ferroquine and Malaria--Vivax

Ferroquine (FQ, SSR97193) is currently the most advanced organo-metallic drug candidate and about to complete phase II clinical trials as a treatment for uncomplicated malaria. This ferrocene-containing compound is active against both chloroquine-susceptible and chloroquine-resistant Plasmodium falciparum and P. vivax strains and/or isolates. This article focuses on the discovery of FQ, its antimalarial activity, the hypothesis of its mode of action, the current absence of resistance in vitro and recent clinical trials.

Topics: Aminoquinolines; Animals; Antimalarials; Chloroquine; Clinical Trials, Phase II as Topic; Drug Resistance; Ferrous Compounds; Humans; Malaria, Falciparum; Malaria, Vivax; Metallocenes; Plasmodium falciparum; Plasmodium vivax

The novel organometallic chloroquine analog ferroquine (SSR 97193) is effective against chloroquine-resistant Plasmodium falciparum. The ex vivo efficacy of ferroquine against Plasmodium vivax isolates was tested. Ferroquine has a potent ex vivo effect on P. vivax schizont maturation (median 50% inhibitory concentration, 15 nM; n = 42). No significant cross-sensitivity between ferroquine and other antimalarials was detected. This drug may be a suitable replacement for chloroquine in the treatment of drug-resistant P. vivax malaria.

Topics: Aminoquinolines; Antimalarials; Dose-Response Relationship, Drug; Drug Resistance, Bacterial; Ferrous Compounds; Humans; In Vitro Techniques; Malaria, Vivax; Metallocenes; Microbial Sensitivity Tests; Plasmodium vivax; Thailand