Drugs / Atovaquone
last change Mar 2026 re-read 9 days 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

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 Mixed
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 · 1 missed
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 → Mar 2027 expected 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 Missed primary
Phase 2 NCT04339426 Apr 2020 → Feb 2022 COVID-19 HonorHealth Research Institute Terminated No outcome recorded Stop: Enrollment
Phase 2 NCT00984256 Sep 2009 → Apr 2010 malaria U.S. Army Medical Research and Development Command 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 NCT00000794 ? → Apr 1998 HIV infectious disease, cerebral toxoplasmosis National Institute of Allergy and Infectious Diseases (NIAID) 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 NCT00001996 — HIV infectious disease, pneumocystosis Glaxo Wellcome 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
— NCT00001994 — HIV infectious disease, cerebral toxoplasmosis Glaxo Wellcome Completed No outcome recorded
— NCT00001990 — HIV infectious disease, pneumocystosis Glaxo Wellcome Completed No outcome recorded
Comparator or background therapy16 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

Press releases naming this drug 2 releases

DateIssuerRelease
2018-11-12 Lupin Limited Lupin launches generic Atovaquone Oral Suspension USP in the US lupin.com ↗
2018-09-12 Lupin Limited Lupin receives FDA approval for generic Atovaquone Oral Solution USP lupin.com ↗

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 ↗

“Atovaquone” NCT00984256 ↗

NCT00000655 ↗

NCT06624371 ↗

NCT02836002 ↗

NCT00000811 ↗

Show 34 more sources

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 ↗