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Malaria Drugs Discovery

Today, artemisinin is the last defense against drug resistant malaria and recent reports suggest that decades of continuous use of these potent antimalarials as monotherapies may have fostered artemisinin drug resistance in Plasmodium. Unfortunately there are few ongoing efforts to discover and develop novel and effective antimalarial drugs to fight this ancient and resilient scourge.
 

To address this unmet global health need, NITD has led the formation of a research consortium to bring together Novartis' cutting-edge drug discovery with world-class malaria biology expertise. Armed with a grant from the Wellcome Trust, the Medicines for Malaria Venture and the Singapore Economic Development Board, the consortium has the ambitious goals of identifying (1) new drugs with a potential for a single-dose cure for P. falciparum malaria and, (2) a curative modality for P. vivax malaria.
 

These two goals were set to address two weaknesses with the current antimalarials, namely the poor patient compliance with most P. falciparum malaria treatments and the inability to rapidly and safely eradicate the parasite liver stages following a P. vivax infection.

Anti-Malarial Discovery Portfolio at NITD

The following constitutes our current antimalarial drug discovery portfolio (last updated April 25, 2008)
 

1) Malaria Signal Peptide Peptidase as a new antimalarial drug target (in collaboration with Bruno Martoglio NIBR-Basel)
 

2) Spiro-Indolone scaffold lead optimization
 

3) New Artemisinin derivatives (in collaboration with Gary Posner at Johns Hopkins University)
 

4) Quinazoline derivatives - Inhibition of antifolate drug resistant Plasmodium (in collaboration with Alexis Nzila at KEMRI/WT Kilifi)
 

5) Hit-to-Lead follow-up of cellular screens (in collaboration with GNF and Novartis Natural Products Unit)

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