GHIT will invest 131 million yen (US$1.1 million) in identification of lead compound series with antimalarial activity that has clear potential for further development and progression to lead optimization. Previous project supported by GHIT, four novel hit compounds with antimalarial activity were identified from screening of Astellas’s 20,000 compounds. The compounds will be designed to explore both structure activity relationships and scope for structural modification to improve the compound profile such as potency, DMPK, and safety.

The project will consist of two phases. The first 6-month phase will involve the synthesis and profiling of small set of compounds designed around each of the four hit compounds identified in the previous project. The compounds will be designed to explore both structure activity relationships (SAR) and scope for structural modification to improve the compound profile (potency, DMPK, safety, etc.). Two series will be selected for Hit-to-Lead studies. The second 18-month phase of the project will involve the optimization of the series (prioritizing the series with the greatest potential) with the goal of identifying a series with a frontrunner compound meeting the MMV Early Lead criteria.