Voclosporin
Also known as: Cyclosporin analogue C, ISA-247, ISA247, Lupkynis, Voclosporin
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Summary
Voclosporin (ISA247) is an oral, modified cyclosporine A analog approved for the treatment of active lupus nephritis. It provides immunosuppression by inhibiting calcineurin, reducing renal inflammation and proteinuria.
Mechanism of Action
Binds cyclophilin, forming a complex that inhibits calcineurin phosphatase activity, thereby suppressing T‑cell activation and cytokine production (e.g., IL‑2).
Routes of Administration
Goals & Uses
- T-cell immunosuppressionImmunologyHigh
- IgA nephropathy (investigational)RenalLow
- Lupus nephritis remissionAutoimmune Renal DiseaseHigh
- Proteinuria reductionRenalHigh
- Podocyte stabilizationRenalModerate
- Lupus nephritis treatmentAutoimmune / RenalHigh
- Reduce systemic disease activityAutoimmune DiseaseModerate
Contraindications
- Live vaccinesVaccinationModerate
- Known hypersensitivity to voclosporin or cyclosporineAllergyHigh
- Active serious infectionsInfectiousHigh
- Hypersensitivity to voclosporin or cyclosporin analoguesAllergyHigh
- Severe uncontrolled hypertensionCardiovascularHigh
- Severe renal impairment or eGFR <45 mL/min/1.73m² at initiationRenalHigh
- Concurrent use of strong CYP3A4 inhibitorsDrug InteractionHigh
Adverse Effects
- HypertensionCardiovascularCommonHigh blood pressure
- HeadacheNeurologicCommonPain in the head or upper neck
- TremorNeurologicUncommonInvoluntary shaking
- Urinary tract infectionGenitourinaryCommon
- InfectionsImmunologicCommon
- HyperkalemiaElectrolyte ImbalanceCommon
- Nephrotoxicity / decreased eGFRRenalCommon
- NephrotoxicityRenalCommon
- HyperlipidemiaMetabolicUncommon
Drug Interactions
- RifampinModerate
- Strong CYP3A4 inducers (e.g., rifampin, carbamazepine)High
- KetoconazoleHigh
- Potassium-sparing diuretics / ACE inhibitors / ARBsModerate
- Moderate CYP3A4 inhibitors (e.g., fluconazole, diltiazem)Moderate
- Other calcineurin inhibitors (e.g., tacrolimus)High
- Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin)High
- Nephrotoxic agents (e.g., NSAIDs, aminoglycosides)Moderate
Population Constraints
- PregnancyReproductive SafetyRelative
- Pediatric patients (<18 years)AgeRelative
- LactationReproductiveRelative
- Patients with active or chronic serious infectionsInfectionRelative
- Severe hepatic impairmentOrgan ImpairmentRelative
- BreastfeedingReproductiveRelative
Regulatory Status
- European UnionApprovedApproved: Active lupus nephritisEMA approval 2022.
- United StatesApprovedApproved: Active lupus nephritisFDA approval 2021 (Lupkynis).
- United KingdomApprovedApproved: Active lupus nephritisMHRA approval 2022.
First FDA‑approved oral calcineurin inhibitor specifically indicated for lupus nephritis; later approved in the EU and UK.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Voclosporin?
Voclosporin (ISA247) is an oral, modified cyclosporine A analog approved for the treatment of active lupus nephritis. It provides immunosuppression by inhibiting calcineurin, reducing renal inflammation and proteinuria.
What is Voclosporin used for?
Voclosporin is educationally associated with: T-cell immunosuppression, IgA nephropathy (investigational), Lupus nephritis remission, Proteinuria reduction, Podocyte stabilization, Lupus nephritis treatment, Reduce systemic disease activity. Educational only — not medical advice.
How is Voclosporin administered?
Recorded routes of administration: Oral.
What are the potential side effects of Voclosporin?
Reported adverse effects include: Hypertension, Headache, Tremor, Urinary tract infection, Infections, Hyperkalemia, Nephrotoxicity / decreased eGFR, Nephrotoxicity, Hyperlipidemia. This list is not exhaustive — consult a qualified clinician.
Who should avoid Voclosporin?
Recorded contraindications: Live vaccines, Known hypersensitivity to voclosporin or cyclosporine, Active serious infections, Hypersensitivity to voclosporin or cyclosporin analogues, Severe uncontrolled hypertension, Severe renal impairment or eGFR <45 mL/min/1.73m² at initiation, Concurrent use of strong CYP3A4 inhibitors. Consult a qualified clinician before use.