产品描述:
Pralsetinib is an inhibitor of RET (IC50s = 0.4, 0.3, 0.4, and 0.4 nM for wild-type RET, RETV804L, RETV804M, and RETM918T, respectively).{69564} It is selective for RET over VEGFR2 (IC50 = 35 nM) and a panel of 371 kinases at 300 nM. Pralsetinib also inhibits a fusion protein of coiled-coil domain-containing protein 6 with RET (CCDC6-RET) and autophosphorylation of RET in Ba/F3 cells expressing a fusion protein of kinesin-1 heavy chain with RET (KIF5B-RET; IC50s = 0.4 and 5 nM, respectively). It induces tumor regression in a KIF5B-RET-positive patient-derived xenograft (PDX) mouse model of non-small cell lung cancer (NSCLC) when administered at a dose of 30 mg/kg. Formulations containing pralsetinib have been used in the treatment of metastatic RET-fusion-positive NSCLC.