Drug intelligence / Profile preview

ganaplacide + lumefantrine + cipargamin

Development stage
Phase 2
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

ganaplacide + lumefantrine + cipargamin is an investigational non-artemisinin triple combination therapy being developed by Novartis, in collaboration with the Medicines for Malaria Venture (MMV), for the treatment of uncomplicated *Plasmodium falciparum* malaria. The combination consists of KLU156 (a fixed-dose combination of the novel imidazolopiperazine ganaplacide and a solid dispersion formulation of lumefantrine) and cipargamin (KAE609), a novel spiroindolone. This triple combination is designed to achieve a single-dose cure by combining fast parasite clearance, transmission-blocking activity, and a high barrier to resistance. Ganaplacide is believed to disrupt the parasite's internal protein secretory/trafficking pathway, lumefantrine inhibits the polymerization of toxic heme into non-toxic hemozoin, and cipargamin inhibits PfATP4, an essential sodium efflux pump of the malaria parasite.

Other names
KAF156 + lumefantrine + KAE609KAF156 + lumefantrine + cipargaminKLU156 + KAE609KLU156 + cipargaminganaplacide + lumefantrine + cipargaminganaplacide-lumefantrine + cipargaminganaplacide/lumefantrine + cipargamin
02

Targets

PfATP4 (Plasmodium falciparum ATPase 4)

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