Therapy Detail
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| Therapy Name | Bemcentinib |
| Synonyms | |
| Therapy Description |
Bemcentinib (BGB-324) is a small molecule inhibitor of Axl, which inhibits tumor growth and may overcome EMT-mediated acquired drug resistance (PMID: 20145120, PMID: 31134766). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Bemcentinib | BGB 324|BGB-324|BGB324|R428|R-428 | AXL Inhibitor 29 | Bemcentinib (BGB-324) is a small molecule inhibitor of Axl, which inhibits tumor growth and may overcome EMT-mediated acquired drug resistance (PMID: 20145120, PMID: 31134766). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| AXL positive | myelodysplastic syndrome | sensitive | Bemcentinib | Phase I | Actionable | In a Phase I trial, Bemcentinib (BGB-324) treatment inhibited Axl phosphorylation, resulted in stable disease in 100% (3/3) of myelodysplastic syndrome patients (J Clin Oncol 34, 2016 (suppl; abstr 2561)). | detail... |
| AXL negative | head and neck squamous cell carcinoma | decreased response | Bemcentinib | Preclinical | Actionable | In a preclinical study, Bemcentinib (BGB-324) did not inhibit proliferation or invasion of AXL-negative head and neck squamous cell carcinoma cell lines in culture (PMID: 25767293). | 25767293 |
| AXL over exp | melanoma | sensitive | Bemcentinib | Preclinical - Cell culture | Actionable | In a preclinical study, Bemcentinib (BGB-324) treatment inhibited viability of a BRAF wild-type melanoma cell line overexpressing Axl in culture (PMID: 35332208). | 35332208 |
| AXL positive | breast cancer | sensitive | Bemcentinib | Preclinical | Actionable | In a preclinical study, Bemcentinib (BGB-324) inhibited tumor growth and metastasis in xenograft models of Axl-positive breast cancer cell lines, resulting in prolonged survival (PMID: 20145120). | 20145120 |
| AXL positive | Ewing sarcoma | sensitive | Bemcentinib | Preclinical - Cell culture | Actionable | In a preclinical study, Bemcentinib (BGB-324) inhibited growth of Ewing sarcoma cell lines positive for Axl expression in culture (PMID: 25528764). | 25528764 |
| AXL over exp | prostate cancer | sensitive | Bemcentinib | Preclinical | Actionable | In a preclinical study, Bemcentinib (BGB-324) inhibited growth of prostate cancer cell lines harboring elevated Axl protein level in culture (PMID: 26036314). | 26036314 |
| AXL positive | head and neck squamous cell carcinoma | sensitive | Bemcentinib | Preclinical | Actionable | In a preclinical study, Bemcentinib (BGB-324) inhibited proliferation and invasion of head and neck squamous cell carcinoma cell lines positive for Axl expression in culture (PMID: 25767293). | 25767293 |
| EML4 - ALK AXL over exp | lung adenocarcinoma | no benefit | Bemcentinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xalkori (crizotinib)-resistant lung adenocarcinoma cells harboring EML4-ALK and overexpressing AXL did not demonstrate sensitivity to Bemcentinib (BGB-324) treatment in culture (PMID: 32558295). | 32558295 |
| AXL positive | acute myeloid leukemia | sensitive | Bemcentinib | Phase I | Actionable | In a Phase I trial, Bemcentinib (BGB-324) treatment inhibited Axl phosphorylation, resulted in complete response in 12.5% (1/8), partial response in 12.5% (1/8), and stable disease in 37.5% (3/8) of acute myeloid leukemia patients (J Clin Oncol 34, 2016 (suppl; abstr 2561)). | detail... |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT03965494 | Phase I | Bemcentinib | AXL Inhibitor BGB324 in Treating Participants With Recurrent Glioblastoma Undergoing Surgery | Active, not recruiting | USA | 0 |
| NCT02488408 | Phase I | Cytarabine Bemcentinib | Multicenter Open-label Study of BGB324 as a Single Agent and in Combination With Cytarabine in Patients With AML | Active, not recruiting | USA | ITA | DEU | 1 |
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