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Mepron (ATOVAQUONE)
Mepron works by inhibiting the electron transport chain in the mitochondria of Plasmodium parasites, ultimately leading to their death.
Mepron (Atovaquone) is a small molecule antimalarial drug developed by Wellcome Foundation and currently owned by GlaxoSmithKline LLC. It targets the ATP-binding cassette sub-family G member 2 and is used to treat and prevent various forms of malaria, including chloroquine-resistant Plasmodium falciparum, as well as Pneumocystis carinii pneumonia. Mepron is off-patent and has multiple generic manufacturers. It has a half-life of 63 hours and bioavailability of 23%. Key safety considerations include potential liver toxicity and interactions with other medications.
At a glance
| Generic name | ATOVAQUONE |
|---|---|
| Sponsor | Glaxosmithkline Llc |
| Drug class | Antimalarial [EPC] |
| Target | ATP-binding cassette sub-family G member 2 |
| Modality | Small molecule |
| Therapeutic area | Immunology |
| Phase | FDA-approved |
| First approval | 1992 |
Mechanism of action
The constituents, atovaquone and proguanil hydrochloride, interfere with different pathways involved in the biosynthesis of pyrimidines required for nucleic acid replication. Atovaquone is selective inhibitor of parasite mitochondrial electron transport. Proguanil hydrochloride primarily exerts its effect by means of the metabolite cycloguanil, dihydrofolate reductase inhibitor. Inhibition of dihydrofolate reductase in the malaria parasite disrupts deoxythymidylate synthesis.
Approved indications
- Chloroquine-Resistant Plasmodium Falciparum Malaria Prevention
- Falciparum malaria
- Plasmodium Falciparum Malaria Prevention
- Pneumocystis Carinii Pneumonia Prevention
- Pneumocystosis jiroveci pneumonia
Common side effects
- Rash
- Diarrhea
- Nausea
- Fever
- Treatment-limiting adverse reactions
- Headache
- Vomiting
- Sweat
- Insomnia
- Cough
- Monilia, oral
- Laboratory abnormality
Drug interactions
- metoclopramide
- tetracycline
- zidovudine
Key clinical trials
- First-in-Human PfSPZ-LARC2 Vaccination/CHMI (PHASE1)
- Efficacy, Safety, and PK of M5717 in Combination With Pyronaridine as Chemoprevention in Adults and Adolescents With Asymptomatic Plasmodium Falciparum Infection (CAPTURE-2) (PHASE2)
- Atovaquone With Radical ChemorADIotherapy in Locally Advanced NSCLC (PHASE1)
- Atovaquone (Mepron®) Combined With Conventional Chemotherapy for de Novo Acute Myeloid Leukemia (AML) (EARLY_PHASE1)
- Positioning Second-line Therapies for Pneumocystis Jirovecii Pneumonia (PCP Alternatives) (PHASE4)
- Repurposing Atovaquone for the Treatment of Platinum-Resistant Ovarian Cancer (PHASE2)
- Atovaquone Combined With Radiation in Children With Malignant Brain Tumors (PHASE1)
- A Study to Evaluate Antimalarial Activity and Safety of MK-7602 in Healthy Adults (MK-7602-003) (PHASE1)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Mepron CI brief — competitive landscape report
- Mepron updates RSS · CI watch RSS