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Article
Open AccessDifferential kinetic profiles and metabolism of primaquine enantiomers by human hepatocytes
The clinical utility of primaquine (PQ), used as a racemic mixture of two enantiomers, is limited due to metabolism-linked hemolytic toxicity in individuals with genetic deficiency in glucose-6-phosphate dehyd...
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Article
Open AccessEnantioselective metabolism of primaquine by human CYP2D6
Primaquine, currently the only approved drug for the treatment and radical cure of Plasmodium vivax malaria, is still used as a racemic mixture. Clinical use of primaquine has been limited due to haemolytic toxic...
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Article
Open AccessTafenoquine and NPC-1161B require CYP 2D metabolism for anti-malarial activity: implications for the 8-aminoquinoline class of anti-malarial compounds
Tafenoquine (TQ) is an 8-aminoquinoline (8AQ) that has been tested in several Phase II and Phase III clinical studies and is currently in late stage development as an anti-malarial prophylactic agent. NPC-1161...
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Article
Open AccessCYP450 phenoty** and metabolite identification of quinine by accurate mass UPLC-MS analysis: a possible metabolic link to blackwater fever
The naturally occurring alkaloid drug, quinine is commonly used for the treatment of severe malaria. Despite centuries of use, its metabolism is still not fully understood, and may play a role in the haemolyti...
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Article
Open AccessThe metabolism of primaquine to its active metabolite is dependent on CYP 2D6
The efficacy of the 8-aminoquinoline (8AQ) drug primaquine (PQ) has been historically linked to CYP-mediated metabolism. Although to date no clear evidence exists in the literature that unambiguously assigns t...
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Article
Open AccessCYP450 phenoty** and accurate mass identification of metabolites of the 8-aminoquinoline, anti-malarial drug primaquine
The 8-aminoquinoline (8AQ) drug primaquine (PQ) is currently the only approved drug effective against the persistent liver stage of the hypnozoite forming strains Plasmodium vivax and Plasmodium ovale as well as ...
