CYCLACEL PHARMACEUTICALS, INC. The data will be presented at three poster sessions and report activity and antitumor effects of fadraciclib in biliary tract cancer, lung cancer, Richter transformation and lymphoma cell lines.
Details of the presentations are as follows
Title: The CDK2/9 inhibitor fadraciclib is active in Richter transformation and lymphoma cell lines by targeting both cell survival and proliferation
Abstract No: 518 / 15
Session Topic: Session PO.ET05.01 - Cell Cycle, Transcription Regulation, and Anticancer Drug Action
Date and Time:
Location: Exhibition Hall, Section 21
Title: Elucidation of the fates of CDK2 inhibited aneuploid and residual lung cancers
Abstract No: 2117 / 8
Session Topic: Session PO.ET07.02 - Pharmacodynamic Biomarkers of Drug Response
Date and Time:
Location: Exhibition Hall, Section 30
Title: Anti-tumor effects of fadraciclib, CDK2/9 inhibitor, in biliary tract cancer
Abstract No: 5711 / 11
Session Topic: Session PO.MCB01.01 - Pharmacologic Targeting of Cell Cycle Proteins
Date and Time:
Location: Exhibition Hall, Section 18
About Cyclin-Dependent Kinases and Fadraciclib
Cyclin-dependent kinases (CDKs) are critical for cell cycle control and transcriptional regulation. Dysregulated CDKs have been linked to the cancer hallmarks of uncontrolled proliferation and increased cancer cell survival. Fadraciclib is a highly selective, potent, orally and intravenously available, next generation inhibitor of CDK2 and CDK9. By inhibiting CDK2 and CDK9 fadraciclib causes apoptotic death through anaphase catastrophe of cancer cells at sub-micromolar concentrations.
To date single agent activity, including CR, PR and SD, has been observed in patients with advanced endometrial, squamous NSCLC lung cancer and T-cell lymphoma. Encouraging signals of activity were observed in patients with advanced cervical, hepatocellular, ovarian and pancreatic cancers.
065-101 Study of Oral Fadraciclib
Oral fadraciclib is being tested in a Phase 1/2 trial for the treatment of advanced solid tumors and lymphoma (065-101; NCT#04983810). A total of 29 patients have been treated as monotherapy in this ongoing study. The study is enrolling unselected, all comer patients with advanced solid tumors and lymphoma.
The Phase 2 part of the 065-101 study is designed to further evaluate fadra safety and efficacy in up to 8 cohorts defined by histology and/or NGS. The study is powered to demonstrate response in the molecular subtype suggested by the Phase 1 data and others that may be sensitive.
CDKN2A, CDKN2B, MTAP deletions
CDKN2A gene deletions occur in over 40% of several solid tumors, including glioma, head and neck, pancreatic, esophageal, lung (incl. squamous), bladder, melanoma, and others. CDKN2B deletions occur in over 30% of several solid tumors, including bladder, glioma, pancreatic, esophageal, lung (incl. squamous), head and neck, melanoma, and others. MTAP deletions occur in over 25% of several solid tumors, including glioma, mesothelioma, pancreatic, bladder, esophageal and others. MTAP deletion confers dependency on the PRMT5 enzyme in cancer cells which was identified as a synthetic lethal target for MTAP deleted cancers.
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