tolomeitinib

Tolomeitinib (HLP-290) is an orally bioavailable, potent, and selective small-molecule inhibitor of mitogen-activated protein kinase kinase 1 and 2 (MEK1/2). Developed by Jiangsu Hengrui Pharmaceuticals, it targets the MAPK/ERK signaling pathway, which is frequently dysregulated in various cancers, particularly those harboring NRAS or BRAF mutations. By inhibiting MEK1/2, tolomeitinib prevents the phosphorylation of ERK1/2, thereby suppressing tumor cell proliferation and inducing apoptosis. It is primarily being investigated for the treatment of advanced solid tumors, with a focus on NRAS-mutant advanced melanoma, including mucosal and cutaneous subtypes, where it has shown promising clinical activity in pivotal trials.

Other names

tolomeitinib