Breena Fraga-Walton
Senior Scientist Circle Pharma
Seminars
Wednesday 29th April 2026
Discovery of Orally Bioavailable First-in-Class Cyclin A/B RxL Inhibitors to Treat Cancers with High E2F Activity
2:00 pm
- Previously we’ve disclosed passive permeable macrocyclic peptides that bind to the HP of both Cyclin A and B to induce potent and selective apoptosis of E2F high cancer cells. However, their oral bioavailability was insufficient to advance to pre-clinical development
- Discussing the optimization of this scaffold for drug-like properties and oral bioavailability, resulting in a new scaffold with improved ADME properties and demonstrating tumor regression in CDX models of small-cell lung cancer via oral dosing
- This compound is a close analog of our lead compound CID- 078, currently being investigated in a Ph.1 trial for patients with SCLC, TNBC, or solid tumors harboring RB1 mutation, sharing similar characteristics and allowing us to show how we optimized properties within the series
NEW DATA
