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bemcentinib + dabrafenib + trametinib
- Development stage
- Unknown
- Lead developer
- Oncoinvent Solutions
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Bemcentinib (BGB324) is an oral small molecule inhibitor of AXL receptor tyrosine kinase. Dabrafenib is a small molecule inhibitor targeting the BRAF V600E mutation and is marketed as Tafinlar. Trametinib is a MEK1/2 inhibitor marketed as Mekinist. The combination of these drugs has been studied in metastatic melanoma and other cancers with BRAF V600E mutations. Bemcentinib targets the AXL pathway to potentially overcome resistance mechanisms to standard-of-care therapies such as dabrafenib plus trametinib, which together inhibit the MAPK pathway by blocking BRAF and MEK activity respectively[3][6]. Dabrafenib plus trametinib are approved for unresectable or metastatic solid tumors with BRAF V600E mutation[1][2][4].
- Brand names
- TafinlarMekinist
- Other names
- BGB324 + dabrafenib + trametinibbemcentinib + dabrafenib + trametinibBGB324 + Tafinlar + Mekinist
02
Targets
AXL (AXL receptor tyrosine kinase)BRAF (B-Raf proto-oncogene, serine/threonine kinase)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)RAF1 (c-Raf-1 (Y340D/Y341D))MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)
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