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Dec 19, 2013
 |  BC Innovations  |  Targets & Mechanisms

Lipid kinase enters the malaria stage

A Novartis AG-University of California, San Diego-led consortium has identified a new class of antimalarials that, unlike marketed drugs, eliminates Plasmodium at all stages of its infection cycle.1 The pharma is developing derivatives of the lead inhibitor with improved drug-like properties.

Plasmodium's life cycle consists of several distinct stages. Mosquito-injected sporozoites rapidly populate liver cells, in which they either proliferate and produce merozoites that emerge in the bloodstream or enter a dormant phase as hypnozoites in the liver.

Emerging merozoites can undergo several cycles of asexual multiplication in the blood, resulting in thousands of infected red blood cells and causing malaria symptoms. Merozoites also can develop into sexual-stage gametocytes, which are taken up by mosquitoes and ultimately give rise to a new generation of sporozoites to be injected into the next host.2

Latent hypnozoites, on the other hand, can linger in the liver for long periods of time, causing disease relapse sometimes years after the initial infection when mobilized back into the bloodstream as merozoites.

Thus, eradicating malarial disease requires Plasmodium to be targeted at replicating stages in liver and blood, dormant stages in...

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