ArticleAntimicrobial agents and chemotherapy2007
Mechanism of antimalarial action of the synthetic trioxolane RBX11160 (OZ277).
Article in Antimicrobial agents and chemotherapy, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
27 citing papers in PubMed, 73 citations in OpenAlex.
- A Phase 3, Double-Blind, Randomized Study of Arterolane Maleate-Piperaquine Phosphate vs Artemether-Lumefantrine for Falciparum Malaria in Adolescent and Adult Patients in Asia and Africa.Clinical infectious diseases : an official publication of the Infectious Diseases Society of America · 2016Trial
- Trial
- Natural products as transmission-blocking agents against malaria: a comprehensive review of bioactive compounds and their therapeutic potential.Malaria journal · 2025Review
- Chemo-proteomics in antimalarial target identification and engagement.Medicinal research reviews · 2023Review
- Reactive Oxygen Species as the Brainbox in Malaria Treatment.Antioxidants (Basel, Switzerland) · 2021Review
- Challenges to replace ACT as first-line drug.Malaria journal · 2017Article
- In vitro activity of anti-malarial ozonides against an artemisinin-resistant isolate.Malaria journal · 2017Article
- Honoring antiparasitics: The 2015 Nobel Prize in Physiology or Medicine.Biomedical journal · 2016Review
- Monoclonal Antibodies That Recognize the Alkylation Signature of Antimalarial Ozonides OZ277 (Arterolane) and OZ439 (Artefenomel).ACS infectious diseases · 2016Article
- Rearrangements of organic peroxides and related processes.Beilstein journal of organic chemistry · 2016Review
- Fixed dose combination of arterolane and piperaquine: a newer prospect in antimalarial therapy.Annals of medical and health sciences research · 2014Review
- Synthesis of five- and six-membered cyclic organic peroxides: Key transformations into peroxide ring-retaining products.Beilstein journal of organic chemistry · 2014Review
- The lipophilic bullet hits the targets: medicinal chemistry of adamantane derivatives.Chemical reviews · 2013Review
- In vitro interaction of artemisinin derivatives or the fully synthetic peroxidic anti-malarial OZ277 with thapsigargin in Plasmodium falciparum strains.Malaria journal · 2013Article
- The global pipeline of new medicines for the control and elimination of malaria.Malaria journal · 2012Review
- Investigating the antimalarial action of 1,2,4-trioxolanes with fluorescent chemical probes.Journal of medicinal chemistry · 2011Article
- The molecular mechanism of action of artemisinin--the debate continues.Molecules (Basel, Switzerland) · 2010Review
- Artemisinin directly targets malarial mitochondria through its specific mitochondrial activation.PloS one · 2010Article
- Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.Antimicrobial agents and chemotherapy · 2010Article
- Next-Generation Antimalarial Drugs: Hybrid Molecules as a New Strategy in Drug Design.Drug development research · 2010Article
Corrections and comments
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Authors and funding
5 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
RBX11160 (OZ277) is a fully synthetic peroxidic antimalarial in clinical development. To study the possible mechanisms of action of RBX11160, we have examined its ability to inhibit PfATP6, a sarcoplasmic reticulum calcium ATPase and proposed target for semisynthetic peroxidic artemisinin derivatives. RBX11160 inhibits PfATP6 (apparent half-maximal inhibitory constant=7,700 nM) less potently than artemisinin (79 nM). Inhibition of PfATP6 is abrogated by desferrioxamine, an iron-chelating agent. Consistent with this finding, the killing of Plasmodium falciparum organisms by RBX11160 in vitro is antagonized by desferrioxamine. Artesunate and RBX11160 also act antagonistically against P. falciparum in vitro. A fluorescent derivative of RBX11160 localizes to the parasite cytosol in some parasites and to the food vacuole in other parasites. These data demonstrate that there are both similarities and differences between the antimalarial properties of RBX11160 and those of semisynthetic antimalarials such as artesunate and artemisinin.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.