tp-1287

TP-1287 is an investigational oral phosphate prodrug of the CDK9 inhibitor alvocidib. Upon administration, TP-1287 is enzymatically hydrolyzed to yield alvocidib, which binds to the ATP-binding site of CDK9 and prevents phosphorylation. This inhibits productive transcription and causes reduction of messenger RNA in genes including c-MYC and MCL-1, leading to downregulation of key antiapoptotic proteins and inducing apoptosis in tumor cells. The drug has shown potent inhibition of intracellular kinases including CDK9 and has demonstrated tumor growth inhibition in preclinical models of hematologic malignancies and several solid tumor types.

Other names

2-(2-chlorophenyl)-5-hydroxy-8-((3S,4R)-3-hydroxy-1-methylpiperidin-4-yl)-4-oxo-4H-chromen-7-yl dihydrogen phosphate4h-1-benzopyran-4-one, 2-(2-chlorophenyl)-5-hydroxy-8-((3s,4r)-3-hydroxy-1-methyl-4-piperidinyl)-7-(phosphonooxy)-Alvocidib Prodrug TP-1287