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CGT1263

Development stage: Preclinical
Lead developer: Cogent Biosciences
Modality: Small Molecules

Overview

CGT1263 is a small-molecule KRAS(ON/OFF) inhibitor developed by Cogent Biosciences. It is designed to target both the active (ON) and inactive (OFF) states of KRAS, demonstrating picomolar activity across various KRAS mutant cell lines while maintaining selectivity over HRAS and NRAS. The drug is part of a pan-KRAS program aimed at treating cancers driven by KRAS mutations, such as colorectal cancer, pancreatic cancer, and lung adenocarcinomas. A prodrug version, CGT1815, is also being developed to optimize pharmacokinetic performance for human clinical use.

Targets

Kirsten rat sarcoma viral oncogene homolog mutated protein

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