Overview
Ripretinib was specifically designed to improve the treatment of GIST patients by inhibiting the full spectrum of known mutations in KIT and PDGFRA.
Ripretinib is a KIT and PDGFRA inhibitor that blocks initiating and secondary KIT mutations in exons 9, 11, 13, 14, 17, and 18, known to be present in GIST patients. Ripretinib also inhibits PDGFRA mutations in exon 12,14 and 18, including the D842V mutation that drives a subset of GIST.
Currently, ripretinib is approved in the U.S., Canada, Australia, UK, European Union, Switzerland, New Zealand, Israel, and Greater China (mainland China, Hong Kong, Taiwan and Macau). In June 2019, we obtained an exclusive license to commercialize ripretinib in Greater China (mainland China, Hong Kong, Taiwan and Macau) from Deciphera Pharmaceuticals.
Mechanism of Action
Ripretinib is a novel switch-control tyrosine kinase inhibitor engineered to broadly inhibit KIT and PDGFRA mutated kinase by using a unique dual mechanism of action that regulates the kinase switch pocket and activation loop