crenolanib

Crenolanib is an orally bioavailable, highly selective small molecule inhibitor of type III receptor tyrosine kinases, specifically targeting platelet-derived growth factor receptors alpha and beta (PDGFRα/β) and Fms-like tyrosine kinase 3 (FLT3). It is classified as a benzimidazole type I kinase inhibitor. Crenolanib inhibits both wild-type and mutant forms of FLT3—including internal tandem duplication (ITD) and tyrosine kinase domain (TKD) mutations—as well as PDGFRα/β, leading to the inhibition of downstream signaling pathways involved in cell proliferation and survival. Unlike some other FLT3 inhibitors, crenolanib does not significantly inhibit c-KIT or other receptor tyrosine kinases at clinically relevant concentrations. The drug has demonstrated activity in preclinical models against leukemia cells harboring FLT3 mutations resistant to other TKIs. Crenolanib is being developed primarily for the treatment of acute myeloid leukemia (AML), especially in patients with FLT3 mutations, as well as gastrointestinal stromal tumors (GIST), glioma, and other cancers. It is administered orally[1][2][3][4][5][7].

Other names

crenolanib besylate