ArticleClinical pharmacology : advances and applications2020
Pharmacokinetic Disposition Difference Between Cyclosporine and Voclosporin Drives Their Distinct Efficacy and Safety Profiles in Clinical Studies.
Article in Clinical pharmacology : advances and applications, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 23 citations in OpenAlex.
- Comparison of a voclosporin-based triple immunosuppressive therapy to high-dose glucocorticoid-based immunosuppressive therapy: a propensity analysis of the AURA-LV and AURORA 1 studies and ALMS.Lupus science & medicine · 2024Trial
- Voclosporin-induced gingival enlargement: A case report.Clinical advances in periodontics · 2026Article
- Kidney adverse events associated with calcineurin inhibitors: a real-world study based on the FAERS database and network pharmacology.Frontiers in medicine · 2026Article
- Voclosporin shows protective effect and intestinal barrier enforcement in experimental colitis.Frontiers in medicine · 2026Article
- Investigation of Renal Tissue Deposition of the Calcineurin Inhibitors Voclosporin, Cyclosporine and Tacrolimus Using MALDI-MSI Imaging.Pharmaceutical research · 2026Article
- Evaluating the Neuroprotective and Acetylcholinesterase Inhibitory Properties of Four Calcineurin Inhibitor Drugs: Tacrolimus, Pimecrolimus, Cyclosporin A, and Voclosporin.Molecular neurobiology · 2025Article
- Novel Role of Tryptophan Metabolic Pathway in Mediating Peroxisomal Dysfunction in High-Dose Voclosporin-Induced Acute Kidney Injury.Journal of the American Society of Nephrology : JASN · 2025Article
- Calcineurin inhibitor effects on kidney electrolyte handling and blood pressure: tacrolimus versus voclosporin.Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association · 2024Article
- Research trends and frontiers in lupus nephritis: a bibliometric analysis from 2012 to 2022.International urology and nephrology · 2024Article
- Voclosporin and the Antiviral Effect Against SARS-CoV-2 in Immunocompromised Kidney Patients.Kidney international reports · 2023Article
- Clinical Pharmacokinetics and Pharmacodynamics of Voclosporin.Clinical pharmacokinetics · 2023Review
- Protective effect of the novel calcineurin inhibitor voclosporin in experimental colitis.Frontiers in medicine · 2023Article
- Belimumab for systemic lupus erythematosus - Focus on lupus nephritis.Human vaccines & immunotherapeutics · 2022Review
- Calcineurin inhibitors in systemic sclerosis - a systematic literature review.Therapeutic advances in musculoskeletal disease · 2022Review
- Severe lupus nephritis in the present days.Frontiers in nephrology · 2022Review
- The Cyclophilin-Dependent Calcineurin Inhibitor Voclosporin Inhibits SARS-CoV-2 Replication in Cell Culture.Transplant international : official journal of the European Society for Organ Transplantation · 2022Article
- Old and New Calcineurin Inhibitors in Lupus Nephritis.Journal of clinical medicine · 2021Review
- AURORA 1 reports efficacy of voclosporin in lupus nephritis.Nature reviews. Nephrology · 2021Article
- Voclosporin: First Approval.Drugs · 2021Review
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundVoclosporin, a more potent derivative of cyclosporine, has been studied extensively in patients with immunologic disorders such as psoriasis, organ transplantation, uvetitis and lupus nephritis. Although better tolerated and safer than cyclosporine, voclosporin is inferior to cyclosporine in treating psoriasis, non-inferior to tacrolimus in organ transplantation and efficacious in treating lupus nephritis.
methodsThe pharmacokinetic dispositions of voclosporin and cyclosporine in central and peripheral compartments were analyzed and correlated with their distinct clinical efficacy and safety profiles.
resultsBoth drugs demonstrated non-linear pharmacokinetics with increasing doses, more prominently at lower doses of voclosporin than at 10-fold higher doses of cyclosporine. Repeated lower dosing of voclosporin produced preferential calcineurin inhibition in and near blood circulation, leading to relatively lower cardiovascular and renal adverse effects but inferior efficacy for psoriasis compared to cyclosporine. With 10-fold higher plasma levels and deeper tissue penetration, cyclosporine has more prevalent renal and cardiac toxicities but superior efficacy to treat psoriasis.
conclusionAlthough the two drugs are similar in structure and mechanism of action, the high potency and low dose compounded by the non-linear disposition of voclosporin resulted in more systemic versus local calcineurin inhibition than with cyclosporine. The dispositional difference between voclosporin and cyclosporine accounted for the puzzling efficacy and safety observations in different patients and was the basis for their optimal and differential use in treating diverse immunologic disorders.
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