Novartis discovers new antimalarial compounds

 Researchers at Novartis and its academic partners have discovered a new class of antimalarial compounds that attacks the liver phase as well as the blood phase of the parasite’s life cycle.

The newly-discovered imidazolopiperazines (IZPs) have the potential to treat malaria in its dormant phase, which has so far proved very difficult to treat.

Drugs based on IZP compounds could be taken orally and could prevent recurrence of the disease in infected patients.

The Plasmodium amoeboid, transmitted by infected mosquito bites, travels in the human bloodstream and multiplies in the liver, where the disease can remain dormant for months or years before recurring.

Most existing antimalarial drugs only attack the blood-borne parasite, and those that target the liver phase tend to have dangerous side-effects.

Malaria kills an estimated one million people worldwide every year.

In addition, the need for new antimalarial drugs has been exacerbated by the recent spread of drug-resistant Plasmodium strains, due in part to improper use and counterfeiting of the existing drugs.

The study was conducted by scientists at the Novartis Institutes for BioMedical Research (NIBR), in collaboration with other Novartis research institutes and with academic researchers.

By using a novel assay to determine the liver stage activity of candidate compounds and developing a chemical scaffold effective in attacking both phases of the parasite life cycle, the researchers produced the IZP class – which has been shown to protect mice from developing the liver cycle of the parasite.

Novartis plans to start clinical trials of the lead IZP candidate in 2012.

Mark Fishman, President of the NIBR, said that the study had been published “to facilitate broad-based discovery efforts across the globe towards elimination of this disease.”