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Last Updated: 09/05/2024

Dual-acting aspartyl protease antimalarials

Objectives

The proposed lead optimization research aims to increase potency against the parasite whilst maintaining selectivity, progressing to a Iab development stage clinical candidate.

Principal Investigators / Focal Persons

David B. Olsen
Alan Cowman

Rationale and Abstract

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.

Thematic Categories

Product Development

Date

Mar 2020 — Jun 2024

Total Project Funding

$8.49M

Funding Details
Wellcome Trust, United Kingdom

Grant ID: 202749/Z/16/C
GBP 5.73M
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