Synonyms: ACT451840 | Actelion-451840
Compound class:
Synthetic organic
Comment: ACT-451840 is an investigational antimalarial drug, selected from a new class of compounds identified from a phenotypic screen [2,4]. Chemically it is a piperazine-containing compound.
The Malaria tab on this ligand page provides additional curator comments of relevance to the Guide to MALARIA PHARMACOLOGY. |
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References |
1. Aissaoui H., Boss C., Corminboeuf O., Heidmann B., Siegrist R. (2011)
Piperazines as antimalarial agents. Patent number: WO2011083413A1. Assignee: Actelion Pharmaceuticals Ltd.. Priority date: 05/01/2010. Publication date: 14/07/2011. |
2. Boss C, Aissaoui H, Amaral N, Bauer A, Bazire S, Binkert C, Brun R, Bürki C, Ciana CL, Corminboeuf O et al.. (2016)
Discovery and Characterization of ACT-451840: an Antimalarial Drug with a Novel Mechanism of Action. ChemMedChem, 11 (18): 1995-2014. [PMID:27471138] |
3. Bruderer S, Hurst N, de Kanter R, Miraval T, Pfeifer T, Donazzolo Y, Dingemanse J. (2015)
First-in-humans study of the safety, tolerability, and pharmacokinetics of ACT-451840, a new chemical entity with antimalarial activity. Antimicrob Agents Chemother, 59 (2): 935-42. [PMID:25421475] |
4. Brunner R, Aissaoui H, Boss C, Bozdech Z, Brun R, Corminboeuf O, Delahaye S, Fischli C, Heidmann B, Kaiser M et al.. (2012)
Identification of a new chemical class of antimalarials. J Infect Dis, 206 (5): 735-43. [PMID:22732921] |
5. Brunner R, Ng CL, Aissaoui H, Akabas MH, Boss C, Brun R, Callaghan PS, Corminboeuf O, Fidock DA, Frame IJ et al.. (2013)
UV-triggered affinity capture identifies interactions between the Plasmodium falciparum multidrug resistance protein 1 (PfMDR1) and antimalarial agents in live parasitized cells. J Biol Chem, 288 (31): 22576-83. [PMID:23754276] |
6. Krause A, Dingemanse J, Mathis A, Marquart L, Möhrle JJ, McCarthy JS. (2016)
Pharmacokinetic/pharmacodynamic modelling of the antimalarial effect of Actelion-451840 in an induced blood stage malaria study in healthy subjects. Br J Clin Pharmacol, 82 (2): 412-21. [PMID:27062080] |
7. Le Bihan A, de Kanter R, Angulo-Barturen I, Binkert C, Boss C, Brun R, Brunner R, Buchmann S, Burrows J, Dechering KJ et al.. (2016)
Characterization of Novel Antimalarial Compound ACT-451840: Preclinical Assessment of Activity and Dose-Efficacy Modeling. PLoS Med, 13 (10): e1002138. [PMID:27701420] |
8. Ng CL, Siciliano G, Lee MC, de Almeida MJ, Corey VC, Bopp SE, Bertuccini L, Wittlin S, Kasdin RG, Le Bihan A et al.. (2016)
CRISPR-Cas9-modified pfmdr1 protects Plasmodium falciparum asexual blood stages and gametocytes against a class of piperazine-containing compounds but potentiates artemisinin-based combination therapy partner drugs. Mol Microbiol, 101 (3): 381-93. [PMID:27073104] |