molecules of the month

Context. UCB7362(UCB Biopharma) is an oral plasmepsin X (PMX) inhibitor being developed as an antimalarial agent. Malaria is a protozoan disease caused by Plasmodium sp. and remains a significant public health concern in many parts of the world, with 627,000 reported global deaths in 2020 despite the significant strides in the antimalarial drug space. Artemisin-based combination therapies (ACTs) are the standard in care for the disease, but increasing resistance to the therapy poses a significant challenge to treating and eradicating malaria. UCB7362 is a member of a novel class of compounds that target PMX, an aspartyl protease that plays a key role in P. falciparum egress. Structure-based optimization of a cyclic guanidine core, a privileged scaffold for aspartyl proteases, led…