Kura Oncology, Inc. reported preclinical data supporting the development of its next-generation farnesyl transferase inhibitor (FTI) KO-2806 in combination with KRASG12C inhibitors to drive tumor regressions and durable responses in KRASG12C-mutant non-small cell lung cancer (NSCLC). KRASG12C inhibitors have previously been shown to activate RTK signaling, leading to ERK-RSK and/or mTOR-S6 pathway reactivation. The Company?s new preclinical data show that co-treatment of preclinical models of KRASG12C-mutant NSCLC with KO-2806 and adagrasib deepens signaling inhibition at multiple nodes, including the MAPK and mTOR pathways, while decreasing cell proliferation.

In both cell-derived (CDX) and patient-derived (PDX) xenograft models originating from NSCLC tumors, the combination of KO-2806 with adagrasib induced tumor regressions. In addition, the CDX and PDX models demonstrated enhanced duration and depth of antitumor response compared to adagrasib as a single-agent therapy. Kura is on track to dose the first patient in its Phase 1 dose-escalation trial of KO-2806 (FIT-001) in the second half of 2023.

Concurrent with the monotherapy dose escalation, the Company plans to evaluate KO-2806 in dose-escalation combination cohorts with other targeted therapies in advanced solid tumors, including clear cell renal cell carcinoma (ccRCC) and KRASG12C NSCLC.