Cipargamin is an antimalarial agent.1,2,3 It inhibits the Na+-ATPase activity of wild-type or mutant P. falciparum P-type ATPase (PfATP4; IC50s = 12.3-13.9 and 21.1-32.5 nM, respectively, in P. falciparum membranes).1 Cipargamin is active against the P. falciparum chloroquine-sensitive strain NF54 and chloroquine-resistant strain K1 (IC50s = 0.5 and 0.6 nM, respectively).2 It reduces parasitemia and increases survival in a mouse model of P. berghei infection when administered at doses of 10, 30, and 100 mg/kg.3
1.Rosling, J.E.O., Ridgway, M.C., Summers, R.L., et al.Biochemical characterization and chemical inhibition of PfATP4-associated Na+-ATPase activity in Plasmodium falciparum membranesJ. Biol. Chem.293(34)13327-13337(2018) 2.van Pelt-Koops, J.C., Pett, H.E., Graumans, W., et al.The spiroindolone drug candidate NITD609 potently inhibits gametocytogenesis and blocks Plasmodium falciparum transmission to Anopheles mosquito vectorAntimicrob. Agents Chemother.56(7)3544-3548(2012) 3.Rottmann, M., McNamara, C., Yeung, B.K.S., et al.Spiroindolones, a potent compound class for the treatment of malariaScience329(5996)1175-1180(2010)