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CT7439 + PARP inhibitor is an investigational combination therapy developed by Carrick Therapeutics for the treatment of ovarian cancer. CT7439 is a first-in-class small molecule that functions as a selective inhibitor of Cyclin-Dependent Kinase 12 (CDK12) and CDK13, while also acting as a molecular glue to induce the degradation of Cyclin K. The inhibition of CDK12 leads to the downregulation of DNA damage response (DDR) genes, effectively inducing a state of 'BRCAness' or homologous recombination deficiency (HRD) in tumor cells. This phenotype sensitizes the cells to PARP inhibitors, which block the repair of single-strand DNA breaks. The resulting accumulation of genomic instability leads to synthetic lethality and cell death. The combination is currently being evaluated in Phase 1 clinical trials as part of a combination expansion cohort.
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