Characterization of Novel Antimalarial Compound ACT-451840: Preclinical Assessment of Activity and Dose-Efficacy Modeling.
Amélie Le BihanRuben de KanterIñigo Angulo-BarturenChristoph BinkertChristoph BossReto BrunRalf BrunnerStephan BuchmannJeremy N BurrowsKoen J DecheringMichael DelvesSonja EwerlingSantiago FerrerChristoph FischliFrancisco Javier Gamo-BenitoNina F GnädigBibia HeidmannMaría Belén Jiménez-DíazDidier LeroyMaria Santos MartínezSolange MeyerJoerg J MoehrleCaroline L NgRintis NoviyantiAndrea RueckerLaura María SanzRobert W SauerweinChristian ScheurerSarah SchleiferboeckRobert SindenChristopher SnyderJudith StraimerGrennady WirjanataJutta MarfurtRichard N PriceThomas WellerWalter FischliDavid A FidockMartine ClozelSergio WittlinPublished in: PLoS medicine (2016)
The dual activity of ACT-451840 against asexual and sexual stages of P. falciparum and the activity on P. vivax have the potential to meet the specific profile of a target compound that could replace the fast-acting artemisinin component and harbor additional gametocytocidal activity and, thereby, transmission-blocking properties. The fast parasite reduction ratio (PRR) and gametocytocidal effect of ACT-451840 were recently also confirmed in a clinical proof-of-concept (POC) study.