Missing content? – Request curation!
Request curation for specific Genes, variants, or PubMed publications.
Have questions, comments or suggestions? - Let us know!
Email us at : ckbsupport@jax.org
Therapy Name | Encorafenib |
Synonyms | |
Therapy Description |
Braftovi (encorafenib) is an inhibitor of Raf kinase with selective activity against BRAF V600E, resulting in growth inhibition (PMID: 24864047). Braftovi (encorafenib) in combination with Mektovi (binimetinib) is FDA approved for use in patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation (FDA.gov). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
Encorafenib | Braftovi | LGX818 | BRAF Inhibitor 20 | Braftovi (encorafenib) is an inhibitor of Raf kinase with selective activity against BRAF V600E, resulting in growth inhibition (PMID: 24864047). Braftovi (encorafenib) is FDA approved for use in combination with Mektovi (binimetinib) in patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, and in combination with Erbitux (cetuximab) in patients with metastatic colorectal cancer with BRAF V600E(FDA.gov). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
BRAF S363F BRAF K601E | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited growth of a melanoma cell line harboring BRAF K601E, as well as BRAF S363F, in culture (PMID: 29903896). | 29903896 |
BRAF L597S | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited ERK activation and proliferation of melanoma cell lines harboring BRAF L597S in culture (PMID: 29903896). | 29903896 |
BRAF V600E | melanoma | sensitive | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) treatment inhibited Erk phosphorylation and reduced proliferation of melanoma cells harboring monomeric BRAF V600E in culture (PMID: 30559419). | 30559419 |
BRAF V600E | melanoma | sensitive | Encorafenib | Preclinical - Cell line xenograft | Actionable | In preclinical studies, Encorafenib (LGX818) treatment of human melanoma xenograft models with BRAF V600E significantly decreased Mek activation and resulted in tumor regression (Cancer Res: 72(8) Suppl 1, Abstract #3790). | detail... |
BRAF V600E | colorectal cancer | sensitive | Encorafenib | Phase I | Actionable | In a Phase I trial, Encorafenib (LGX818) showed activity in patients with advanced metastatic colorectal cancer harboring a BRAF V600E mutation, resulting in a median progression-free survival of 4 months and a best response of stable disease in 66.7% (12/18) (Ann Oncol (2014) 25 (suppl 4): iv182-iv183). | detail... |
BRAF G469V | melanoma | no benefit | Encorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) did not inhibit ERK phosphorylation or proliferation of a melanoma cell line harboring BRAF G469V (PMID: 29903896). | 29903896 |
BRAF L597V | lung adenocarcinoma | resistant | Encorafenib | Preclinical - Patient cell culture | Actionable | In a preclinical study, cells derived from a lung adenocarcinoma patient harboring BRAF L597V were resistant to treatment with Braftovi (encorafenib) in culture (PMID: 32540409). | 32540409 |
BRAF mutant | melanoma | sensitive | Encorafenib | Phase I | Actionable | In a Phase I trial, Encorafenib (LGX818) treatment resulted in an overall response rate (ORR) of 60% (15/25) and a median progression-free survival (mPFS) of 12.4 months in BRAF inhibitor-naïve melanoma patients harboring BRAF mutations, and an ORR of 22% (6/29) and mPFS of 1.9 months in BRAF inhibitor-pretreated patients (PMID: 28611198; NCT01436656). | 28611198 |
BRAF R239Q BRAF L597S | melanoma | sensitive | Encorafenib | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, Braftovi (encorafenib) inhibited ERK activation and proliferation of patient-derived melanoma cells harboring BRAF L597S, as well as BRAF R239Q, in culture, and delayed tumor growth and induced shrinkage in 8% (1/12) of tumors in a melanoma patient-derived xenograft (PDX) model (PMID: 29903896). | 29903896 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
---|---|---|---|---|---|---|
NCT01909453 | Phase III | Vemurafenib Encorafenib Binimetinib + Encorafenib | Study Comparing Combination of LGX818 Plus MEK162 Versus Vemurafenib and LGX818 Monotherapy in BRAF Mutant Melanoma (COLUMBUS) | Active, not recruiting | USA | ITA | FRA | ESP | DEU | CAN | 23 |
NCT04801966 | Phase 0 | Palbociclib Alpelisib Atezolizumab Vemurafenib Ribociclib Talazoparib Cobimetinib Trametinib Abemaciclib Dabrafenib Nivolumab Binimetinib Pembrolizumab Encorafenib | Safety and Oversight of the Individually Tailored Treatment Approach: A Novel Pilot Study (TAILOR) | Recruiting | 1 | |
NCT01436656 | Phase I | Encorafenib | A Phase I Study of Oral LGX818 in Adult Patients With Advanced or Metastatic BRAF Mutant Melanoma | Active, not recruiting | FRA | ESP | 2 |
NCT01777776 | Phase Ib/II | Encorafenib Encorafenib + Ribociclib | Safety and Efficacy of LEE011 and LGX818 in Patients With BRAF Mutant Melanoma. | Terminated | USA | CAN | 2 |
NCT01981187 | Phase II | Encorafenib | LGX818 for Patients With BRAFV600 Mutated Tumors | Terminated | USA | 0 |
NCT01894672 | Phase II | Encorafenib | BRAF Inhibitor, LGX818, Utilizing a Pulsatile Schedule in Patients With Stage IV or Unresectable Stage III Melanoma Characterized by a BRAFV600 Mutation | Completed | USA | 0 |