molecules of the month


oral PMX inhibitor for malaria

50 mg QD/7 days estimated to be curative

from guanidine-based focused lib. screen. and SBDD

J. Med. Chem.

UCB Biopharma, Braine-l’Alleud, BE

UCB7362 chemical structure oral PMX inhibitor for malaria - UCB Biopharma, Braine-l’Alleud, BE
5 mins read

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…

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