Encorafenib

Encorafenib is a kinase inhibitor that targets BRAF V600E, as well as wild-type BRAF and CRAF in in vitro cell-free assays with IC 50 values of 0.35, 0.47, and 0.3 nM, respectively. Mutations in the BRAF gene, such as BRAF V600E, can result in constitutively activated BRAF kinases that may stimulate tumor cell growth.

• BRAFTOVI is a kinase inhibitor indicated: Melanoma • in combination with binimetinib, for the treatment of patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, as detected by an FDA-authorized test. ( 1.1 , 2.1 ) Colorectal Cancer (CRC) • in combination with cetuximab and fluorouracil-based chemotherapy, for the treatment of adult patients with metastatic colorectal cancer (mCRC) with a BRAF V600E mutation, as detected by an FDA‑authorized test.ICD-10: C18.9, C43.9

• None. None.contraindicated

Melanoma • Confirm the presence of BRAF V600E or V600K mutation in tumor specimens prior to the initiation of BRAFTOVI. ( 2.1 ) • The recommended dose is 450 mg orally once daily in combination with binimetinib. ( 2.2 ) CRC • Confirm the presence of BRAF V600E mutation in plasma or tumor specimens prior to the initiation of BRAFTOVI. ( 2.1 ) • The recommended dose is 300 mg orally once daily in combination with o biweekly cetuximab and mFOLFOX6 (fluorouracil, leucovorin and oxaliplatin) or cetuximab and FOLFIRI (fluorouracil, leucovorin and irinotecan) ( 2.3 ) o weekly cetuximab ( 2.3 ) NSCLC • Confirm the presence of BRAF V600E mutation in tumor or plasma specimens prior to initiating BRAFTOVI. ( 2.1 ) • The recommended dose is 450 mg orally once daily in combination with binimetinib. ( 2.2 ) Take BRAFTOVI with or without food. ( 2.4 ) 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 BRAFTOVI [see Warnings and Precautions (5.2) , Clinical Studies (14.1) ] . Information on FDA-authorized 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 Colorectal Cancer (CRC) Confirm the presence of a BRAF V600E mutation in plasma or tumor tissue prior to initiating BRAFTOVI [see Warnings and Precautions (5.2) , Clinical Studies (14.2 , 14.3) ]. If no mutation is detected in a plasma specimen, test tumor tissue.

• New Primary Malignancies, cutaneous and noncutaneous : Can occur. Monitor for malignancies and perform dermatologic evaluations prior to, while on therapy, and following discontinuation of treatment. ( 5.1 ) • Tumor Promotion in BRAF Wild-Type Tumors : Increased cell proliferation can occur with BRAF inhibitors. ( 5.2 ) • Cardiomyopathy : Assess left ventricular ejection fraction (LVEF) before initiating treatment with BRAFTOVI and binimetinib, and after one month of treatment, then every 2 to 3 months thereafter. The safety of BRAFTOVI in combination with binimetinib has not been established in patients with LVEF below 50%. ( 5.3 ) • Hepatotoxicity : Monitor liver function tests before and during treatment with BRAFTOVI and binimetinib and as clinically indicated. ( 5.4 ) • Hemorrhage : Major hemorrhagic events can occur in patients receiving BRAFTOVI and binimetinib. ( 5.5 ) • Uveitis : Perform ophthalmologic evaluation at regular intervals and for any visual disturbances. ( 5.6 ) • QT Prolongation : Monitor electrolytes before and during treatment. Correct electrolyte abnormalities and control for cardiac risk factors for QT prolongation. Withhold BRAFTOVI for QTc of 500 ms or greater. ( 5.7 ) • Embryo-Fetal Toxicity : Can cause fetal harm. Advise females with reproductive potential of potential risk to the fetus and to use effective nonhormonal method of contraception. ( 5.8 , 8.1 , 8.3 ) • Risks Associated with BRAFTOVI as a Single Agent : If binimetinib is temporarily interrupted or permanently discontinued, reduce the dose of BRAFTOVI as recommended.

The following adverse reactions are described elsewhere in the labeling: • New Primary Malignancies [see Warnings and Precautions (5.1) ] • Tumor Promotion in BRAF Wild-Type Tumors [see Warnings and Precautions (5.2) ] • Cardiomyopathy [see Warnings and Precautions (5.3) ] • Hepatotoxicity [see Warnings and Precautions (5.4) ] • Hemorrhage [see Warnings and Precautions (5.5) ] • Uveitis [see Warnings and Precautions (5.6) ] • QT Prolongation [see Warnings and Precautions (5.7) ] • Embryo-Fetal Toxicity [see Warnings and Precautions (5.8) ] • Risks Associated with BRAFTOVI as a Single Agent [see Warnings and Precautions (5.9) ] • Risks Associated with Combination Treatment [see Warnings and Precautions (5.10) ] • Melanoma : Most common adverse reactions (≥25%) for BRAFTOVI, in combination with binimetinib, are fatigue, nausea, vomiting, abdominal pain, and arthralgia. ( 6.1 ) • CRC : Most common adverse reactions (≥25%) for BRAFTOVI, in combination with cetuximab and mFOLFOX6, are peripheral neuropathy, nausea, fatigue, diarrhea, decreased appetite, rash, vomiting, hemorrhage, abdominal pain, arthralgia, pyrexia, and constipation. ( 6.1 ) • Most common adverse reactions (≥25%) for BRAFTOVI, in combination with cetuximab and FOLFIRI are nausea, diarrhea, fatigue, vomiting, alopecia, constipation, abdominal pain, decreased appetite, and rash. ( 6.1 ) • Most common adverse reactions (≥25%) for BRAFTOVI, in combination with cetuximab, are fatigue, nausea, diarrhea, dermatitis acneiform, abdominal pain, decreased appetite, arthralgia, and rash.

• Lactation : Advise not to breastfeed. ( 8.2 ) • Males of Reproductive Potential : BRAFTOVI may impair fertility. ( 8.3 ) 8.1 Pregnancy Risk Summary Based on its mechanism of action, BRAFTOVI can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology (12.1) ] . There are no available clinical data on the use of BRAFTOVI during pregnancy. In animal reproduction studies, encorafenib produced embryo-fetal developmental changes in rats and rabbits and was an abortifacient in rabbits at doses greater than or equal to those resulting in exposures approximately 26 (in the rat) and 178 (in the rabbit) times the human exposure at the clinical dose of 450 mg, with no clear findings at lower doses (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.

Metabolism

The pharmacokinetics of encorafenib were studied in healthy subjects and patients with solid tumors, including advanced and unresectable or metastatic cutaneous melanoma harboring a BRAF V600E or V600K mutation, BRAF V600E mutation-positive metastatic CRC. After a single dose, systemic exposure of encorafenib was dose proportional over the dose range of 50 mg to 700 mg (0.1 to 1.6 times the maximum recommended dose of 450 mg).

Since encorafenib is 86% bound to plasma proteins, hemodialysis is likely to be ineffective in the treatment of overdose with BRAFTOVI.

• Jun 27, 2018NDANDA210496Array Biopharma Inc

1. 1Death1,13312%
2. 2Off Label Use1,12212%
3. 3Nausea8268.7%
4. 4Fatigue7467.8%
5. 5Diarrhoea6166.5%
6. 6Pyrexia5836.1%
7. 7Neoplasm Progression5525.8%
8. 8Product Use In Unapproved Indication5205.5%
9. 9Vomiting4674.9%
10. 10Rash4554.8%
11. 11Serous Retinal Detachment3343.5%
12. 12Arthralgia3063.2%
13. 13Decreased Appetite2953.1%
14. 14Malaise2863.0%
15. 15Asthenia2392.5%

The 10 most recently updated of 102 ClinicalTrials.gov registrations naming Encorafenib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• 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
• Hydroxychloroquine in Combination With Encorafenib and Cetuximab or Panitumumab in the Treatment of Metastatic BRAF-mutated Colorectal Cancer Refractory
  Terminated · Phase 2 · Interventional · 7 enrolled · Northwestern University
  NCT05576896updated 2026-06-12
• A Study of Encorafenib Plus Cetuximab With or Without Chemotherapy in People With Previously Untreated Metastatic Colorectal Cancer
  Active not recruiting · Phase 3 · Interventional · 841 enrolled · Pfizer
  NCT04607421updated 2026-06-11
• 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
• ASCEND-CRC: Profiling and Targeting Dynamic Tumor Resistance in Patients With Metastatic Colorectal Cancer
  Not yet recruiting · Early phase 1 · Interventional · 100 enrolled · M.D. Anderson Cancer Center
  NCT07318389updated 2026-06-11
• Encorafenib, Cetuximab, and Nivolumab in Treating Patients With Microsatellite Stable, BRAFV600E Mutated Unresectable or Metastatic Colorectal Cancer
  Active not recruiting · Phase 1 · Phase 2 · Interventional · 38 enrolled · M.D. Anderson Cancer Center
  NCT04017650updated 2026-06-11
• 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
• 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
• Testing the Addition of Anti-cancer Drug, ZEN003694, to the Usual Chemotherapy Treatment, Cetuximab Plus Encorafenib, for Colorectal Cancer
  Suspended · Phase 1 · Interventional · 30 enrolled · National Cancer Institute (NCI)
  NCT06102902updated 2026-06-03

Frequently asked questions

How does Encorafenib work?

Encorafenib is a kinase inhibitor that targets BRAF V600E, as well as wild-type BRAF and CRAF in in vitro cell-free assays with IC 50 values of 0.35, 0.47, and 0.3 nM, respectively. Mutations in the BRAF gene, such as BRAF V600E, can result in constitutively activated BRAF kinases that may stimulate tumor cell growth.

What is Encorafenib used for?

According to FDA labeling, Encorafenib carries indications including: BRAFTOVI is a kinase inhibitor indicated: Melanoma • in combination with binimetinib, for the treatment of patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, as detected by an FDA-authorized test. ( 1.1 , 2.1 ) Colorectal Cancer (CRC) • in combination with cetuximab and fluorouracil-based chemotherapy, for the treatment of adult patients with metastatic colorectal cancer (mCRC) with a BRAF V600E mutation, as detected by an FDA‑authorized test.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Encorafenib?

Encorafenib is classified as B-Raf serine-threonine kinase (BRAF) inhibitors, BRAF Serine/Threonine Kinase Inhibitors, Cellular Proliferation Alteration.

What are the brand names for Encorafenib?

Encorafenib is marketed under brand names including Braftovi.

What are the contraindications for Encorafenib?

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