CGT1263 / Cogent Biosci - LARVOL DELTA

Characterization of CGT1263, a KRAS (ON/OFF) inhibitor clinical candidate with selectivity for mutant KRAS over HRAS and NRAS (AACR 2026) - "CGT1263 demonstrates robust anti-proliferative activity across a tumor spheroid panel of KRAS altered cell lines. In vivo characterization of CGT1815, the prodrug of CGT1263, includes steady state pharmacokinetics across species, pharmacodynamics, and efficacy in KRAS altered mouse tumor models."

Clinical • Colorectal Cancer • Oncology • HRAS • KRAS • NRAS

Title: Characterization of CGT1263, a KRAS (ON/OFF) inhibitor clinical candidate with selectivity for mutant KRAS over HRAS and NRAS (GlobeNewswire) - "Cogent Biosciences announces poster presentations at the American Association for Cancer Research (AACR) Annual Meeting 2026....The preclinical poster highlights Cogent’s internally developed pan-KRAS(ON) inhibitor with >500x selectivity for KRAS over HRAS and NRAS. Plasma exposure following oral administration across species resulted in sustained pERK inhibition and robust antitumor activity....Overall, these findings suggest CGT1263 could provide an advantage for patients, enabling higher dosing designed to elicit a more profound molecular response. Investigational New Drug (IND) enabling studies are ongoing with an IND submission expected later this year."

IND • Preclinical • Oncology

Cogent Biosciences Announces KRAS Poster Presentation at the 2025 AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics (GlobeNewswire) - "...'We look forward to advancing this program with the goal of filing an Investigational New Drug (IND) application to the U.S. Food and Drug Administration (FDA) in 2026.'...The poster presented today describes Cogent’s internally developed KRAS(ON/OFF) inhibitor CGT1263, showing clear selectivity over HRAS and NRAS, with picomolar (pM) activity across a broad panel of KRAS mutant cell lines. In addition, the poster also characterizes CGT1815 (the prodrug of CGT1263), which is designed to optimize human pharmacokinetic performance, supported by pharmacokinetics data from both CGT1815 and CGT1263 across multiple species."

IND • Preclinical • Solid Tumor