Drug name
Last update: Jul 2025Atovaquone
Developer(s)
Drug information
Not provided
Atovaquone
Mepron
Small molecule
Not provided
Atovaquone is a broad spectrum antiparasitic drug utilised for the treatment and prevention of malaria. As a structural mimic of coenzyme Q (also known as ubiquinone), atovaquone functions by selectively binding the malarial cytochrome b protein resulting in the disruption of both the parasite’s transmitochondrial membrane potential and pyrimidine biosynthesis. Atovaquone is often synergistically combined with proguanil to avoid the possibility of emerging drug-resistance in erythrocytic P. falciparum. However, recent research has suggested that mosquitoes are unable to transmit atovaquone-resistant P. falciparum, indicating the potential viability of atovaquone monotherapy for malaria chemoprophylaxis. Long-acting injectable versions of atovaquone are currently in preclinical development.
Unknown
Unknown
Therapeutic area(s)
- Malaria
- Pre-Exposure Prophylaxis (PrEP)
- Treatment
Administration route
Oral, Intramuscular
Associated long-acting platforms
Aqueous drug particle suspension
Use of drug
- Administered by a nurse
- Administered by a specialty health worker
Not provided
Dosage
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Associated compounds, formulations and regimens
Not provided
Associated technologies
CompareAdditional information
Developer(s)
GSK
GSK (formerly GlaxoSmithKline) is a British-based global biopharmaceutical company that manufactures therapeutic medicines and vaccines across four core areas including oncology, respiratory/immunology, HIV and infectious diseases. Founded in 2000 following a merger between Glaxo Wellcome and SmithKline Beecham, GSK are currently moving their global headquarters from Brentford to central London.
Various generic manufacturersVarious generic manufacturers
Drug structure
Scale-up and manufacturing prospects
Long-acting versions of atovaquone are currently in pre-clinical development. Atovaquone’s physiochemical properties including its low systemic clearance and high hydrophobicity make it a suitable candidate for long-acting injectable (LAI) formulation. Development approaches for solid-drug nanoparticle formulations focus on attrition methods or require the generation of drug-associated nano-carriers. However, an alternative approach may instead utilise emulsion-templated freeze drying screening to identify high drug content solid-drug particles prior to scale-up by emulsion spray drying.
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Researchers as part of the LONGEVITY project have developed a preclinical LAI solid-drug nanoparticle (SDN) atovaquone formulation for intramuscular admin. Initially, a library of SDNs containing atovaquone in combination with surfactant and polymer stabiliser excipients was generated, creating a range of formulations composing of 80% atovaquone, 13% polymer and 7% surfactant using FDA-approved inactive ingredients. Formulations were retained if they met the following criteria: (1) SDN average diameter <1000nm, (2) full aqueous dispersion at 0.5 mg/ml, (3) uniformity of size and drug release.
Dynamic light-scattering analysis equipment (e.g. using Malvern Zetasizer Nano ZS) to measure the Z-average diameter of solid drug nanoparticles to assess formulation stability.
Excipients & delivery device(s)
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No delivery device
Safety, Efficacy and Evidence Summary
Not provided
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Atovaquone compound
Not provided
US5053432
Compound
BURROUGHS WELLCOME CO
Not provided
April 14, 2003
expired