Antimalarial Activity of KAF156 in Falciparum and Vivax Malaria

Antimalarial Activity of KAF156 in Falciparum and Vivax Malaria

With the emergence and spread of artemisinin resistance, new therapies for malaria are needed. This study shows that the imidazolopiperazine KAF156, a new antimalarial compound, has in vivo antimalarial activity. Expanding artemisinin resistance and worsening partner-drug resistance in Southeast Asi...

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Bibliographic Details
Published in:The New England journal of medicine Vol. 375; no. 12; pp. 1152 - 1160
Main Authors: White, Nicholas J, Duong, Tran T, Uthaisin, Chirapong, Nosten, François, Phyo, Aung P, Hanboonkunupakarn, Borimas, Pukrittayakamee, Sasithon, Jittamala, Podjanee, Chuthasmit, Kittiphum, Cheung, Ming S, Feng, Yiyan, Li, Ruobing, Magnusson, Baldur, Sultan, Marc, Wieser, Daniela, Xun, Xiaolei, Zhao, Rong, Diagana, Thierry T, Pertel, Peter, Leong, F. Joel
Format: Journal Article
Language:English
Published: United States Massachusetts Medical Society 22-09-2016
Subjects:
Administration, Oral
Adult
Antimalarial activity
Antimalarial agents
Antimalarials - administration & dosage
Antimalarials - adverse effects
Antimalarials - pharmacokinetics
Antiparasitic agents
Bradycardia
Clinical trials
Drug therapy
Female
Fever
Humans
Hyperbilirubinemia
Hypokalemia
Imidazoles - administration & dosage
Imidazoles - adverse effects
Imidazoles - pharmacokinetics
Liver
Malaria
Malaria, Falciparum - drug therapy
Malaria, Vivax - drug therapy
Male
Middle Aged
Parasite Load
Parasites
Patients
Piperazines - administration & dosage
Piperazines - adverse effects
Piperazines - pharmacokinetics
Plasmodium falciparum - isolation & purification
Plasmodium vivax - isolation & purification
Thrombocytopenia
Vomiting
Young Adult
Thailand
Bangkok Thailand
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Summary:With the emergence and spread of artemisinin resistance, new therapies for malaria are needed. This study shows that the imidazolopiperazine KAF156, a new antimalarial compound, has in vivo antimalarial activity. Expanding artemisinin resistance and worsening partner-drug resistance in Southeast Asia threaten the global control of Plasmodium falciparum malaria. 1 – 5 New drugs are needed. KAF156 represents a new class of antimalarial agents (imidazolopiperazines) 6 identified by high-throughput phenotypic screening. KAF156 has potent in vitro activity against both asexual and sexual blood stages and the preerythrocytic liver stages of the malarial parasite. 7 The mechanism of antimalarial action is unknown, but drug resistance, mediated by mutations in the P. falciparum cyclic amine resistance locus ( PfCARL ) gene, which encodes a protein of unknown function, can be selected. 7 In a study of 70 healthy . . .
ISSN:0028-4793
1533-4406
DOI:10.1056/NEJMoa1602250