Cpd-1308 / Jiangsu Hengrui Pharma - LARVOL DELTA

Dual-targeting CDK4 and CDK2 overcomes resistance to CDK4/6 inhibitors in HR+ breast cancer (AACR 2026) - "The next generation of CDK inhibitors such as atirmociclib targeting CDK4 and tagtociclib targeting CDK2 have demonstrated encouraging early efficacy, and the combination of a selective CDK4 inhibitor and a selective CDK2 inhibitor has entered clinical trials...These results suggested that CDK4:CDK6 selectivity of Cpd-1308 was greater than that of palbociclib.Further kinetic characterization using surface plasmon resonance (SPR) spectroscopy revealed that Cpd-1308 has long residence time on CDK2 in comparison with tagtociclib...Cpd-1308 indeed showed superior potency on antiproliferation of derived palbociclib resistant MCF7 cells (MCF7-palbo-r) and derived abemaciclib resistant MCF7 cells (MCF7-abema-r)...Cpd-1308 demonstrated significant resistance-overcoming activity.Taken together, we demonstrate activity of Cpd-1308 in HR+ breast cancers and CDK4/6i-resistant breast cancers. Our research results indicate that co-targeting CDK4 and CDK2 with a small-molecule may..."

Breast Cancer • Eye Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Retinoblastoma • Solid Tumor • CD34 • CDK2 • CDK6