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Tafenoquine

Not Open Access | Impact of CYP2D6 Genetic Variation on Radical Cure of Plasmodium vivax Malaria

June 1, 2021 - 15:45 -- NOT Open Access
Author(s): 
Suarez-Kurtz G
Reference: 
Clin Pharmacol Ther. 2021 May 27

Plasmodium vivax is the most widespread human malaria parasite, with 2.5 billion people at risk of infection worlwide. P. vivax forms liver hypnozoites which trigger further symptomatic episodes (relapses) weeks or months after the initial episode. Radical cure of vivax malaria requires hypnozoitocide therapy to prevent relapses. The two FDA-approved hypnozoiticides for human use, primaquine and tafenoquine, are pro-drugs, that require in vivo conversion into metabolites with redox activity. This mini-review focuses on the association between CYP2D6-mediated hydroxylation and hypnozoiticide efficacy of primaquine and tafenoquine.

NOT Open Access | Tafenoquine is a Promising Drug Candidate for the Treatment of Babesiosis

May 5, 2021 - 11:28 -- NOT Open Access
Author(s): 
Liu M, Ji S, Xuan X, et al.
Reference: 
Antimicrob Agents Chemother. 2021 May 3:AAC.00204-21

Due to drug resistance, commonly used anti-Babesia drugs have limited efficacy against babesiosis, and inflict severe side effects. Tafenoquine (TAF) was approved by the U.S. Food and Drug Administration in 2018 for the radical cure of Plasmodium vivax infection and for malaria prophylaxis. Here, we evaluated the efficacy of TAF for the treatment of Babesia infection and elucidated the suspected mechanisms of TAF activity against Babesia parasites. Parasitemia and survival rates of B. rodhaini-infected BALB/c and SCID mice were used to explore the role of the immune response in Babesia infection after TAF treatment.

The integrity and stability of specimens under different storage conditions for glucose-6-phosphate dehydrogenase deficiency screening using WST-8

May 5, 2021 - 08:56 -- Open Access
Author(s): 
Chamchoy K, Praoparotai A, Pakparnich P, Sudsumrit S, Swangsri T, Chamnanchanunt S, Songdej D, Imwong M, Boonyuen U
Reference: 
Acta Trop. 2021 May;217:105864

Accurate measurement of glucose-6-phosphate dehydrogenase (G6PD) activity is critical for malaria treatment as misclassification of G6PD deficiency could cause serious harm to patients. G6PD activity should be assessed in blood samples on the day of collection. Otherwise, specimens should be stored under suitable conditions to prevent loss of G6PD activity.

Estimated impact of tafenoquine for Plasmodium vivax control and elimination in Brazil: A modelling study

April 29, 2021 - 08:00 -- Open Access
Author(s): 
Nekkab N, Lana R, Lacerda M, Obadia T, Siqueira A, Monteiro W, Villela D, Mueller I, White M
Reference: 
PLoS Med. 2021 Apr 23;18(4):e1003535

Despite recent intensification of control measures, Plasmodium vivax poses a major challenge for malaria elimination efforts. Liver-stage hypnozoite parasites that cause relapsing infections can be cleared with primaquine; however, poor treatment adherence undermines drug effectiveness. Tafenoquine, a new single-dose treatment, offers an alternative option for preventing relapses and reducing transmission. In 2018, over 237,000 cases of malaria were reported to the Brazilian health system, of which 91.5% were due to P. vivax.

Glucose-6-phosphate dehydrogenase mutations in malaria endemic area of Thailand by multiplexed high‐resolution melting curve analysis

April 21, 2021 - 15:07 -- Open Access
Author(s): 
Usa Boonyuen, Duantida Songdej, Mallika Imwong, et al.
Reference: 
Malaria Journal 2021 20:194, 20 April 2021

Glucose-6-phosphate dehydrogenase (G6PD) deficiency, the most common enzymopathy in humans, is prevalent in tropical and subtropical areas where malaria is endemic. Anti-malarial drugs, such as primaquine and tafenoquine, can cause haemolysis in G6PD-deficient individuals. Hence, G6PD testing is recommended before radical treatment against vivax malaria. Phenotypic assays have been widely used for screening G6PD deficiency, but in heterozygous females, the random lyonization causes difficulty in interpreting the results. Over 200 G6PD variants have been identified, which form genotypes associated with differences in the degree of G6PD deficiency and vulnerability to haemolysis. This study aimed to assess the frequency of G6PD mutations using a newly developed molecular genotyping test.

NOT Open Access | Efficacy of a 3-day pre-travel schedule of Tafenoquine for malaria chemoprophylaxis: A network meta-analysis

April 13, 2021 - 13:15 -- NOT Open Access
Author(s): 
Islam N, Wright S, Lau CL, Doi SAR, Mills DJ, Clark J, Clements ACA, Furuya-Kanamori L
Reference: 
J Travel Med. 2021 Apr 8:taab057

Chemoprophylaxis with weekly doses of tafenoquine (200 mg/day for 3 days before departure [loading dose], 200 mg/week during travel and one-week post-travel [maintenance doses]) is effective in preventing malaria. Effectiveness of malaria chemoprophylaxis drugs in travellers is often compromised by poor compliance. Shorter schedules that can be completed before travel, allowing ‘drug-free holidays’, could increase compliance and thus reduce travel-related malaria. In this meta-analysis, we examined if a loading dose of tafenoquine alone is effective in preventing malaria in short-term travellers.

Tafenoquine: a toxicity overview

December 16, 2020 - 10:21 -- Open Access
Author(s): 
Chu CS, Hwang J
Reference: 
Expert Opin Drug Saf. 2020 Dec 11

A century long history in 8-aminoquinolines, the only anti-malaria drug class preventing malaria relapse, has resulted in the approval of tafenoquine by the U.S. Food and Drug Administration (FDA) and the Australian Therapeutic Goods Administration (TGA) and to date registration in Brazil and Thailand. Tafenoquine is an alternative anti-relapse treatment for vivax malaria and malaria prophylaxis. It should not be given in pregnancy, during lactation of infants with glucose-6-phosphate dehydrogenase (G6PD) unknown or deficient status, and in those with G6PD deficiency or psychiatric illness.

Efficacy and safety of tafenoquine for malaria chemoprophylaxis (1998-2020): A systematic review and meta-analysis

November 25, 2020 - 12:45 -- Open Access
Author(s): 
Maier JD, Siegfried S, Gültekin N, Stanga Z, Baird JK, Grobusch MP, Schlagenhauf P
Reference: 
Travel Med Infect Dis. 2020 Nov 20:101908

In 2018, tafenoquine was approved for malaria chemoprophylaxis. We evaluated all available data on the safety and efficacy of tafenoquine chemoprophylaxis.

Tafenoquine for preventing relapse in people with Plasmodium vivax malaria

September 8, 2020 - 12:36 -- Open Access
Author(s): 
Rodrigo C, Rajapakse S, Fernando D
Reference: 
Cochrane Database Syst Rev. 2020 Sep 6;9:CD010458

Plasmodium vivax malaria has a persistent liver stage that causes relapse of the disease and continued P vivax transmission. Primaquine (PQ) is used to clear the liver stage of the parasite, but treatment is required for 14 days. Primaquine also causes haemolysis in people with glucose‐6‐phosphate dehydrogenase (G6PD) deficiency. Tafenoquine (TQ) is a new alternative to PQ with a longer half‐life and can be used as a single‐dose treatment.

Activities of artesunate-based combinations and tafenoquine against Babesia bovis in vitro and Babesia microti in vivo

July 21, 2020 - 15:42 -- Open Access
Author(s): 
Carvalho LJM, Tuvshintulga B, Nugraha AB, Sivakumar T, Yokoyama N
Reference: 
Parasit Vectors. 2020 Jul 20;13(1):362

Babesiosis represents a veterinary and medical threat, with a need for novel drugs. Artemisinin-based combination therapies (ACT) have been successfully implemented for malaria, a human disease caused by related parasites, Plasmodium spp. The aim of this study was to investigate whether ACT is active against Babesia in vitro and in vivo.

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