Therapy Detail

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Therapy Name Lifirafenib
Synonyms
Therapy Description

Lifirafenib (BGB-283) is a dual RAF kinase and EGFR inhibitor, which may lead to decreased tumor cell proliferation and reduced growth of tumors with activation of BRAF and/or EGFR (PMID: 26208524, PMID: 32182156).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Lifirafenib BGB-283 BRAF Inhibitor 25 EGFR Inhibitor (Pan) 61 Lifirafenib (BGB-283) is a dual RAF kinase and EGFR inhibitor, which may lead to decreased tumor cell proliferation and reduced growth of tumors with activation of BRAF and/or EGFR (PMID: 26208524, PMID: 32182156).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
BRAF V600E thyroid cancer predicted - sensitive Lifirafenib Case Reports/Case Series Actionable In a Phase I trial, Lifirafenib (BGB-283) treatment resulted in partial response in 15.1% (8/53) of solid tumor patients with BRAF mutations, including 2 thyroid cancer patients harboring BRAF V600E (1 in dose-escalation phase, 1 in the dose-expansion), and in the dose-expansion phase 1 of 3 thyroid cancer patients harboring a BRAF V600 mutation demonstrated a partial response and 2 demonstrated stable disease, resulting in a disease control rate of 100% (3/3) (PMID: 32182156; NCT02610361). 32182156
BRAF L485_P490delinsFS Advanced Solid Tumor predicted - sensitive Lifirafenib Preclinical - Biochemical Actionable In a preclinical study, Lifirafenib (BGB-283) inhibited Mek and Erk phosphorylation in cells expressing BRAF L485_P490delinsFS in culture (PMID: 37656784). 37656784
BRAF V600E ovarian serous carcinoma predicted - sensitive Lifirafenib Case Reports/Case Series Actionable In a Phase I trial, Lifirafenib (BGB-283) treatment demonstrated safety and resulted in partial response (PR) in 15.1% (8/53) of advanced solid tumor patients harboring a BRAF mutation, including 1 patient with BRAF V600E-mutant low-grade serous ovarian cancer (PMID: 32182156; NCT02610361). 32182156
BRAF V600E Advanced Solid Tumor sensitive Lifirafenib Preclinical - Cell culture Actionable In a preclinical study, Lifirafenib (BGB-283) inhibited viability of a variety of cancer cell lines harboring BRAF V600E in culture (PMID: 26208524). 26208524
BRAF V600X Advanced Solid Tumor predicted - sensitive Lifirafenib Phase I Actionable In a Phase I trial, Lifirafenib (BGB-283) treatment demonstrated safety and resulted in partial response (PR) in 15.1% (8/53) of advanced solid tumor patients harboring a BRAF mutation, including 5 patients with BRAF V600E/K-mutant melanoma, 2 patients with BRAF V600E-mutant thyroid cancer, and 1 patient with BRAF V600E-mutant low-grade serous ovarian carcinoma, complete response in 1.9% (1/53), in a patient with melanoma, and stable disease in 50.9% (27/53) (PMID: 32182156; NCT02610361). 32182156
BRAF L597V lung adenocarcinoma sensitive Lifirafenib Preclinical - Patient cell culture Actionable In a preclinical study, cells derived from a lung adenocarcinoma patient harboring BRAF L597V were sensitive to treatment with Lifirafenib (BGB-283) in culture, demonstrating inhibition of cell growth (PMID: 32540409). 32540409
BRAF wild-type Advanced Solid Tumor no benefit Lifirafenib Preclinical - Cell culture Actionable In a preclinical study, a variety of BRAF wild-type tumor cell lines were insensitive to Lifirafenib (BGB-283) in culture (PMID: 26208524). 26208524
BRAF G469A lung adenocarcinoma sensitive Lifirafenib Preclinical - Patient cell culture Actionable In a preclinical study, cells derived from a lung adenocarcinoma patient harboring BRAF G469A were sensitive to treatment with Lifirafenib (BGB-283) in culture, demonstrating inhibition of cell growth (PMID: 32540409). 32540409
BRAF V600E/K melanoma predicted - sensitive Lifirafenib Case Reports/Case Series Actionable In a Phase I trial, Lifirafenib (BGB-283) treatment resulted in partial response in 15.1% (8/53) of solid tumor patients with BRAF mutations, including 5 of 23 patients with melanoma harboring BRAF V600E or V600K overall, and in the dose expansion phase 57.1% (4/7) patient with BRAF V600-mutant melanoma had a partial response (PMID: 32182156; NCT02610361). 32182156
BRAF V600E melanoma sensitive Lifirafenib Preclinical - Cell culture Actionable In a preclinical study, Lifirafenib (BGB-283) treatment inhibited viability of a melanoma cell line harboring BRAF V600E in culture (PMID: 31618628). 31618628
BRAF V600E melanoma sensitive Lifirafenib Preclinical - Cell culture Actionable In a preclinical study, Lifirafenib (BGB-283) inhibited Braf phosphorylation and cell proliferation in melanoma cell lines harboring BRAF V600E in culture (PMID: 26208524). 26208524
BRAF V600E colorectal cancer sensitive Lifirafenib Preclinical - Pdx & cell culture Actionable In a preclinical study, Lifirafenib (BGB-283) inhibited Braf phosphorylation and cell proliferation in colorectal cancer cell lines harboring BRAF V600E in culture, and resulted in partial tumor regression in both cell line and patient-derived xenograft models (PMID: 26208524). 26208524

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT02610361 Phase I Lifirafenib Study of the Safety and Pharmacokinetics of BGB-283 in Patients With Solid Tumors Completed NZL | AUS 0


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