Although many antimalarial drugs are available, the emergence of resistance is an ongoing problem. Worryingly, resistance to artemisinin — the key component of the current first-line drug combinations — has recently emerged in Southeast Asia, and so the need for new drug classes is pressing.

About 8 years ago, many groups seeking such drugs started to focus on phenotypic screening, which has “been incredibly fruitful in terms of generating hits and leads,” says Tim Wells, Chief Scientific Officer of the Medicines for Malaria Venture in Geneva, Switzerland. “Around 80% of the compounds in preclinical or Phase I at the moment have come from phenotypic screening,” he says. KAE609 is the first antimalarial compound identified using such screens to demonstrate efficacy in clinical trials.

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