Cipargamin

Cipargamin (NITD609) is an potent antimalarial compound, with an IC₅₀ of appr 1 nM against P. falciparum. IC50 & Target: IC50: 1 nM (P. falciparum)^[3] In Vitro: Cipargamin (NITD609) inhibits T. gondii with a MIC₉₀ for tachyzoites of 5 μM and a MIC₅₀ of 1 μM, without toxicity to human foreskin fibroblasts (HFFs) at the highest concentration tested (10 μM)^[1]. Cipargamin (NITD609) is the most effective inhibitor of early gametocyte development at 50 and 500 nM. Cipargamin shows a dose-dependent inhibiting effect on late gametocyte development^[2]. Cipargamin (NITD609) shows potent activities against a panel of culture-adapted P. falciparum strains, with ICIC₅₀ values of 0.5-1.4 nM. Cipargamin is effective as artesunate with potency in the low nanomolar range (ICIC₅₀ values consistently <10 nM) against all P. falciparum and P. vivax isolates^[3]. In Vivo: Cipargamin (NITD609) shows favorable pharmacokinetic properties and displays single dose cure efficacy in a malaria mouse model. Cipargamin (100 mg/kg) completely clears P. berghei infection in all treated mice, and partial cure (50%) is achieved with a single oral dose at 30 mg/kg^[3].