clinically indicated. ( 5.6 ) • Rhabdomyolysis: Monitor creatine phosphokinase and creatinine periodically and as clinically indicated. ( 5.7 ) • Hemorrhage: Major hemorrhagic events can occur in patients receiving MEKTOVI and encorafenib. ( 5.8 ) • Embryo-Fetal Toxicity: Can cause fetal harm. Advise females with reproductive potential of potential risk to the fetus and to use effective contraception.

The following adverse reactions are described elsewhere in the labeling: • New Primary Malignancies [see Warnings and Precautions (5.1) ] • Cardiomyopathy [see Warnings and Precautions (5.2) ] • Venous Thromboembolism [see Warnings and Precautions (5.3) ] • Ocular Toxicities [see Warnings and Precautions (5.4) ] • Interstitial Lung Disease [see Warnings and Precautions (5.5) ] • Hepatotoxicity [see Warnings and Precautions (5.6) ] • Rhabdomyolysis [see Warnings and Precautions (5.7) ] • Hemorrhage [see Warnings and Precautions (5.8) ] • Embryo-Fetal Toxicity [see Warnings and Precautions (5.9) ] • Risks Associated with Combination Treatment [see Warnings and Precautions (5.10) ] Melanoma: Most common adverse reactions (≥25%) for MEKTOVI, in combination with encorafenib, are fatigue, nausea, diarrhea, vomiting, and abdominal pain. ( 6.1 ) NSCLC: Most common adverse reactions (≥25%) for MEKTOVI, in combination with encorafenib, are fatigue, nausea, diarrhea, musculoskeletal pain, vomiting, abdominal pain, visual impairment, constipation, dyspnea, rash, and cough. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Pfizer Inc. at 1-800-438-1985 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

Lactation: Advise not to breastfeed. ( 8.2 ) 8.1 Pregnancy Risk Summary Based on findings from animal reproduction studies and its mechanism of action [see Clinical Pharmacology (12.1) ] , MEKTOVI can cause fetal harm when administered to a pregnant woman. There are no available clinical data on the use of MEKTOVI during pregnancy. In animal reproduction studies, oral administration of binimetinib during the period of organogenesis was embryotoxic and an abortifacient in rabbits at doses greater than or equal to those resulting in exposures approximately 5 times the human exposure at the clinical dose of 45 mg twice daily (see Data ) . Advise pregnant women and females of reproductive potential of the potential risk to a fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data In reproductive toxicity studies, administration of binimetinib to rats during the period of organogenesis resulted in maternal toxicity, decreased fetal weights and increased variations in ossification at doses ≥30 mg/kg/day (approximately 37 times the human exposure based on AUC at the recommended clinical dose of 45 mg twice daily).

Metabolism

The pharmacokinetics of binimetinib was studied in healthy subjects and patients with solid tumors. After twice-daily dosing, the accumulation is 1.5-fold and the coefficient of variation (CV%) of the area under the concentration-time curve (AUC) is <40% at steady state.

Since binimetinib is 97% bound to plasma proteins, hemodialysis is likely to be ineffective in the treatment of overdose with MEKTOVI.

• Jun 27, 2018NDANDA210498Array Biopharma Inc

1. 1Off Label Use96713%
2. 2Death79711%
3. 3Nausea7059.3%
4. 4Fatigue5927.8%
5. 5Diarrhoea5567.4%
6. 6Pyrexia5287.0%
7. 7Product Use In Unapproved Indication5216.9%
8. 8Vomiting4065.4%
9. 9Neoplasm Progression3945.2%
10. 10Rash3885.1%
11. 11Serous Retinal Detachment3334.4%
12. 12Arthralgia2212.9%
13. 13Malaise2192.9%
14. 14Decreased Appetite2172.9%
15. 15Vision Blurred2072.7%

The 10 most recently updated of 141 ClinicalTrials.gov registrations naming Binimetinib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Targeted Therapy Directed by Genetic Testing in Treating Patients With Locally Advanced or Advanced Solid Tumors, The ComboMATCH Screening Trial
  Recruiting · Phase 2 · Interventional · 2,900 enrolled · National Cancer Institute (NCI)
  NCT05564377updated 2026-06-12
• Encorafenib Plus Binimetinib for People With BRAF V600 Mutated Relapsed/Refractory HCL
  Active not recruiting · Phase 2 · Interventional · 28 enrolled · National Cancer Institute (NCI)
  NCT04324112updated 2026-06-12
• Nivolumab With Trametinib and Dabrafenib, or Encorafenib and Binimetinib in Treating Patients With BRAF Mutated Metastatic or Unresectable Stage III-IV Melanoma
  Active not recruiting · Phase 2 · Interventional · 52 enrolled · M.D. Anderson Cancer Center
  NCT02910700updated 2026-06-11
• Study of IDE196 in Patients With Solid Tumors Harboring GNAQ/11 Mutations or PRKC Fusions
  Recruiting · Phase 1 · Phase 2 · Interventional · 336 enrolled · IDEAYA Biosciences
  NCT03947385updated 2026-06-08
• Binimetinib and Encorafenib for the Treatment of Advanced Solid Tumors With Non-V600E BRAF Mutations
  Active not recruiting · Phase 2 · Interventional · 26 enrolled · University Health Network, Toronto
  NCT03839342updated 2026-06-08
• A Study to Learn About the Study Medicine Called PF-07799933 in People With Advanced Solid Tumors With BRAF Alterations.
  Recruiting · Phase 1 · Interventional · 267 enrolled · Pfizer
  NCT05355701updated 2026-06-05
• Binimetinib Encorafenib Pembrolizumab +/- Stereotactic Radiosurgery in BRAFV600 Melanoma With Brain Metastasis
  Active not recruiting · Phase 2 · Interventional · 10 enrolled · UNICANCER
  NCT04074096updated 2026-06-05
• PF-07284892 in Participants With Advanced Solid Tumors
  Terminated · Phase 1 · Interventional · 53 enrolled · Pfizer
  NCT04800822updated 2026-06-04
• Binimetinib and Imatinib for Unresectable Stage III-IV KIT-Mutant Melanoma
  Recruiting · Phase 2 · Interventional · 25 enrolled · University of California, San Francisco
  NCT04598009updated 2026-06-04
• Targeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial)
  Active not recruiting · Phase 2 · Interventional · 6,452 enrolled · National Cancer Institute (NCI)
  NCT02465060updated 2026-06-03

Frequently asked questions

How does Binimetinib work?

Binimetinib is a reversible inhibitor of mitogen-activated extracellular signal regulated kinase 1 (MEK1) and MEK2 activity. MEK proteins are upstream regulators of the extracellular signal-related kinase (ERK) pathway.

What is Binimetinib used for?

According to FDA labeling, Binimetinib carries indications including: MEKTOVI is a kinase inhibitor indicated: • in combination with encorafenib, for the treatment of patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, as detected by an FDA-approved test. ( 1.1 , 2.1 ) • in combination with encorafenib, for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) with a BRAF V600E mutation, as detected by an FDA-approved test.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Binimetinib?

Binimetinib is classified as Mitogen-activated protein kinase (MEK) inhibitors, Protein Kinase Inhibitors, Cellular Proliferation Alteration.

What are the brand names for Binimetinib?

Binimetinib is marketed under brand names including Mektovi.

What are the contraindications for Binimetinib?

Binimetinib labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.