The worldwide health problem created by malaria has been made more difficult by the spread of drug- resistant parasites. We have developed an orally available and inexpensive class of novel drugs that act against both chloroquine-resistant and chloroquine-sensitive malaria. This project carries on preclinical development of a drug candidate that has been selected from this innovative class of potent antimalarials designed to overcome drug resistance. The candidate will be advanced through the ultimate stages of preclinical testing. Thus, pharmacokinetics, pharmacodynamics, pharmacology, and toxicity evaluations will be performed in both rats and monkeys. The overall goal will be completion of preclinical studies leading to approval of an Investigative New Drug (IND) application for the drug to be used in a Phase 1 human clinical trial.

Public Health Relevance

Malaria is a disease that infects about half a billion people annually, and kills nearly one million, most of whom are children or pregnant women. The impact of malaria remains, partly because the parasite that causes malaria has evolved into strains that are resistant to the best current drugs for treating the disease. This project completes preclinical evaluation of a novel drug candidate that was designed to circumvent malaria's drug resistance, paving the way toward approval for human clinical trials. The drug candidate has shown very promising results in early studies, and also has been designed to be inexpensive as well as safe for all target groups, including pregnant women and children.

National Institute of Health (NIH)
Small Business Technology Transfer (STTR) Grants - Phase II (R42)
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Special Emphasis Panel (ZRG1)
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Mcgugan, Glen C
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Designmedix, Inc.
United States
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Wirjanata, Grennady; Sebayang, Boni F; Chalfein, Ferryanto et al. (2015) Contrasting ex vivo efficacies of "reversed chloroquine" compounds in chloroquine-resistant Plasmodium falciparum and P. vivax isolates. Antimicrob Agents Chemother 59:5721-6