NEQ1153

NEQ1153 is a dipeptidyl nitrile-based covalent cysteine protease inhibitor developed by the Universidade de São Paulo in collaboration with Columbia University. It is being investigated as an antimalarial agent targeting Plasmodium falciparum asexual blood stages, where it interferes with hemoglobin digestion. NEQ1153 acts as an inhibitor of cysteine proteases, including falcipain-2a (FP2a) in P. falciparum, cruzain in Trypanosoma cruzi, and human cathepsin L (hCatL). In vitro studies have demonstrated submicromolar inhibitory activity against both sensitive and resistant strains of P. falciparum, with resistance mediated primarily by mutations in falcipain-2a.