BioCentury
ARTICLE | Distillery Therapeutics

Infectious disease

November 15, 2016 5:39 PM UTC

In vitro and mouse studies identified an EEF2 inhibitor that could help treat malaria. In cultured Plasmodium falciparum, a previously reported quinoline-4-carboxamide-based EEF2 inhibitor blocked growth of late-stage gametocytes and blood-stage parasites with EC50 values of 24 nM and 1 nM, respectively. Also in cultured parasites, the compound inhibited the growth of one mefloquine-resistant strain, two chloroquine-resistant strains, and three multidrug-resistant blood-stage strains of P. falciparum with EC50 values below 1 nM; P. yoelii liver-stage parasites with an EC50 of 1 nM; and P. berghei ookinetes with an EC50 of 5 nM. In a mouse model of P. berghei infection, oral 1 mg/kg doses of the compound decreased parasitemia and oral 30 mg/kg doses decreased parasitemia and increased survival compared with vehicle. Next steps could include testing the compound in models of drug-resistant malaria...