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 30 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 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
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 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 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 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...
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
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

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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 Terminated 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 Unknown status USA | ITA | DEU 1


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