Encorafenib (Braftovi)

General information

Class/mechanism (from NCI Drug Dictionary): An orally available Raf kinase inhibitor with potential antineoplastic activity. LGX818 specifically inhibits Raf kinase, a serine/threonine enzyme in the RAF/mitogen-activated protein kinase kinase (MEK)/extracellular signal-related kinase (ERK) signaling pathway.

Diseases for which it is established

• BRAF-mutated CRC
• BRAF-mutated melanoma
• BRAF-mutated NSCLC

History of changes in FDA indication

• 2018-06-27: Initial approval in combination with Binimetinib (Mektovi) for patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, as detected by an FDA-approved test. (Based on COLUMBUS)
• 2020-04-09: Approved in combination with cetuximab for the treatment of adult patients with metastatic colorectal cancer (CRC) with a BRAF V600E mutation, detected by an FDA-approved test, after prior therapy. (Based on BEACON CRC)
• 2023-10-11: Approved with Binimetinib (Mektovi) for adult patients with metastatic non-small cell lung cancer (NSCLC) with a BRAF V600E mutation, as detected by an FDA-approved test. (Based on PHAROS)

History of changes in EMA indication

• 2018-09-19: Iniital authorization

History of changes in Health Canada indication

• 2021-03-02: Initial notice of compliance for use in combination with binimetinib for the treatment of adult patients with unresectable or metastatic melanoma with a BRAF V600 mutation, as detected by a validated test.

History of changes in PMDA indication

• 2019-01-08: New approval for the treatment of unresectable melanoma with BRAF gene mutation.
• 2020-11-27: New indication and a new dosage for the treatment of unresectable, advanced or recurrent BRAF mutation-positive colorectal cancer that has progressed after cancer chemotherapy.

Also known as

• Code name: LGX-818
• Brand name: Braftovi