osimertinib + dalpiciclib

Osimertinib + dalpiciclib is an investigational combination therapy comprising two small molecule inhibitors: osimertinib, a third-generation, irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI), and dalpiciclib, a selective cyclin-dependent kinase 4/6 (CDK4/6) inhibitor. This combination is being studied primarily in patients with advanced non-small cell lung cancer (NSCLC) harboring EGFR mutations and alterations in the CDK4/6 pathway who have developed acquired resistance to prior third-generation EGFR TKI therapy. Osimertinib targets mutant forms of EGFR to inhibit tumor cell proliferation and survival, while dalpiciclib blocks CDK4/6-mediated cell cycle progression from G1 to S phase by inhibiting phosphorylation of the retinoblastoma protein. The rationale for combining these agents is to overcome resistance mechanisms involving activation of the CDK4/6 pathway that can limit the efficacy of EGFR TKIs alone[1][2][3][4][7].

Other names

osimertinib + dalpiciclib