Encorafenib (Braftovi): BRAF Inhibitor for Melanoma & CRC
Encorafenib is a potent oral small-molecule BRAF kinase inhibitor. It specifically targets enzymes in the MAPK signaling pathway, which is often hyperactivated in cancers harboring BRAF mutations.
Encorafenib (Braftovi) is designed to block the defective BRAF protein, thereby stopping the signal that tells cancer cells to grow. It is a cornerstone of targeted therapy for patients with specific genetic profiles.
Depending on the cancer type, it is never used alone: it is paired with binimetinib for melanoma or cetuximab for colorectal cancer to maximize efficacy and overcome resistance mechanisms.
Indications
- Unresectable or Metastatic Melanoma: Indicated for patients with a BRAF V600E or V600K mutation, in combination with binimetinib.
- Metastatic Colorectal Cancer (mCRC): Indicated for patients with a BRAF V600E mutation, who have received prior therapy, in combination with cetuximab.
- Biomarker: Confirmation of the mutation by an FDA-approved test is required before starting therapy.
Dosage and administration
The dosage varies by indication. Taken once daily.
- For Melanoma: 450 mg (six 75 mg capsules) orally once daily. Used in combination with binimetinib.
- For Colorectal Cancer: 300 mg (four 75 mg capsules) orally once daily. Used in combination with cetuximab.
- Administration: Swallow capsules whole with water. Can be taken with or without food. Do not take a missed dose within 12 hours of the next scheduled dose.
- Pregnancy and Breastfeeding: Can cause fetal harm. Effective contraception is mandatory.
- Hypersensitivity to encorafenib.
- Cardiac Conditions: Monitoring of QT interval is recommended.
Side effects depend on the combination used.
- Dermatologic: Hyperkeratosis (thickening of skin), Palmar-plantar erythrodysesthesia (hand-foot syndrome), rash. Also, risk of new primary cutaneous malignancies (e.g., cuSCC), which are usually managed by excision.
- Musculoskeletal: Arthralgia (joint pain), myalgia.
- Gastrointestinal: Nausea, vomiting, abdominal pain.
- General: Fatigue.
List of medicines by active substance Encorafenib
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