Last Updated: 29/06/2026
Dual-acting aspartyl protease antimalarials
Objectives
The proposed lead optimization research aims to increase potency against the parasite whilst maintaining selectivity, progressing to a lab development stage clinical candidate.
Malaria is one of the world’s most devastating diseases of humans and results in over 400,000 deaths annually. Novel therapies are urgently required to populate the antimalarial clinical portfolio, as the current therapeutics that treat this disease are becoming less effective due to emerging resistance. A collaboration between Dr David Olsen from Merck & Co., Kenilworth, NJ USA (known as MSD outside the US and Canada) and Professor Alan Cowman from the Walter and Eliza Hall Institute (WEHI), has demonstrated that malaria aspartyl protease enzymes are attractive drug targets, as they perform essential functions for survival in liver, blood, and sexual stages of the parasite life cycle. Through screening aspartyl protease inhibitor libraries, the collaboration has identified novel drugwfike hit compounds that are potently active against the malaria parasite.
- Article: First-in-human safety and pharmacokinetics of MK-7602, the antimalarial inhibitor of plasmepsins IX/X, in single- and multiple-ascending-dose studies - [Antimicrob Agents Chemother, 2026]
- Article: MK-7602: a potent multi-stage dual-targeting antimalarial - [eBioMedicine, 2025]
- Article: Basis for drug selectivity of plasmepsin IX and X inhibition in Plasmodium falciparum and vivax - [Structure, 2022]
Mar 2020 — Jun 2024
$8.49M