HH2710

HH2710 is a highly potent, selective, reversible, ATP-competitive small molecule inhibitor of the serine/threonine-protein kinases ERK1 and ERK2 (extracellular signal-regulated kinases 1 and 2). By binding to and inhibiting ERK1/2 activity, it prevents phosphorylation of downstream substrates and blocks MAPK/ERK-mediated signal transduction. This mechanism targets tumors with abnormal activation of the MAPK pathway due to mutations in genes such as RAS or RAF. Developed by Haihe Biopharma (Shanghai Haihe Pharmaceutical), HH2710 was investigated for use in advanced solid tumors including non-small cell lung cancer (NSCLC), melanoma, Erdheim-Chester disease, and other cancers with RAS/RAF/MEK/ERK pathway mutations. Clinical development included first-in-human Phase I/II studies; however, development has since been discontinued[1][2][3][4][5].