ALTA3263

ALTA3263 is an investigational, orally bioavailable small molecule inhibitor developed by Alterome Therapeutics for the treatment of advanced solid tumors harboring KRAS mutations. It is a highly potent and selective dual ON/OFF state inhibitor designed to target more than 90% of all KRAS driver mutations in cancer—including the most common variants such as G12D, G12V, and G12C. Unlike first-generation KRAS inhibitors that primarily target the OFF state (e.g., sotorasib for G12C), ALTA3263 inhibits both active (ON) and inactive (OFF) states of KRAS with picomolar to low nanomolar potency. The drug demonstrates high selectivity for KRAS over other RAS isoforms (HRAS and NRAS), aiming to provide complete target coverage with improved safety and efficacy profiles. Preclinical studies have shown deep tumor regressions in multiple xenograft models with various KRAS mutations while maintaining tolerability during prolonged oral dosing. Currently in Phase 1 clinical trials, ALTA3263 is being evaluated in adults with advanced unresectable or metastatic solid tumors—including non-small cell lung cancer (NSCLC), pancreatic ductal carcinoma (PDAC), colorectal cancer (CRC), adenocarcinoma, and other cancers driven by KRAS mutations[2][4][5][6][7][8].

Other names

ALTA3263ALTA-3263ALTA 3263