ezurpimtrostat + trametinib

Ezurpimtrostat + trametinib is a combination therapy under investigation for the treatment of advanced cancers, most notably advanced KRAS-mutated cholangiocarcinoma (bile duct cancer)[3][5]. Ezurpimtrostat (also known as GNS561) is a new small molecule inhibitor targeting autophagy, and trametinib is a highly selective, reversible, allosteric small molecule inhibitor of MEK1 and MEK2 in the MAPK pathway[4]. The combination aims to exploit dual pathway inhibition, with trametinib blocking the MAPK pathway and ezurpimtrostat inhibiting autophagy, to synergistically impair tumor cell survival and overcome resistance mechanisms. Trametinib is approved for certain cancers and is typically used in combination regimens; in this combination, both drugs are being explored experimentally, with early-phase trials ongoing in solid tumors such as cholangiocarcinoma[3][5].

Brand names

Mekinist

Other names

GNS561 + trametinib