ArticleThe Journal of antimicrobial chemotherapy2016
Efficacy of OZ439 (artefenomel) against early Plasmodium falciparum blood-stage malaria infection in healthy volunteers.
Article in The Journal of antimicrobial chemotherapy, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 46 papers.
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The trial behind it
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Who cites it
46 citing papers in PubMed, 102 citations in OpenAlex.
- Trial
- Trial
- Safety, pharmacokinetics, and antimalarial activity of the novel plasmodium eukaryotic translation elongation factor 2 inhibitor M5717: a first-in-human, randomised, placebo-controlled, double-blind, single ascending dose study and volunteer infection study.The Lancet. Infectious diseases · 2021Trial
- Safety, infectivity and immunogenicity of a genetically attenuated blood-stage malaria vaccine.BMC medicine · 2021Trial
- Trial
- Safety and parasite clearance of artemisinin-resistant Plasmodium falciparum infection: A pilot and a randomised volunteer infection study in Australia.PLoS medicine · 2020Trial
- A controlled human malaria infection model enabling evaluation of transmission-blocking interventions.The Journal of clinical investigation · 2018Trial
- A Phase II pilot trial to evaluate safety and efficacy of ferroquine against early Plasmodium falciparum in an induced blood-stage malaria infection study.Malaria journal · 2016Trial
- Article
- Double Mutations inbioRxiv : the preprint server for biology · 2026Article
- Artemisinin-Related Therapeutic Strategies for Autoimmune Thyroiditis: Chemokine-Receptor Networks, Spatial Thyroid Biology, and Molecular Mechanisms.Drug design, development and therapy · 2026Review
- Controlled human malaria infection studies: insights into recent advances and key immunological and ethical implementation lessons.Frontiers in immunology · 2025Review
- Recent advances, challenges and updates on the development of therapeutics for malaria.EXCLI journal · 2024Review
- Semi-mechanistic population pharmacokinetic/pharmacodynamic modeling of aAntimicrobial agents and chemotherapy · 2023Article
- Parasite proteostasis and artemisinin resistance.Research square · 2023Article
- Antimalarial mass drug administration in large populations and the evolution of drug resistance.PLOS global public health · 2023Article
- Safety, Tolerability, and Parasite Clearance Kinetics in Controlled Human Malaria Infection after Direct Venous Inoculation of Plasmodium falciparum Sporozoites: A Model for Evaluating New Blood-Stage Antimalarial Drugs.The American journal of tropical medicine and hygiene · 2022Article
- Antimalarial Activity of Artefenomel Against Asexual Parasites and Transmissible Gametocytes During Experimental Blood-Stage Plasmodium vivax Infection.The Journal of infectious diseases · 2022Article
- Scoping Review of Antimalarial Drug Candidates in Phase I and II Drug Development.Antimicrobial agents and chemotherapy · 2022Article
- Cytochrome P450-Mediated Metabolism and CYP Inhibition for the Synthetic Peroxide Antimalarial OZ439.ACS infectious diseases · 2021Article
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 2 countries.
Funding
Abstract
objectivesOZ439, or artefenomel, is an investigational synthetic ozonide antimalarial with similar potency, but a significantly improved pharmacokinetic profile, compared with artemisinins. We wished to measure key pharmacokinetic and pharmacodynamic parameters and the pharmacokinetic/pharmacodynamic relationship of artefenomel in humans to guide the drug's further development as combination therapy in patients. PATIENTS AND
methodsWe tested artefenomel in the human induced blood-stage malaria (IBSM) model. Plasmodium infection was monitored by quantitative PCR (qPCR) and upon reaching 1000 parasites/mL single doses of 100, 200 and 500 mg of artefenomel were administered orally with evaluation of drug exposure and parasitaemia until rescue treatment after 16 days or earlier, if required.
resultsA single 100 mg dose had only a transient effect, while the 200 mg dose resulted in a significant reduction in parasitaemia before early recrudescence. At the highest (500 mg) dose, initial clearance of parasites below the limit of detection of qPCR was observed, with a 48 h parasite reduction ratio (PRR48) >10 000 and a parasite clearance half-life of 3.6 h (95% CI 3.4-3.8 h). However, at this dose, recrudescence was seen in four of eight subjects 6-10 days after treatment. Pharmacokinetic/pharmacodynamic modelling predicted an MIC of 4.1 ng/mL.
conclusionsThese results confirm the antimalarial potential of artefenomel for use in a single-exposure combination therapy. The observations from this study support and will assist further clinical development of artefenomel.
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