Encorafenib (Braftovi) is a kinase inhibitor targeting BRAF V600E or V600K mutations, indicated for use in combination with drugs such as binimetinib or cetuximab for the treatment of specific types of melanoma, colorectal cancer, and non-small cell lung cancer.

What Are the Precautions for Encorafenib (Braftovi) Administration?

Genetic Testing

All patients must confirm the presence of BRAF V600E or V600K mutations in the tumor using FDA-approved testing methods before initiating encorafenib treatment.

Contraindicated in patients with wild-type BRAF tumors, as its use may promote tumor growth.

Combination Therapy Regimens

Encorafenib must be used in combination with other drugs and is not for monotherapy.

Combined with binimetinib for the treatment of melanoma and non-small cell lung cancer.

Combined with cetuximab ± mFOLFOX6 for the treatment of colorectal cancer.

Risk of New Malignancies

Cutaneous malignancies: Including squamous cell carcinoma, basal cell carcinoma, etc. Regular skin examinations should be performed before treatment, every 2 months during treatment, and within 6 months after discontinuation.

Non-cutaneous malignancies: Such as RAS mutation-related tumors. Patients should seek medical attention promptly if any new symptoms arise.

Bleeding Risk

Severe, even fatal, bleeding events may occur, such as gastrointestinal bleeding and intracranial hemorrhage.

Symptoms to monitor: Abnormal nosebleeds, hemoptysis, melena, hematuria, headache, confusion, etc.

Pregnancy and Contraception

Encorafenib has embryotoxic potential and may cause fetal harm.

Female patients: Effective non-hormonal contraceptive measures should be adopted during treatment and for 2 weeks after the last dose.

Pregnancy testing: Confirm non-pregnancy status before initiating medication.

Drugs to Avoid Concomitant Use

Strong or moderate CYP3A4 inhibitors (e.g., ketoconazole, grapefruit juice): May increase encorafenib plasma concentrations. If co-administration is unavoidable, dose adjustment is required.

Strong CYP3A4 inducers (e.g., rifampicin): May reduce encorafenib efficacy; concomitant use should be avoided.

Hormonal contraceptives: Encorafenib may decrease their efficacy; non-hormonal contraceptive methods are recommended.

Medication Monitoring for Encorafenib (Braftovi)

Cardiotoxicity Monitoring

Combination with binimetinib may cause cardiomyopathy, manifested as decreased left ventricular ejection fraction (LVEF).

Monitoring requirements: Perform echocardiography or MUGA scan before treatment, 1 month after treatment initiation, and every 2–3 months thereafter.

Symptoms to monitor: Palpitations, shortness of breath, lower extremity edema, dizziness, etc.

Hepatotoxicity Monitoring

Combination with binimetinib may cause elevated liver enzymes.

Monitoring requirements: Test liver function (ALT, AST, alkaline phosphatase, etc.) before treatment and monthly thereafter.

Symptoms to monitor: Jaundice, dark urine, nausea, decreased appetite, fatigue, etc.