CT7439: CDK12/13 inhibitor/Cyclin-K Degrader

Implicated in many types of cancer

CT7439 is a CDK12/13/Cyclin-K degrader, which potently inhibits the cellular activity of CDK12/13. CDK12/13 is implicated in multiple cancer types including breast, ovarian and Ewing's Sarcoma.

Program Cancer Indications Stage of Development Collaborator
Discovery Pre-Clinical Phase 1 Phase 2 Phase 3
Cyclin Dependent Kinase 12/13 (CDK12/13) Inhibitor / Cyclin K degrader
  • CT7439
Monotherapy: Fusion driven cancers (e.g. Ewing’s)
Discovery Phase complete
Pre-Clinical Phase in progress
Phase 1 Phase not started
Phase 2 Phase not started
Phase 3 Phase not started
PARP inhibitor combination
Discovery Phase complete
Pre-Clinical Phase in progress
Phase 1 Phase not started
Phase 2 Phase not started
Phase 3 Phase not started
Checkpoint inhibitor combination
Discovery Phase complete
Pre-Clinical Phase in progress
Phase 1 Phase not started
Phase 2 Phase not started
Phase 3 Phase not started

One molecule, two distinct mechanisms

Our CDK12/13 inhibitor/Cyclin-K degrader has two modes of action. The compound acts as an inhibitor of CDK12 but also as a 'glue degrader' of Cyclin-K, which is the obligate co-factor for CDK12/13. This 'double punch' significantly increases the potency of the compound and leads to the inhibition of DNA repair at the transcriptional level.

Regulating gene transcription

CDK12/13 regulates gene transcription through the activation of RNA Polymerase II. Our molecule inhibits CDK12/13 activity and the DNA damage response (DDR) pathway in cancer cells. As such, it has the potential to synergise with other agents targeting DDR such as the PARP inhibitors.

View CDK12/13 Biology Schematic