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 | 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 | 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 | 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 |
| 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 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 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 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 | 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 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 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 | 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 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 |
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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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