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Sumitomo - Model TP-1287 -Investigational Oral CDK9 Inhibitor
TP-1287 is an investigational oral CDK9 inhibitor that has shown favorable oral bioavailability in preclinical models. TP-1287 is enzymatically cleaved, yielding the active moiety, a potent inhibitor of CDK9.35 Inhibiting CDK9 is thought to downregulate the transcription of target genes, including MCL-1, reducing leukemic blast viability in MCL-1–dependent hematologic malignancies, and c-MYC, an important oncogene across multiple tumor types.36-38
Understanding our target
The primary function of CDK9 is to activate transcription elongation by phosphorylating the C-terminal domain of RNA polymerase II. By inhibiting CDK9, the active moiety in TP-1287 downregulates the transcription of target genes, including the myeloid cell leukemia-1 (MCL-1) and c-MYC genes.40-42 In MCL-1–dependent hematologic malignancies, downregulation of MCL-1 protein expression can trigger apoptosis of leukemic blasts.39,40 As many tumor types are “addicted” to c-MYC, it represents a potentially effective target for therapy.41
Clinical evidence
TP-1287 is the oral prodrug of an active moiety that has shown clinical activity in multiple types of solid tumors and hematologic malignancies, possibly due to its ability to downregulate CDK9.39,40,43
TP-1287 has shown clinical activity and modulation of downstream biomarkers in a first-in-human, phase I study in patients with advanced solid tumors.43
Ongoing development
TP-1287 is currently undergoing a first-in-human, phase I clinical trial in patients with advanced solid tumors.
