Under development by SuperGen, Amuvatinib (MP470) inhibits not only wild-type c-Kit and PDGFRA, but also imatinib-resistant mutants including V560G, D816V, N822K and K642E. It also inhibits AXL kinase and cMet, which are upregulated in some imatinib-resistant GISTs. Finally, it also inhibits cRet and Rad51 protein.
Manufacturer: SuperGen Inc.
Definition from NCI Drug Dictionary: MP470 is a substance being studied in the treatment of several types of cancer. It blocks the action of certain enzymes involved in cell growth and the repair of DNA damaged by some anticancer drugs. It is a type of tyrosine kinase inhibitor and a type of recombinase inhibitor.
Two Phase I trials using amuvatinib have closed to recruitment, but Phase II trials are expected to be launched for several tumor types in the second half of 2010.