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UCB7362 is an orally active plasmepsin X (PMX) inhibitor currently investigated for the treatment of malaria. Plasmepsins are aspartyl proteases produced by the malaria parasite Plasmodium falciparum, and PMX is considered to be essential for parasite egress and invasion. UCB7362 is estimated to achieve a significant reduction in asexual blood-stage parasites. It has shown high potency in biochemical (IC = 7 nM), in vitro (P. falciparum 3D7 lactate dehydrogenase growth inhibition assay IC = 10 nM), and in vivo (50 mg/kg dose in mice) studies.
UCB7362 is an orally active plasmepsin X (PMX) inhibitor currently investigated for the treatment of malaria. Plasmepsins are aspartyl proteases produced by the malaria parasite Plasmodium falciparum, and PMX is considered to be essential for parasite egress and invasion. UCB7362 is estimated to achieve a significant reduction in asexual blood-stage parasites. It has shown high potency in biochemical (IC = 7 nM), in vitro (P. falciparum 3D7 lactate dehydrogenase growth inhibition assay IC = 10 nM), and in vivo (50 mg/kg dose in mice) studies.
Plasmepsins are aspartic acid proteases produced by malaria Plasmodium parasites. Several plasmepsins have been identified, and each one of them has a specific function. Plasmepsin X (PMX) controls parasite egress and invasion of erythrocytes and is essential during the red blood cell stages. UCB7362 binds to and inhibits PMX, disrupting the malaria parasite life cycle.
每项发明一条，涵盖美国、欧洲、PCT 与中国的同族专利。
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