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8-aminoquinoline

Probing the distinct chemosensitivity of Plasmodium vivax liver stage parasites and demonstration of 8-aminoquinoline radical cure activity in vitro

October 13, 2021 - 12:50 -- Open Access
Author(s): 
Maher SP, Vantaux A, Kyle DE, et al.
Reference: 
Sci Rep. 2021 Oct 7;11(1):19905

Improved control of Plasmodium vivax malaria can be achieved with the discovery of new antimalarials with radical cure efficacy, including prevention of relapse caused by hypnozoites residing in the liver of patients. We screened several compound libraries against P. vivax liver stages, including 1565 compounds against mature hypnozoites, resulting in one drug-like and several probe-like hits useful for investigating hypnozoite biology. Primaquine and tafenoquine, administered in combination with chloroquine, are currently the only FDA-approved antimalarials for radical cure, yet their activity against mature P. vivax hypnozoites has not yet been demonstrated in vitro.

Protective effect of Mediterranean type glucose-6-phosphate dehydrogenase deficiency against Plasmodium vivax malaria

February 8, 2021 - 10:44 -- Open Access
Author(s): 
Awab GR, Aaram F, Jamornthanyawat N, Suwannasin K, Pagornrat W, Watson JA, Woodrow CJ, Dondorp AM, Day NP, Imwong M, White NJ
Reference: 
Elife. 2021 Feb 5;10:e62448

X-linked glucose-6-phosphate dehydrogenase (G6PD) deficiency is the most common human enzymopathy. The severe Mediterranean variant (G6PD Med) found across Europe and Asia is thought to confer protection against malaria, but its effect is unclear. We fitted a Bayesian statistical model to observed G6PD Med allele frequencies in 999 Pashtun patients presenting with acute Plasmodium vivax malaria and 1408 population controls.

NOT Open Access | Liver-targeted polymeric prodrugs of 8-aminoquinolines for malaria radical cure

January 1, 2021 - 16:00 -- NOT Open Access
Author(s): 
Srinivasan S, Roy D, Stayton PS, et al.
Reference: 
J Control Release. 2020 Dec 27:S0168-3659(20)30770-7

Primaquine and tafenoquine are the two 8-aminoquinoline (8-AQ) antimalarial drugs approved for malarial radical cure - the elimination of liver stage hypnozoites after infection with Plasmodium vivax. A single oral dose of tafenoquine leads to high efficacy against intra-hepatocyte hypnozoiites after efficient first pass liver uptake and metabolism. Unfortunately, both drugs cause hemolytic anemia in G6PD-deficient humans. This toxicity prevents their mass administration without G6PD testing given the approximately 400 million G6PD deficient people across malarial endemic regions of the world.

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