KRASG12C-selective inhibitor

KRASG12C-selective inhibitors are a class of small molecule targeted therapies designed to inhibit the G12C mutant form of the KRAS protein. These inhibitors typically function by forming a covalent bond with the cysteine residue at position 12, specifically when the protein is in its inactive, GDP-bound state. This interaction locks KRAS in an inactive conformation, thereby blocking the activation of downstream signaling pathways such as the RAF-MEK-ERK (MAPK) pathway, which drives tumor cell growth and survival. The development of these inhibitors, such as sotorasib and adagrasib, represented a major breakthrough in targeting KRAS, which was previously considered "undruggable" due to its high affinity for GTP and lack of accessible binding pockets.

Other names

KRAS G12C inhibitorKRAS G12C-selective inhibitorKRAS(G12C) inhibitor