BI 1701963

BI 1701963 is an orally available small molecule that acts as a protein-protein interaction inhibitor targeting the guanine nucleotide exchange factor Son of sevenless homolog 1 (SOS1). By binding to SOS1, it prevents the interaction between SOS1 and KRAS-GDP, thereby inhibiting the activation of KRAS from its inactive GDP-bound state to its active GTP-bound state. This mechanism blocks downstream proliferative signaling pathways such as MAPK/ERK and PI3K that are driven by oncogenic KRAS mutations. The drug is being developed primarily for cancers with KRAS mutations, including advanced or metastatic solid tumors. It has been studied both as monotherapy and in combination with trametinib (a MEK inhibitor) in early-phase clinical trials[1][2][4][5][8].

Other names

pan-KRAS inhibitor