Alisporivir
Also known as: Alisporivir, ALV, Cyclophilin inhibitor Debio 025, DEB025, Debio 025, Debio‑025, SCY‑635
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Summary
Alisporivir (Debio‑025) is a non‑immunosuppressive cyclosporine A derivative that inhibits cyclophilin. It has been studied in hepatitis C, HIV, coronavirus and muscular dystrophy trials but development was halted due to hepatotoxicity; it has never received regulatory approval.
Mechanism of Action
Binds cyclophilin A, inhibiting its peptidyl‑prolyl cis‑trans isomerase activity and thereby blocking replication of several viruses and modulating host cell pathways.
Routes of Administration
Goals & Uses
- Duchenne muscular dystrophyMuscle DiseaseLow
- Treatment of chronic hepatitis C infectionAntiviral / Infectious DiseaseModerate
- Hepatitis C virus infectionAntiviralModerate
- Prevention of ischemia-reperfusion injuryCardioprotection / CytoprotectionLow
- Combination antiviral therapy (with pegIFN/ribavirin or DAAs)Antiviral Combination RegimenModerate
- Treatment of mitochondrial diseases (e.g., MELAS, Sengers syndrome)Rare / Orphan DiseaseLow
- Broad‑spectrum antiviral therapyAntiviralModerate
Contraindications
- Hypersensitivity to cyclosporine analoguesAllergy / ImmunologyHigh
- Severe hepatic impairmentOrganHighLiver function concerns
- Known hypersensitivity to cyclosporine derivativesAllergyModerate
- PregnancyPopulationModeratePotential fetal risk or insufficient safety data
- History of pancreatitisGastrointestinalHigh
Adverse Effects
- Elevated transaminases (ALT/AST)HepaticCommon
- HeadacheNeurologicCommonPain in the head or upper neck
- Elevated liver enzymes (ALT/AST)HepaticUncommon
- NauseaGastrointestinalCommonFeeling of sickness or urge to vomit
- FatigueGeneralCommonLow energy or tiredness
- Acute pancreatitisGastrointestinalUncommon
- HyperbilirubinemiaHepaticUncommon
Drug Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole, ritonavir)High
- Cyclosporine AModerate
- P‑gp inhibitors (e.g., verapamil)Moderate
- Strong CYP3A4 inducers (e.g., rifampicin, carbamazepine)Moderate
- P-glycoprotein substratesModerate
Population Constraints
- PregnancyReproductive SafetyRelative
- Renal impairmentOrgan ImpairmentRelative
- Pediatric patientsAgeRelative
- Patients with prior pancreatitis or risk factors for pancreatitisGastrointestinalAbsolute
- Elderly (>75 y)AgeRelative
Regulatory Status
- European UnionInvestigationalClinical trial authorization only; no EMA marketing authorization.
- United StatesInvestigationalInvestigational New Drug (IND) status; no FDA approval.
- United KingdomInvestigationalMHRA clinical trial permission; not marketed.
Development discontinued after phase II/III studies because of liver safety signals; not approved in any jurisdiction.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Alisporivir?
Alisporivir (Debio‑025) is a non‑immunosuppressive cyclosporine A derivative that inhibits cyclophilin. It has been studied in hepatitis C, HIV, coronavirus and muscular dystrophy trials but development was halted due to hepatotoxicity; it has never received regulatory approval.
What is Alisporivir used for?
Alisporivir is educationally associated with: Duchenne muscular dystrophy, Treatment of chronic hepatitis C infection, Hepatitis C virus infection, Prevention of ischemia-reperfusion injury, Combination antiviral therapy (with pegIFN/ribavirin or DAAs), Treatment of mitochondrial diseases (e.g., MELAS, Sengers syndrome), Broad‑spectrum antiviral therapy. Educational only — not medical advice.
How is Alisporivir administered?
Recorded routes of administration: Oral.
What are the potential side effects of Alisporivir?
Reported adverse effects include: Elevated transaminases (ALT/AST), Headache, Elevated liver enzymes (ALT/AST), Nausea, Fatigue, Acute pancreatitis, Hyperbilirubinemia. This list is not exhaustive — consult a qualified clinician.
Who should avoid Alisporivir?
Recorded contraindications: Hypersensitivity to cyclosporine analogues, Severe hepatic impairment, Known hypersensitivity to cyclosporine derivatives, Pregnancy, History of pancreatitis. Consult a qualified clinician before use.