encorafenib

Encorafenib is a small-molecule targeted cancer therapy that inhibits the activity of the BRAF kinase, particularly the V600-mutant form, to block the MAPK signaling pathway and slow the growth of tumor cells. It is used in combination regimens for certain BRAF-mutant cancers and is marketed under the brand name Braftovi in various markets.

In melanoma, encorafenib is approved in combination with binimetinib, a MEK inhibitor, for unresectable or metastatic disease harboring BRAF V600E or V600K mutations. In metastatic colorectal cancer, encorafenib is approved in combination with cetuximab for patients with BRAF V600E-mutant tumors that have progressed after prior therapy. These indications reflect the drug’s role as part of combination strategies designed to more effectively suppress MAPK signaling.

Mechanistically, encorafenib binds selectively to mutant BRAF kinase, reducing aberrant signaling through the MAPK pathway and decreasing tumor cell proliferation. Combining a BRAF inhibitor with a MEK inhibitor or with an anti-EGFR antibody is intended to improve efficacy and mitigate certain adverse effects associated with BRAF inhibition alone, such as paradoxical activation of pathway signaling.

Administration and safety profile: encorafenib is taken orally, typically in capsule form, as part of combination regimens. Common adverse effects include fever, fatigue, nausea, diarrhea, vomiting, rash, and decreased appetite. More serious risks include dermatologic cancers such as squamous cell carcinoma and potential liver or heart-related effects; monitoring and dose management are advised.

Regulatory status: approval for melanoma and colorectal cancer indications has been granted by major regulatory agencies in multiple regions, with ongoing investigation of additional indications and combination strategies in BRAF-mutant cancers.