Synonyms: OZ439
Compound class:
Synthetic organic
Comment: Artefenomel is a synthetic ozonide (synthetic peroxide), a class of compound that retains the endoperoxide bridge of the artemisinin class of antimalarials but also contains the sterically bulky amantadine ring, which increases blood plasma stability [6].
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. Charman SA, Arbe-Barnes S, Bathurst IC, Brun R, Campbell M, Charman WN, Chiu FC, Chollet J, Craft JC, Creek DJ et al.. (2011)
Synthetic ozonide drug candidate OZ439 offers new hope for a single-dose cure of uncomplicated malaria. Proc Natl Acad Sci USA, 108 (11): 4400-5. [PMID:21300861] |
2. Delves M, Plouffe D, Scheurer C, Meister S, Wittlin S, Winzeler EA, Sinden RE, Leroy D. (2012)
The activities of current antimalarial drugs on the life cycle stages of Plasmodium: a comparative study with human and rodent parasites. PLoS Med, 9 (2): e1001169. [PMID:22363211] |
3. Giannangelo C, Siddiqui G, De Paoli A, Anderson BM, Edgington-Mitchell LE, Charman SA, Creek DJ. (2020)
System-wide biochemical analysis reveals ozonide antimalarials initially act by disrupting Plasmodium falciparum haemoglobin digestion. PLoS Pathog, 16 (6): e1008485. [PMID:32589689] |
4. Macintyre F, Adoke Y, Tiono AB, Duong TT, Mombo-Ngoma G, Bouyou-Akotet M, Tinto H, Bassat Q, Issifou S, Adamy M et al.. (2017)
A randomised, double-blind clinical phase II trial of the efficacy, safety, tolerability and pharmacokinetics of a single dose combination treatment with artefenomel and piperaquine in adults and children with uncomplicated Plasmodium falciparum malaria. BMC Med, 15 (1): 181. [PMID:28988541] |
5. Phyo AP, Jittamala P, Nosten FH, Pukrittayakamee S, Imwong M, White NJ, Duparc S, Macintyre F, Baker M, Möhrle JJ. (2016)
Antimalarial activity of artefenomel (OZ439), a novel synthetic antimalarial endoperoxide, in patients with Plasmodium falciparum and Plasmodium vivax malaria: an open-label phase 2 trial. Lancet Infect Dis, 16 (1): 61-69. [PMID:26448141] |
6. Vennerstrom JL, Arbe-Barnes S, Brun R, Charman SA, Chiu FC, Chollet J, Dong Y, Dorn A, Hunziker D, Matile H et al.. (2004)
Identification of an antimalarial synthetic trioxolane drug development candidate. Nature, 430 (7002): 900-4. [PMID:15318224] |