Pepstatin
Also known as: Acetyl-pepstatin, Isovaleryl-Val-Val-Sta-Ala-Sta, Pepstatin A, Pepstatin I, Statine-containing hexapeptide
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Summary
Pepstatin is a hexapeptide (Pepstatin A) containing the unusual amino acid statine; it is widely used as a potent, specific inhibitor of aspartic proteases in biochemical research.
Mechanism of Action
Reversible competitive inhibition of aspartic proteases (e.g., pepsin, cathepsin D) by binding to the active site
Routes of Administration
Goals & Uses
- HIV protease inhibitionAntiviral ResearchLow
- Anti-cancer (cathepsin D inhibition)Investigational TherapeuticLow
- Protease inhibitor cocktail componentResearch ToolHigh
- Neuroprotection in neurodegeneration modelsInvestigational TherapeuticLow
- Protease inhibitionResearch ToolHigh
- Inhibition of cathepsin D in lysosomal researchResearch ToolHigh
Contraindications
- Clinical therapeutic use in humansRegulatoryHigh
Adverse Effects
- Poor oral/systemic bioavailabilityPharmacokineticCommon
- Non-selective aspartyl protease inhibitionPharmacodynamicCommon
Drug Interactions
- Renin inhibitorsModerate
Population Constraints
- Human clinical populationsGeneralAbsolute
Regulatory Status
- European UnionUnapprovedNo EMA approval; sold as laboratory chemical.
- United StatesUnapprovedAvailable only as a research reagent; no FDA approval or IND on record for therapeutic use.
- United KingdomUnapprovedNo MHRA approval; available as research reagent only.
Not approved for any clinical indication; used only as a research reagent.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Pepstatin?
Pepstatin is a hexapeptide (Pepstatin A) containing the unusual amino acid statine; it is widely used as a potent, specific inhibitor of aspartic proteases in biochemical research.
What is Pepstatin used for?
Pepstatin is educationally associated with: HIV protease inhibition, Anti-cancer (cathepsin D inhibition), Protease inhibitor cocktail component, Neuroprotection in neurodegeneration models, Protease inhibition, Inhibition of cathepsin D in lysosomal research. Educational only — not medical advice.
How is Pepstatin administered?
Recorded routes of administration: Intravenous, Topical.
What are the potential side effects of Pepstatin?
Reported adverse effects include: Poor oral/systemic bioavailability, Non-selective aspartyl protease inhibition. This list is not exhaustive — consult a qualified clinician.
Who should avoid Pepstatin?
Recorded contraindications: Clinical therapeutic use in humans. Consult a qualified clinician before use.