MK-7602: a potent multi-stage dual-targeting antimalarial.

ABSTRACT:

Background

The global burden of malaria remains substantial, and increasing parasite resistance to current antimalarials necessitates the development of drugs with unique mechanisms of action. This study aimed to develop and characterise a new antimalarial compound targeting Plasmodium aspartic proteases.

Methods

We conducted high-throughput screening, medicinal chemistry optimisation, and extensive in vitro and in vivo testing to develop and evaluate MK-7602, a dual inhibitor of plasmepsins IX and X.

Findings

MK-7602, a clinical candidate, acts as a dual sub-nanomolar inhibitor of plasmepsins IX and X in multiple Plasmodium species. It exhibits favourable pharmacokinetic properties and a promising safety profile. MK-7602 demonstrates activity against liver and blood

SUBMITTER: Favuzza P 

PROVIDER: S-EPMC12721278 | biostudies-literature | 2025 Dec

REPOSITORIES: biostudies-literature