CT7439 / Carrick Therap - LARVOL DELTA

Inhibition of transcriptional cyclin-dependent kinases, CDK12/13, as a treatment for colorectal cancer with CDK12 upregulation. (ASCO 2025) - "Validation in colorectal cancer PDO showed greater inhibition by covalent inhibitors than standard of care chemotherapies for colorectal cancer (oxaliplatin, SN38, and 5-FU)... Here we highlight CDK12/13 inhibition as a compelling target for colorectal cancers and other solid tumors and show the importance of CDK13 compensation during CDK12 inhibition. These findings support further evaluation of the novel CDK12/13 inhibitor, CT7439, for the treatment of solid tumors with CDK12/13 upregulation."

Colorectal Cancer • Oncology • Solid Tumor • Targeted Protein Degradation • BRCA1 • CDK12 • CDK13

CT7439 an oral first-in class selective CDK12 and 13 inhibitor and cyclin K degrader: Profiling activity and combination efficacy in an ovarian cancer model (AACR 2025) - "CT7439 activity in OV-90 in cellular assays:OV-90GrowthCCNK**BRAC1*ERCC4*RAD51C*POLQ*MCL-1*IC50 nM (SD)4.40.66 (0.1)1.7 (0.4)0.82(0.3)1.2 (0.7)1.9(0.2)>20Data is mean ± SD (**Western blot, *qPCR) In addition to single agent activity of CT7439 a strong combination activity between CT7439 and the PARP inhibitors Olaparib, Niraparib and AZD10530 as well as the carboplatin was observed in an OV-90 cellular confluency assay. CT7439 is an orally bioavailable selective CDK12/13 inhibitor and degrader of CCNK. Pre-clinical studies demonstrates clinical potential for monotherapy use in solid tumors and as a combination therapy with agents known to cause a DNA damage response."

Clinical • Preclinical • Oncology • Ovarian Cancer • Solid Tumor • BRCA1 • CDK12 • CDK13 • ERCC4 • MCL1 • POLQ • RAD51C

Carrick Therapeutics Announces First Patient Dosed in Phase 1 Clinical Trial of CT7439 (CDK12/13 Inhibitor) (GlobeNewswire) - "Carrick Therapeutics Inc...announced that the first patient has been dosed in the Phase 1 clinical trial evaluating CT7439, a novel cyclin dependent kinase 12/13 (CDK12/13) inhibitor / Cyclin-K glue-degrader. CDK12/13 is implicated in multiple cancer types, as they regulate transcription elongation, RNA splicing, as well as cleavage and polyadenylation. DNA damage response genes are particularly suppressed by loss of CDK12/13 activity. The clinical trial is enrolling patients with advanced solid tumors, including ovarian, breast and Ewing's Sarcoma."

Trial status • Breast Cancer • Ewing Sarcoma • Gynecologic Cancers • Oncology • Ovarian Cancer • Sarcoma • Solid Tumor

A Modular Phase 1/2 Study with CT7439 in Participants with Solid Malignancies (clinicaltrials.gov) - P1/2 | N=50 | Recruiting | Sponsor: Carrick Therapeutics Limited

Combination therapy • New P1/2 trial • Oncology • Solid Tumor

Carrick Therapeutics Announces U.S. FDA Clearance of IND for CT7439, a First-In-Class Inhibitor of CDK12/13 (GlobeNewswire) - "Carrick Therapeutics...today announced that the U.S. Food and Drug Administration (FDA) has cleared the Company’s Investigational New Drug (IND) application for CT7439...The Company plans to initiate the Phase 1 clinical trial in the first half of 2024 and intends to enroll patients with advanced solid tumors, including breast, ovarian and Ewing's Sarcoma."

IND • New P1 trial • Breast Cancer • Ewing Sarcoma • Gynecologic Cancers • Oncology • Ovarian Cancer • Sarcoma • Solid Tumor

Systematic high-throughput combination drug screen to enhance poly (ADP-ribose) polymerase (PARP) inhibitor efficacy in ovarian cancer. (ASCO 2023) - "Following a combination screen with olaparib, the compounds selected for final validation were: AZD 7762 (CHK1/2 inhibitor), dinaciclib (pan-CDK inhibitor), onalespib (HSP90 inhibitor), and SN-38 (topoisomerase 1 inhibitor)...In MTT assays, we identified robust synergy between olaparib and CT7439, a next-generation oral CDK12/13 inhibitor, with a mean Bliss synergy score of 1.31 and scores as high as 22.03 at certain concentrations in the non-HRD model OVCAR-5... Pairing a PARP inhibitor and CDK inhibitor, a strategy identified by a high-throughput drug screen and known to impair homologous recombination, resulted in robust synergy in both HRD and non-HRD ovarian cancer models. Clinical translation of this combination may enhance the efficacy of PARP inhibitors in patients with ovarian cancer. >"

Clinical • Oncology • Ovarian Cancer • Solid Tumor • BRCA1 • CDK12 • HRD

Carrick Therapeutics Closes Series C Financing (GlobeNewswire) - "Carrick Therapeutics...announced it has raised $25 million in a Series C financing....The financing round was supported by existing investors, including ARCH Venture Partners, Rosetta Capital, Lightstone Ventures, Google Ventures, Cambridge Innovation Capital, and Evotec. The Company intends to use the proceeds to fund ongoing and planned samuraciclib clinical trials, ongoing development of its CDK12/13 inhibitor / Cyclin-K glue-degrader, and for working capital and general corporate purposes....Carrick has raised a total of $60 million from the Series C financing and Pfizer investment. The Company recently announced Pfizer Inc. has made a $35 million investment in Carrick. Carrick will maintain full economic ownership and control of samuraciclib and the rest of its pipeline."

Financing • Oncology