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Cytochrome P450-Mediated Metabolism and CYP Inhibition for the Synthetic Peroxide Antimalarial OZ439

June 15, 2021 - 14:50 -- Open Access
Shackleford DM, Chiu FCK, Charman SA, et al.
ACS Infect Dis. 2021 Jun 8

OZ439 is a potent synthetic ozonide evaluated for the treatment of uncomplicated malaria. The metabolite profile of OZ439 was characterized in vitro using human liver microsomes combined with LC/MS-MS, chemical derivatization, and metabolite synthesis. The primary biotransformations were monohydroxylation at the three distal carbon atoms of the spiroadamantane substructure, with minor contributions from N-oxidation of the morpholine nitrogen and deethylation cleavage of the morpholine ring.

Anti-malarial ozonides OZ439 and OZ609 tested at clinically relevant compound exposure parameters in a novel ring-stage survival assay

December 23, 2019 - 15:09 -- Open Access
Annabelle Walz, Didier Leroy, Nicole Andenmatten, Pascal Mäser and Sergio Wittlin
Malaria Journal 2019 18:427, 18 December 2019

Drug efficacy against kelch 13 mutant malaria parasites can be determined in vitro with the ring-stage survival assay (RSA). The conventional assay protocol reflects the exposure profile of dihydroartemisinin.

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