Valinomycin

Summary

Valinomycin is a naturally occurring cyclic depsipeptide produced by Streptomyces species. It is one of the most potent and selective K+ ionophores known, widely used as a research tool in membrane biophysics and biochemistry. It has demonstrated broad-spectrum antimicrobial, antifungal, antiviral (including anti-SARS-CoV activity), and anticancer activities in preclinical studies, but has not advanced to approved clinical use due to significant systemic toxicity.

Mechanism of Action

Valinomycin is a potassium-selective ionophore that forms a lipophilic complex with K+ ions, facilitating their transport across lipid bilayer membranes down the electrochemical gradient, thereby dissipating the mitochondrial membrane potential and disrupting cellular energy production.

Routes of Administration

Goals & Uses

• Antimicrobial activityAnti InfectiveLow
• Anticancer activityOncologyLow
• Antiviral activity (SARS-CoV)AntiviralLow
• Ion channel / transport researchBasic ResearchHigh
• Research tool – membrane potential studiesBasic ResearchHigh

Contraindications

• Human therapeutic administrationClinical UseHigh
• Renal impairmentOrgan DysfunctionHigh
• Cardiac arrhythmia riskCardiovascularHigh

Adverse Effects

• Mitochondrial uncouplingMetabolicCommon
• Hyperkalemia / hypokalemiaElectrolyte DisturbanceUnknown
• Apoptosis inductionCellular ToxicityCommon
• HemolysisHematologicUnknown
• CytotoxicityCell ViabilityCommon

Drug Interactions

• Cardiac glycosides (e.g., digoxin)High
• Mitochondrial complex inhibitors (e.g., rotenone)High
• Potassium-sparing diureticsHigh

Population Constraints

• All human populations (therapeutic use)GeneralAbsolute
• Pediatric patientsAgeAbsolute
• Patients with cardiac diseaseCardiovascularAbsolute
• Pregnant individualsReproductiveAbsolute

Regulatory Status

• European UnionUnapprovedNot approved by EMA; used solely as a laboratory reagent.
• United StatesUnapprovedNot FDA-approved for any human use; classified as a research chemical.
• United KingdomUnapprovedNot approved by MHRA for any therapeutic indication.

Not approved by FDA, EMA, or any major regulatory authority for human therapeutic use. Used exclusively as a laboratory research reagent. Some interest in repurposing as an antiviral or anticancer agent remains at the preclinical stage.

Evidence & Sources

No sources recorded yet.