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atovaquone

Trade name: mepron

Small moleculeapprovedOrphan Drug FDA

Approved

Nov 25, 1992

Atovaquone is a chemical compound that belongs to the class of naphthoquinones; it is manufactured in the US in the liquid form, or oral suspension, under the brand name Mepron. Meron is used for the treatment or prevention of Pneumocystis carinii pneumonia in patients who are intolerant to trimethoprim-sulfamethoxazole (TMP-SMX). Also indicated for the acute oral treatment of mild to moderate PCP in patients who are intolerant to TMP-SMX. The mechanism of action against Pneumocystis jiroveci has not been fully elucidated. In Plasmodium species, the site of action appears to be the cytochrome bc1 complex (Complex III). Several metabolic enzymes are linked to the mitochondrial electron transport chain via ubiquinone. Inhibition of electron transport by atovaquone results in indirect inhibition of these enzymes. The ultimate metabolic effects of such blockade may include inhibition of nucleic acid and adenosine triphosphate (ATP) synthesis. Several laboratories, using different in vitro methodologies, have shown the IC50 (50% inhibitory concentration) of atovaquone against P. jiroveci to be 0.1 to 3.0 mcg/mL. — NCATS

Clinical trial activity

52 trials · 45 clinical orgs · 14 marketing orgs

Phase 1
17
Phase 2
14
Phase 3
4
Phase 4
9

Earliest trial started Nov 2, 1999 (NCT00001990)

Timeline

1990s

  1. Sep 10, 1990

    Orphan Drug Designation

  2. Nov 25, 1992

    GlaxoSmithKline — Earliest FDA Approval

  3. Nov 25, 1992

    GlaxoSmithKline — NDA Organization

  4. Nov 25, 1992

    GlaxoSmithKline — NDA Secondary Org

  5. Jan 1, 1999

    Earliest Phase 1 Sponsor(trial)

  6. Jan 1, 1999

    Earliest Phase 2 Sponsor(trial)

  7. Jan 1, 1999

    Earliest Phase 3 Sponsor(trial)

2000s

  1. Jul 14, 2000

    GlaxoSmithKline — Marketing Organization

2010s

  1. Jan 12, 2011

    Glenmark Pharmaceuticals — Marketing Organization

  2. Mar 18, 2014

    Amneal Pharmaceuticals — Marketing Organization

  3. May 27, 2014

    Mylan — Marketing Organization

  4. Apr 28, 2017

    Paddock Laboratories — Marketing Organization

  5. Apr 28, 2017

    Padagis Us — Marketing Organization

  6. Apr 28, 2017

    Chartwell Pharmaceuticals — Marketing Organization

  7. Oct 11, 2017

    Apotex — Marketing Organization

  8. Sep 11, 2018

    Lupin — Marketing Organization

  9. Oct 11, 2018

    Hetero Labs Ltd — Marketing Organization

  10. May 31, 2019

    Abhai LLC — Marketing Organization

2020s

  1. Mar 30, 2021

    Bionpharma Inc — Marketing Organization

  2. Oct 25, 2021

    Abon Pharmaceuticals — Marketing Organization

  3. Oct 25, 2021

    Pharmaceutical Associates — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Combination products

  • malarone pediatric

    with proguanil

    Also known as malarone

Approval history

  • approvedPriority reviewNov 25, 1992

Chemistry & pharmacology

Loading structure…

SMILES

OC1=C([C@H]2CC[C@@H](CC2)C3=CC=C(Cl)C=C3)C(=O)C4=CC=CC=C4C1=O
Mol. weight
366.837 g/mol
Lipinski Ro5
1 violation(s)
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Prescription Only

Oral

Yes

Parenteral

No

Topical

No

Sources

Also known as

  • 2-(trans-4-(p-chlorophenyl)cyclohexyl)-3-hydroxy-1,4-naphthoquinone
  • 2-(trans-4-(p-chlorophenyl)cyclohexyl)-3-hydroxy-1,4-naphthoquinone
  • 566c
  • 566c
  • 566c80
  • 566c80
  • 566c80
  • 566c80
  • 566c80
  • 566c80
  • acuvel
  • acuvel
  • atovaquone
  • atovaquone
  • atovaquone
  • atovaquone
  • atovaquone
  • atovaquone
  • atovaquone
  • atovaquone
  • atovaquone
  • atovaquone and proguanil
  • malarone
  • malarone
  • malarone
  • malarone
  • mepron
  • mepron
  • mepron
  • mepron
  • wellvone
  • wellvone
  • wellvone

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07011511Phase 1Jun 30, 2025Medicines for Malaria Venture, Quotient, The Doctors Laboratory Ltd
NCT06624371Phase 1Jan 31, 2025Emory University
NCT06558643Phase 1Aug 27, 2024Medicines for Malaria Venture, Quotient, The Doctors Laboratory Ltd
NCT06294912Phase 1Apr 18, 2024Merck
NCT05974267Phase 2Nov 28, 2023Merck KGaA
NCT05998135Phase 2Sep 1, 2023Emory University, National Cancer Institute (NCI)
NCT04866602Phase 1Nov 30, 2021Medicines for Malaria Venture, Richmond Pharmacology
NCT04648033Phase 1Nov 30, 2020Cancer Research UK, National Institute for Health Research, United Kingdom, NHS Lothian, NHS Research Scotland, University of Oxford
NCT04568772Phase 1Oct 31, 2020Seoul National University
NCT04339426N/AApr 30, 2020HonorHealth Research Institute
NCT04203186N/AMar 31, 2020United States Army, United States Navy
NCT03991208Phase 4May 24, 2019United States Army
NCT04002687Phase 1Apr 4, 2019Medicines for Malaria Venture, Richmond Pharmacology
NCT03813108N/AApr 1, 2019PATH, Radboud University
NCT03726593Phase 4Oct 4, 2018Government of Thailand, National Center for Parasitology, Entomology and Malaria Control
NCT03278808Phase 2Sep 15, 2018United States Army
NCT03568994Early Phase 1 (Phase 1)Jul 31, 2018Baylor University, William Marsh Rice University
NCT03454048N/AMay 7, 2018PATH, Radboud University, University of Queensland
NCT02858817Phase 1Nov 28, 2016Sanaria Inc., University of Tuebingen
NCT02836002Phase 1/Phase 2 (Phase 2)Jun 1, 2016PATH, Radboud University, University of Queensland
Showing 20 of 52 trials
Page 1 / 3

Organizations

Research & Development (45)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Radboud UniversityAcademic/Hospital101032007
Glaxo WellcomeFor profit7531999
National Institute of Allergy and Infectious Diseases (NIAID)Government6631999
United States ArmyGovernment6532006
Medicines for Malaria VentureAcademic/Hospital5512015
Leiden UniversityAcademic/Hospital3012011
PATHAcademic/Hospital3022016
University of OxfordAcademic/Hospital3222011
Bill and Melinda Gates FoundationAcademic/Hospital2012014
Emory UniversityAcademic/Hospital2222023
Government of ThailandGovernment2212014
National Center for Parasitology, Entomology and Malaria ControlGovernment2012014
National Institutes of Health (NIH)Government2121999
PfizerFor profit2121999
QuotientFor profit2012024
Richmond PharmacologyFor profit2012019
The Doctors Laboratory LtdAcademic/Hospital2012024
United States NavyGovernment2022014
University of QueenslandAcademic/Hospital2022016
University of TuebingenAcademic/Hospital2112015
45 organizations
Page 1 / 3

Marketing (24)

OrganizationOrg typeRelationshipDate
Abhai LLCFor profitMKTGMay 31, 2019
Abon PharmaceuticalsFor profitMKTGOct 25, 2021
Amneal PharmaceuticalsFor profitMKTGMar 18, 2014
ApotexFor profitMKTGOct 11, 2017
ApotexFor profitSYNOct 11, 2017
Bionpharma IncFor profitMKTGMar 30, 2021
Bionpharma IncFor profitSYNMar 30, 2021
Chartwell PharmaceuticalsFor profitMKTGApr 28, 2017
GlaxoSmithKlineFor profitMKTGJul 14, 2000
GlaxoSmithKlineFor profitNDANov 25, 1992
GlaxoSmithKlineFor profitNDA2Nov 25, 1992
Glenmark PharmaceuticalsFor profitMKTGJan 12, 2011
Glenmark PharmaceuticalsFor profitSYNNov 21, 2018
Glenmark PharmaceuticalsFor profitSYNJan 12, 2011
Glenmark PharmaceuticalsFor profitSYNNov 21, 2018
Hetero Labs LtdFor profitMKTGOct 11, 2018
LupinFor profitMKTGSep 11, 2018
LupinFor profitSYNSep 11, 2018
MylanFor profitMKTGMay 27, 2014
MylanFor profitSYNMay 27, 2014
Padagis UsFor profitMKTGApr 28, 2017
Paddock LaboratoriesFor profitSYNApr 28, 2017
Paddock LaboratoriesFor profitMKTGApr 28, 2017
Pharmaceutical AssociatesFor profitMKTGOct 25, 2021