Ganaplacide(KAF156)hydrochloride是一种首创的具有口服活性的咪唑哌嗪类抗疟药(antimalarial)。Ganaplacidehydrochloride对多种疟原虫有活性，包括耐药寄生虫。Ganaplacidehydrochloride对无性和有性血液阶段以及肝脏阶段都有杀虫作用。
Ganaplacide (KAF156) hydrochloride is a first-in-class, orally active imidazolopiperazine antimalarial agent. Ganaplacide hydrochloride is active against a broad range of Plasmodium species, including drug-resistant parasites. Ganaplacide hydrochloride is parasiticidal against both asexual and sexual blood stages as well as the liver stages of the parasite[1][2].
Ganaplacide (KAF156) hydrochloride shows blood schizonticidal activity with 50% inhibitory concentrations of 6 to 17.4 nM against P. falciparum drug-sensitive and drug-resistant strains[1].
KAF156 displays cidal activity against mature Plasmodium falciparum gametocytes and thus blocks parasite transmission to Anopheles mosquitoes[1].Ganaplacide (KAF156) hydrochloride (1-15 mg/kg; p.o.) is fully protective in a causal prophylactic mouse model of malaria[1]. Animal Model: Mice (causal prophylactic rodent malaria model)[1]
[1]. Kuhen KL, et al. KAF156 is an antimalarial clinical candidate with potential for use in prophylaxis, treatment, and prevention of disease transmission. Antimicrob Agents Chemother. 2014;58(9):5060-5067. [2]. Leong FJ, et al. A first-in-human randomized, double-blind, placebo-controlled, single- and multiple-ascending oral dose study of novel Imidazolopiperazine KAF156 to assess its safety, tolerability, and pharmacokinetics in healthy adult volunteers. Antimicrob Agents Chemother. 2014;58(11):6437-6443.
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