Malaria is a dangerous disease which kills more than one million people worldwide. To control the disease caused by parasite Plasmodium falciparum, scientists from an international collaboration of AstraZeneca, GlaxoSmithKline, Columbia University and Harvard Medical School have discovered a new drug candidate that can kill the malaria parasite quickly and over a long duration. The research was funded by Medicines for Malarial venture, Switzerland-based nonprofit foundation.
Triaminopyrimidine (TAP) is the drug which has shown positive response by remaining in the blood for an extended period of time with 36 hour half-life.
“Drug discovery is a rigorous and expensive endeavor with a high rate of attrition. To put it in perspective, we screened around 5,00,000 small molecules from the AZ collection and prioritized TAPs as promising lead series for further evaluation. Further medicinal chemistry optimization of TAPs resulted in selection of MMV253 from TAPs series as a candidate drug with ideal properties like novel chemical class, novel mechanism of action, fast kill in-vitro and in-vivo, predicted long half-life in humans and good safety margins in rats and guinea pigs. Since the skill sets were spread across the globe, coordinating and getting the right experiment done at the shortest possible time at a reasonable cost was a real challenge”, said Dr Sambandamurthy.
Deaths from mosquito-borne malaria have been nearly halved since 2000, but the infection still killed about 584,000 people in 2013, mostly in Africa, according to the World Health Organization (WHO). Rising temperatures could be the main reason for transmitting and with the positive results of single dose treatment for malaria, the malarial cases are expected to decrease in the coming years.