Encorafenib (Braftovi)
Targeted Therapy · Approved since 2020
Description
Encorafenib is an oral BRAF kinase inhibitor specifically approved for the treatment of metastatic colorectal cancer harboring BRAF V600E mutations. This targeted therapy is administered in combination with cetuximab (an EGFR inhibitor) for patients with BRAF V600E-mutated metastatic colorectal cancer who have received prior therapy. Encorafenib represents a precision medicine approach for this specific molecular subtype of colorectal cancer, which accounts for approximately 8-12% of metastatic colorectal cancers and historically has had poor outcomes with standard chemotherapy.
Mechanism of Action
Encorafenib selectively inhibits BRAF V600E mutant kinase, which is constitutively active in tumors harboring this mutation and drives oncogenic MAPK pathway signaling. By blocking mutant BRAF kinase activity, encorafenib disrupts the aberrant cell proliferation and survival signals that promote tumor growth. The combination with cetuximab provides dual pathway inhibition by simultaneously blocking EGFR-mediated feedback activation that can lead to resistance.
Molecular Targets
Side Effects
Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.