ArticleAntimicrobial agents and chemotherapy2015
The Oral Antimalarial Drug Tafenoquine Shows Activity against Trypanosoma brucei.
Article in Antimicrobial agents and chemotherapy, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers, 1 of them a synthesis that pooled it.
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Who cites it
13 citing papers in PubMed, 1 synthesis or guideline pooled it, 27 citations in OpenAlex.
- Promising Drug Repurposing Candidates Targeting Free-Living Amoebae: A Systematic and Critical Review of Laboratory-Based Evidence.Pathogens (Basel, Switzerland) · 2026Pooled it
- Tafenoquine: A Breakthrough Option for Babesiosis Treatment.Tropical medicine and infectious disease · 2026Article
- Tafenoquine-Atovaquone Combination Achieves Radical Cure and Confers Sterile Immunity in Experimental Models of Human Babesiosis.The Journal of infectious diseases · 2024Article
- Efficacy Evaluation of 10-Hydroxy Chondrofoline and Tafenoquine againstPharmaceuticals (Basel, Switzerland) · 2022Article
- Tafenoquine Is a Promising Drug Candidate for the Treatment of Babesiosis.Antimicrobial agents and chemotherapy · 2021Article
- Synthesis and In Vitro Antiprotozoan Evaluation of 4-/8-Aminoquinoline-based Lactams and Tetrazoles.Molecules (Basel, Switzerland) · 2020Article
- Tafenoquine: A Step toward Malaria Elimination.Biochemistry · 2020Article
- Tafenoquine: First Global Approval.Drugs · 2018Review
- Autophagic-related cell death of Trypanosoma brucei induced by bacteriocin AS-48.International journal for parasitology. Drugs and drug resistance · 2018Article
- Discovery of a quinoline-based phenyl sulfone derivative as an antitrypanosomal agent.Bioorganic & medicinal chemistry letters · 2018Article
- Fresh insights into the pyrimidine metabolism in the trypanosomatids.Parasites & vectors · 2018Review
- G-Quadruplex Identification in the Genome of Protozoan Parasites Points to Naphthalene Diimide Ligands as New Antiparasitic Agents.Journal of medicinal chemistry · 2018Article
- Interactions between tafenoquine and artemisinin-combination therapy partner drug in asexual and sexual stage Plasmodium falciparum.International journal for parasitology. Drugs and drug resistance · 2017Article
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The protozoan parasite Trypanosoma brucei causes human African trypanosomiasis, or sleeping sickness, a neglected tropical disease that requires new, safer, and more effective treatments. Repurposing oral drugs could reduce both the time and cost involved in sleeping sickness drug discovery. Tafenoquine (TFQ) is an oral antimalarial drug belonging to the 8-aminoquinoline family which is currently in clinical phase III. We show here that TFQ efficiently kills different T. brucei spp. in the submicromolar concentration range. Our results suggest that TFQ accumulates into acidic compartments and induces a necrotic process involving cell membrane disintegration and loss of cytoplasmic content, leading to parasite death. Cell lysis is preceded by a wide and multitarget drug action, affecting the lysosome, mitochondria, and acidocalcisomes and inducing a depolarization of the mitochondrial membrane potential, elevation of intracellular Ca(2+), and production of reactive oxygen species. This is the first report of an 8-aminoquinoline demonstrating significant in vitro activity against T. brucei.
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Registered trials
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