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Drug intelligence / Profile preview
amuvatinib
- Development stage
- Discontinued
- Lead developer
- Astex Pharmaceuticals
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Amuvatinib is an orally bioavailable, synthetic small molecule that acts as a selective multi-targeted tyrosine kinase inhibitor. It suppresses the activity of several receptor tyrosine kinases, including c-MET, c-RET, and mutant forms of c-KIT (stem cell factor receptor), PDGFR (platelet-derived growth factor receptor), and FLT3. In addition to its kinase inhibition profile, amuvatinib disrupts DNA repair by downregulating RAD51 protein expression—a key component in homologous recombination repair—thereby sensitizing tumor cells to DNA-damaging agents such as chemotherapy and radiotherapy. Amuvatinib has been investigated primarily for the treatment of solid tumors and small cell lung carcinoma in clinical trials but was discontinued after failing to meet prespecified endpoints in proof-of-concept studies[1][2][3][6].
- Other names
- amuvatinib hydrochloride850879-09-3
02
Targets
AXL (AXL receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)MET (Mesenchymal-epithelial transition factor receptor)PDGFRA (Platelet-derived growth factor receptor alpha)RAD51 (RAD51 Recombinase)RET (Rearranged during transfection receptor tyrosine kinase)KIT (c-KIT proto-oncogene receptor tyrosine kinase)
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