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primaquine + R-primaquine + S-primaquine + primaquine-University of Mississippi, Oxford-malaria

Development stage
Unknown
Lead developer
University of Mississippi
Modality
Small Molecules
Administration
Oral
01

Overview

This record is a **non-product trial grouping**, not a single drug entity: it covers racemic **primaquine** and the separately administered **R-primaquine** and **S-primaquine** enantiomers evaluated by the University of Mississippi in a Phase 1 healthy-volunteer crossover study. Primaquine is an orally administered synthetic 8-aminoquinoline antimalarial. Its precise molecular target is not established; proposed antimalarial activity involves CYP2D6-dependent formation of hydroxylated metabolites, oxidative stress in infected cells, and disruption of mitochondrial function in dormant *Plasmodium* liver stages. Racemic primaquine is active against *Plasmodium vivax* hypnozoites and *Plasmodium falciparum* gametocytes, whereas the enantiomer program investigated stereoselective pharmacokinetics, metabolism, and tolerability rather than a co-formulated therapy. ([pmc.ncbi.nlm.nih.gov](https://pmc.ncbi.nlm.nih.gov/articles/PMC9885159/))

02

Targets

bc1 complex (Cytochrome bc1 complex (plasmodium))

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