Encorafenib Medication Guide

Encorafenib is an oral BRAF inhibitor. All approved indications are combination regimens and require concomitant use with binimetinib or cetuximab, and must be based on confirmed BRAF V600E or V600K mutation-positive status.

Genetic Testing

Perform genetic testing before considering treatment.

1. Colorectal cancer: Confirm BRAF V600E mutation in plasma or tumor tissue. If not detected in a plasma specimen, tumor tissue must be tested again.

2. Non-small cell lung cancer: Confirm BRAF V600E mutation in tumor or plasma specimens. If not detected in plasma, tissue testing is also required.

3. Melanoma: Confirm BRAF V600E or V600K mutation in a tumor specimen.

Patients with wild-type BRAF test results should be excluded from this drug; these drugs may actually promote the growth of wild-type BRAF tumors.

Combination Regimens

1. Encorafenib with Binimetinib

For melanoma (V600E or V600K) and non-small cell lung cancer (V600E). Encorafenib 450 mg once daily, binimetinib 45 mg twice daily.

2. Encorafenib with Cetuximab

For previously treated colorectal cancer (V600E). Encorafenib 300 mg once daily.

3. Encorafenib with Cetuximab plus Fluoropyrimidine-based Chemotherapy

For first-line colorectal cancer (V600E).

Dosing Guide

1. Starting Dose

Melanoma and lung cancer: 450 mg once daily; colorectal cancer: 300 mg once daily.

2. Maximum Dose

450 mg once daily.

3. Administration

Swallow whole with water; may be taken with or without food; avoid grapefruit and grapefruit juice.

4. Missed Dose

Take the missed dose only if more than 12 hours remain until the next scheduled dose; if less than 12 hours remain, skip it and take the next dose as scheduled. Do not take a double dose at one time.

5. Vomiting After Taking a Dose

Do not take an additional dose; take the next dose at the scheduled time.

Regular Monitoring

Cardiac: Assess left ventricular ejection fraction before treatment, 1 month after starting treatment, and every 2 to 3 months thereafter, using echocardiography or MUGA scan. Patients with cardiovascular risk factors should be monitored more closely. The safety of the combination with binimetinib has not been established in patients with baseline ejection fraction below 50% or below the institutional lower limit of normal.

Liver: Check liver function before treatment and monthly during treatment, and additionally as clinically indicated. Serial testing of ALT, AST, and bilirubin is recommended.

Skin: Perform dermatologic examinations before treatment, every 2 months during treatment, and for up to 6 months after discontinuation. Suspicious skin lesions should be excised and sent for dermatopathologic evaluation.

Electrolytes: Monitor potassium and magnesium before and during treatment; correct hypokalemia and hypomagnesemia both before and during treatment.

Eyes: Perform periodic ophthalmologic evaluations; ask about visual symptoms at each visit; evaluate immediately if new or worsening visual abnormalities occur, or if new/persistent funduscopic findings appear.

Blood pressure: Monitor blood pressure when used in combination with binimetinib.

Pregnancy: Confirm pregnancy status in women of reproductive potential before starting treatment.