Optimization of a novel antimalarial drug candidate for plant-scale synthesis

DESCRIPTION (provided by applicant): There is a great need for anti-malarial drugs that are inexpensive and effective against drug-resistant strains. Malaria is one of the most important diseases worldwide, with over 225 million cases each year, and about800 thousand deaths. Most of these deaths occur in sub-Saharan Africa among the more vulnerable groups, such as children and pregnant women. In addition to the fatalities, malaria imparts a huge economic burden on the endemic countries, many of which are also the world's poorest. In some of the worst affected countries as much as 40% of their total health expenditure is spent on malaria, as current drug treatments are expensive. Although there are several approved antimalarial drugs, the malaria parasite asa great ability to develop resistance, to such an extent that drug resistance has been identified to every current therapy. This drug resistance can be sufficiently strong as to render the drug almost ineffective, as is the case with chloroquine, once the'gold star' treatment for malaria. DesignMedix has developed a novel set of antimalarial compounds, the lead of which is currently undergoing preclinical trials. The goal of this proposal is to optimize the synthesis of the lead compound, developing the method from a research laboratory scale, to one ready for plant-scale production. The aim is to improve the yields and reduce production costs in an effort to keep the overall cost of the drug as low as possible and therefore affordable to those who need it. PUBLIC HEALTH RELEVANCE: Malaria is a parasitic disease which kills around 800 thousand people each year, mainly children and pregnant women in sub-Saharan Africa. The parasite has a great ability to develop drug resistance, such that currentlythere are strains resistant to ever approved drug, so there is a continuing need for new therapies that are less expensive than current drugs. This work is to develop a novel antimalarial drug, from research laboratory scale to a method suitable for fullscale production.