Drugs / Atovaquone
last change Jun 2026 re-read 2 minutes ago

Atovaquone

Small molecule targets STAT3 via inhibition

Developed for
pneumocystosis · malaria · Plasmodium falciparum malaria · cerebral toxoplasmosis · COVID-19 · non-small cell lung carcinoma · acute myeloid leukemia · bacterial infectious disease
+6 more · diffuse midline glioma, H3 K27M-mutant · high grade astrocytic tumor · medulloblastoma · ovarian serous adenocarcinoma · Pneumocystis infectious disease · toxoplasmosis
Investigated by
Glaxo Wellcome · National Institute of Allergy and Infectious Diseases (NIAID) · Emory University · Medicines for Malaria Venture · Pfizer · Richmond Pharmacology Limited
+27 more · University of Oxford · Armed Forces Research Institute of Medical Sciences, Thailand · Baylor College of Medicine · Cancer Research UK · Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) · Guy's and St Thomas' NHS Foundation Trust · HonorHealth Research Institute · Jimma University · Kansas State University · Ludwig-Maximilians - University of Munich · McGill University Health Centre/Research Institute of the McGill University Health Centre · Merck Healthcare KGaA, Darmstadt, Germany, an affiliate of Merck KGaA, Darmstadt, Germany · Morningside Foundation/Peach Bowl LegACy Fund · NHS Lothian · NHS Research Scotland · National Cancer Institute (NCI) · National Center for Parasitology, Entomology, and Malaria Control (CNM) · National Institute for Health Research, United Kingdom · National Institutes of Health Clinical Center (CC) · Naval Medical Research Unit-2 (NAMRU-2) · Oxford University Hospitals NHS Trust · Radboud University Medical Center · State University of New York - Upstate Medical University · U.S. Army Medical Research and Development Command · University of Texas Southwestern Medical Center · Walter Reed Army Institute of Research (WRAIR) · William Marsh Rice University

Regulatory milestones approvals, filings & regulatory actions · 2 recorded

MilestoneJurisdictionBrandIndicationDateSentence it was read from
Label expansion US (FDA) MEPRON 1999-01-05 fda.gov
Approved US (FDA) MEPRON 1992-11-25 fda.gov

Trials 28 · a red edge is where a trial was stopped

PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 02 trials
Phase 0 NCT03568994 Jul 2018 → Sep 2020 acute myeloid leukemia Baylor College of Medicine Completed No outcome recorded
Phase 0 NCT02628080 May 2016 → Oct 2018 non-small cell lung carcinoma University of Oxford Completed No outcome recorded
Phase 16 trials
Phase 1 NCT06624371 Mar 2025 → Oct 2027 expected diffuse midline glioma, H3 K27M-mutant, high grade astrocytic tumor, medulloblastoma Emory University Recruiting No outcome recorded
Phase 1 NCT04866602 Nov 2021 → Mar 2022 Medicines for Malaria Venture Completed No outcome recorded
Phase 1 NCT04648033 Dec 2020 → Oct 2023 non-small cell lung carcinoma University of Oxford Completed No outcome recorded
Phase 1 NCT04002687 Apr → Oct 2019 malaria Medicines for Malaria Venture Completed No outcome recorded
Phase 1 NCT01479361 Oct 2011 → Feb 2014 HIV infectious disease, Pneumocystis infectious disease, toxoplasmosis National Institutes of Health Clinical Center (CC) Completed No outcome recorded
Phase 1 NCT00000773 ? → Sep 1996 HIV infectious disease, pneumocystosis National Institute of Allergy and Infectious Diseases (NIAID) Completed No outcome recorded
Phase 29 trials
Phase 2 NCT05974267 Nov 2023 → Dec 2024 Plasmodium falciparum malaria Merck Healthcare KGaA, Darmstadt, Germany, an affiliate of Merck KGaA, Darmstadt, Germany Completed No outcome recorded
Phase 2 NCT05998135 Nov 2023 → Jun 2026 overdue ovarian serous adenocarcinoma Emory University Recruiting No outcome recorded
Phase 2 NCT04456153 Jul 2020 → Jan 2021 COVID-19 University of Texas Southwestern Medical Center Completed No outcome recorded
Phase 2 NCT04339426 Apr 2020 → Feb 2022 COVID-19 HonorHealth Research Institute Terminated No outcome recorded
Phase 2 NCT00984256 Sep 2009 → Apr 2010 malaria U.S. Army Medical Research and Development Command Completed No outcome recorded
Phase 2 NCT00000811 ? → Nov 2001 HIV infectious disease, bacterial infectious disease, pneumocystosis National Institute of Allergy and Infectious Diseases (NIAID) Completed No outcome recorded
Phase 2 NCT00000794 ? → Apr 1998 HIV infectious disease, cerebral toxoplasmosis National Institute of Allergy and Infectious Diseases (NIAID) Completed No outcome recorded
Phase 2 NCT00001996 HIV infectious disease, pneumocystosis Glaxo Wellcome Completed No outcome recorded
Phase 2 NCT00000655 ? → Jan 1992 HIV infectious disease, pneumocystosis National Institute of Allergy and Infectious Diseases (NIAID) Completed No outcome recorded
Phase 2/31 trial
Phase 2/3 NCT00084227 Jul 2004 → Jul 2005 Plasmodium falciparum malaria Pfizer Completed No outcome recorded
Phase 32 trials
Phase 3 NCT00000802 ? → Jul 1997 HIV infectious disease, pneumocystosis National Institute of Allergy and Infectious Diseases (NIAID) Completed No outcome recorded
Phase 3 NCT00002340 HIV infectious disease, pneumocystosis Glaxo Wellcome Completed No outcome recorded
Phase 45 trials
Phase 4 NCT07357103 Mar 2026 → Mar 2029 expected pneumocystosis McGill University Health Centre/Research Institute of the McGill University Health Centre Not yet recruiting No outcome recorded
Phase 4 NCT03726593 Oct 2018 → Aug 2022 Plasmodium falciparum malaria Armed Forces Research Institute of Medical Sciences, Thailand Unknown No outcome recorded
Phase 4 NCT02564471 Nov 2016 → Aug 2018 rabies State University of New York - Upstate Medical University Completed No outcome recorded
Phase 4 NCT00421473 Mar 2007 → Dec 2008 HIV infectious disease, malaria Radboud University Medical Center Completed No outcome recorded
Phase 4 NCT00451139 malaria Jimma University Completed No outcome recorded
Phase not applicable3 trials
NCT00001991 HIV infectious disease, pneumocystosis Glaxo Wellcome Completed No outcome recorded
NCT00001990 HIV infectious disease, pneumocystosis Glaxo Wellcome Completed No outcome recorded
NCT00001994 HIV infectious disease, cerebral toxoplasmosis Glaxo Wellcome Completed No outcome recorded
Also used as a comparator or background therapy in 16 trials
PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 15 trials
Phase 1 NCT06294912 Background Apr 2024 → Jan 2025 malaria Merck Sharp & Dohme LLC Completed No outcome recorded
Phase 1 NCT04568772 Background Nov 2020 → Jul 2021 gastroesophageal reflux disease Seoul National University Hospital Completed No outcome recorded
Phase 1 NCT02858817 Background Nov 2016 → Nov 2017 malaria University Hospital Tuebingen Completed No outcome recorded
Phase 1 NCT02450578 Comparator Oct 2015 → Apr 2016 Plasmodium falciparum malaria Medicines for Malaria Venture Completed No outcome recorded
Phase 1 NCT01858831 Comparator Apr → May 2012 malaria GlaxoSmithKline Completed No outcome recorded
Phase 1/22 trials
Phase 1/2 NCT02836002 Background Jun 2016 → Jun 2017 malaria Radboud University Medical Center Completed No outcome recorded
Phase 1/2 NCT01442168 Comparator Sep 2011 → Sep 2013 Plasmodium falciparum malaria Modus Therapeutics AB Terminated No outcome recorded
Phase 44 trials
Phase 4 NCT02297477 Comparator Dec 2014 → Dec 2015 Plasmodium falciparum malaria Armed Forces Research Institute of Medical Sciences, Thailand Unknown No outcome recorded
Phase 4 NCT01150344 Comparator Jul 2010 → Apr 2014 malaria Assistance Publique - Hôpitaux de Paris Completed No outcome recorded
Phase 4 NCT00636935 Background Feb 2008 → Aug 2013 pneumocystosis George Washington University Withdrawn No outcome recorded
Phase 4 NCT00444106 Comparator May 2007 → Nov 2008 Plasmodium falciparum malaria Novartis Completed No outcome recorded
Phase not applicable5 trials
NCT04203186 Comparator Mar 2020 → Jun 2021 Plasmodium falciparum malaria U.S. Army Medical Research and Development Command Withdrawn No outcome recorded
NCT03813108 Background Apr 2019 → Feb 2021 Plasmodium falciparum malaria Radboud University Medical Center Terminated No outcome recorded
NCT03454048 Background May → Nov 2018 Plasmodium falciparum malaria Radboud University Medical Center Completed No outcome recorded
NCT02080026 Background Jun 2014 → Jul 2015 malaria Radboud University Medical Center Completed No outcome recorded
NCT01660854 Background Jul 2012 → Jan 2013 Plasmodium falciparum malaria Radboud University Medical Center Completed No outcome recorded

Evidence & citations 15 cited values

Every value below carries the sentence it was read from. 47 sources stand behind the page.

FieldValueCited text
Known as Atovaquone “Drug: Malarone treatment When thick smear positive, of at day 21 after challenge, all volunteers will be treated with malarone. Other Name: atovaquone/proguanil” NCT01660854
44

“Continued standard of care therapy together with an oral dose of 1500 mg atovaquone twice daily (administered with a meal or snack) for up to 10 days” NCT04456153

“antibiotics (Bactrim, Pentamidine, Atovaquone, Primaquine/Clindamycin, or Trimethoprim/Dapsone)” NCT00636935

Atovaquone (ATV),Proguanil (PG) 1000-400 mg + Amodiaquine (AQ) 612 mg on days 1,2, 3.” NCT04002687

“250 mg atovaquone, 100 mg proguanil hydrochloride” NCT02450578

Atovaquone 500 mg + Proguanil 348 mg” NCT04866602

AtovaquoneNCT00984256

NCT00000811

NCT02858817

NCT04339426

NCT00000773

NCT01150344

NCT02628080

NCT05974267

NCT04568772

NCT00000655

NCT00984256

NCT02080026

NCT02836002

NCT06294912

NCT00001994

NCT03726593

NCT00421473

NCT00000794

NCT00002340

NCT06624371

NCT00001996

NCT00000802

NCT01479361

NCT04648033

NCT03813108

NCT02297477

NCT07357103

NCT01442168

NCT03454048

NCT04203186

NCT00444106

NCT02564471

NCT05998135

NCT00001990

NCT03568994

NCT01858831

NCT00001991

NCT00084227

NCT00451139

Known as 566C ChEMBL registry synonym — accepted as the source's own label CHEMBL1450
Known as 566C80 “To compare the safety of atovaquone (566C80) with intravenous (IV) pentamidine for the treatment of mild to moderate Pneumocystis carinii pneumonia (PCP) in AIDS patients who...” NCT00001996
5

“To facilitate provision of atovaquone (566C80) to patients who have mild to moderate Pneumocystis carinii pneumonia (PCP) and are intolerant and/or unresponsive to trimethoprim...” NCT00001991

“To evaluate the effectiveness of atovaquone (566C80) compared to a standard antipneumocystis agent, (SMX/TMP), for the treatment of mild to moderate Pneumocystis carinii...” NCT00000655

“Phase I Safety and Pharmacokinetics Study of Microparticulate Atovaquone (m-Atovaquone; 566C80) in HIV-Infected and Perinatally Exposed Infants and Children” NCT00000773

“To evaluate the safety and tolerance of atovaquone (566C80) in AIDS patients with central nervous system (CNS) toxoplasmosis.” NCT00001994

“atovaquone (566C80)” NCT00001990

Known as Atovacuona ChEMBL registry synonym — accepted as the source's own label CHEMBL1450
Known as Atovaquone component of malarone ChEMBL registry synonym — accepted as the source's own label CHEMBL1450
Known as Atovaquone component of malarone pediatric ChEMBL registry synonym — accepted as the source's own label CHEMBL1450
Known as ATV “Atoguanil™ is a novel complex of atovaquone (ATV) and proguanil (PG) with enhanced ATV bioavailability compared to Malarone®.” PMID 38918235 Jun 2024
1

“Atovaquone (ATV),Proguanil (PG) 1000-400 mg + Amodiaquine (AQ) 612 mg on days 1,2, 3.” NCT04002687

Known as m-Atovaquone “Phase I Safety and Pharmacokinetics Study of Microparticulate Atovaquone (m-Atovaquone; 566C80) in HIV-Infected and Perinatally Exposed Infants and Children” NCT00000773
Known as Mepron ChEMBL registry synonym — accepted as the source's own label CHEMBL1450
Known as NSC-759582 ChEMBL registry synonym — accepted as the source's own label CHEMBL1450
Known as Wellvone ChEMBL registry synonym — accepted as the source's own label CHEMBL1450
Action Inhibit “the mitochondrial inhibitor atovaquone increases tumour oxygenation in NSCLC” PMID 34964932 Dec 2021
Modality Small molecule CHEMBL1450
Route Oral Oral 566C80” NCT00001990
Target STAT3 “To quantitate the on-target STAT3 inhibitory effect of atovaquone on STAT3-dependent gene transcription.” NCT05998135