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Drug intelligence / Profile preview
amuvatinib + topotecan
- Development stage
- Phase 1
- Lead developer
- Astex Pharmaceuticals
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
Amuvatinib (MP-470) is a multi-targeted tyrosine kinase inhibitor with potent activity against several validated cancer targets including mutant forms of c-Kit and platelet-derived growth factor receptor alpha. Its mechanism of action involves inhibition of DNA repair by downregulating RAD51 expression, which impairs homologous recombination and sensitizes tumor cells to DNA-damaging agents such as chemotherapy and radiation. Topotecan is a semi-synthetic derivative of camptothecin that acts as a topoisomerase I inhibitor; it interferes with the DNA replication process in cancer cells by stabilizing the cleavable complex between DNA and topoisomerase I, leading to cell death. The combination has been investigated for synergistic effects in treating cancers such as small cell lung cancer (SCLC), particularly in platinum-refractory cases[2][5][7].
- Other names
- MP470MP-470MP 470amuvatinib hydrochloridetopotecan hydrochloride
02
Targets
PDGFRA (Platelet-derived growth factor receptor alpha)RAD51 (RAD51 Recombinase)KIT (c-KIT proto-oncogene receptor tyrosine kinase)TOP1 (DNA Topoisomerase I)
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