Our Research

TP-1287 (Oral CDK9 Inhibitor)

TP-1287 is an oral CDK9 inhibitor that has shown favorable oral bioavailability in preclinical models. TP-1287 is enzymatically cleaved, yielding the parent drug, alvocidib, a potent inhibitor of CDK9.1

Preclinical Activity

TP-1287, delivered orally in preclinical models, has shown favorable activity in downregulating transcription of target genes of CDK9, such as MCL-1. The consequent downregulation of MCL-1 protein expression is correlated to tumor regression.1

Clinical Development

The oral administration of TP-1287 may allow for chronic dosing, which may lead to a durable inhibition of CDK9.1

TP-1287 is an investigational agent not yet approved by the US FDA or any other regulatory authorities.


    References:
  1. Kim W, Haws H, Peterson P, et al. TP-1287, an oral prodrug of the cyclin-dependent kinase-9 inhibitor alvocidib [Abstract 5133]. Cancer Res. 2017;77(13 suppl). doi: 10.1158/1538-7445.AM2017-5133.