Lilly’s olomorasib receives Breakthrough Therapy designation for KRAS G12C-mutant lung cancer
Friday, September 05, 2025
Eli Lilly and Company has announced that the US Food and Drug Administration (FDA) has granted Breakthrough Therapy designation to olomorasib in combination with pembrolizumab (KEYTRUDA®) for the first-line treatment of patients with unresectable advanced or metastatic non-small cell lung cancer (NSCLC) carrying a KRAS G12C mutation and high PD-L1 expression (≥50%).
Olomorasib is a next-generation, highly selective KRAS G12C inhibitor with early evidence of central nervous system activity. The Breakthrough Therapy designation is intended to accelerate the development and review of medicines that show the potential to provide significant improvements over existing therapies.
Olomorasib (LY3537982) is being investigated as monotherapy and in combination regimens in KRAS G12C-mutated cancers, including NSCLC and other solid tumours. The molecule has shown potential for strong target occupancy, which may enable safer and more effective treatment combinations.
The designation is supported by results from the Phase 1/2 LOXO-RAS-20001 trial and the dose optimisation stage of the Phase 3 SUNRAY-01 trial.
The Phase 3 SUNRAY-01 study is a global, randomised, double-blind trial comparing olomorasib plus pembrolizumab, with or without chemotherapy, against placebo plus standard therapies in patients with KRAS G12C-mutant metastatic NSCLC. SUNRAY-02 and other studies form part of Lilly’s wider clinical programme evaluating olomorasib across multiple treatment settings.
Two oral presentations are scheduled at the congress. The first will provide data on the efficacy and safety of olomorasib combined with pembrolizumab as first-line therapy in KRAS G12C-mutant NSCLC, drawing on results from both LOXO-RAS-20001 and SUNRAY-01. The second will focus on outcomes when olomorasib is combined with chemoimmunotherapy (pembrolizumab, pemetrexed and platinum) as first-line treatment.
Source: lilly.com
