Encorafenib is a targeted drug for BRAFV600E mutant melanoma, exerting anti-tumor effects by inhibiting BRAF kinase activity. The following provides a detailed introduction from the aspects of drug characteristics, indications, usage and dosage, and precautions.

1. Basic information of the drug

Konafenib is an oral small molecule BRAF kinase inhibitor that was approved for marketing by the FDA in 2018. The common names include Enkofeni and Enkofeni, and the trade name is Braftovi.

2 Indications

Mainly used for the treatment of BRAFV600E or V600K mutation patients confirmed by FDA approved testing: unresectable or metastatic melanoma (combined with bimertinib), metastatic colorectal cancer (combined with cetuximab), and metastatic non-small cell lung cancer (combined with bimertinib).

3 Usage and Dosage

3.1 Recommended Dosage

Melanoma and non-small cell lung cancer: 450mg daily in combination with bimertinib; Colorectal cancer: 300mg daily in combination with cetuximab. Continue medication until disease progression or intolerable toxicity occurs.

3.2 Dose adjustment

According to the grading of adverse reactions, the dosage should be reduced to 300mg/day for the first dose, 225mg/day for the second dose, and discontinued for the third dose. When used in combination with CYP3A4 inhibitors, the dosage should be reduced accordingly. For potent inhibitors, the dosage should be reduced to 150mg/day.

4 Precautions

4.1 Taboo Population

BRAF is contraindicated for patients with wild-type tumors (may promote tumor growth); Patients with moderate to severe liver damage (Child Pugh B/C grade) lack safety data and are not recommended for use.

4.2 Important Monitoring Indicators

Regular check ups are required for LVEF (risk of cardiomyopathy), liver function (hepatotoxicity), electrocardiogram (QT interval prolongation), and vision (uveitis). If 3-4 levels of toxicity occur, the medication should be temporarily or permanently discontinued.

4.3 Other Risks

Including newly diagnosed malignant tumors (especially RAS mutation positive non skin tumors), bleeding events, skin reactions, etc. Prohibited during pregnancy, effective contraception is required during treatment.