KH003

KH003 is an investigational, orally bioavailable small molecule inhibitor specifically targeting the KRAS G12C mutation, developed by Sailing Pharmaceutical Technology Group Co., Ltd. The KRAS G12C mutation is a frequent oncogenic driver in various solid tumors, including non-small cell lung cancer (NSCLC) and colorectal cancer. KH003 functions by covalently and irreversibly binding to the cysteine residue at position 12 of the KRAS protein, effectively trapping the GTPase in its inactive, GDP-bound state. This action prevents the activation of downstream signaling pathways, such as the RAF-MEK-ERK (MAPK) pathway, which are critical for tumor cell proliferation and survival. KH003 is currently undergoing Phase 1 clinical evaluation to assess its safety, tolerability, and preliminary anti-tumor activity in patients with advanced solid tumors harboring the KRAS G12C mutation.