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Cyclosporine - cyclosporine microemulsion
Cyclosporine - cyclosporine microemulsion is a Calcineurin inhibitor Small molecule drug developed by Novartis. It is currently FDA-approved for Organ transplant rejection prophylaxis (kidney, heart, liver, pancreas), Rheumatoid arthritis, Psoriasis.
Cyclosporine inhibits calcineurin phosphatase, blocking T-cell activation and proliferation by preventing IL-2 transcription.
Cyclosporine inhibits calcineurin phosphatase, blocking T-cell activation and proliferation by preventing IL-2 transcription. Used for Organ transplant rejection prophylaxis (kidney, heart, liver, pancreas), Rheumatoid arthritis, Psoriasis.
At a glance
| Generic name | Cyclosporine - cyclosporine microemulsion |
|---|---|
| Sponsor | Novartis |
| Drug class | Calcineurin inhibitor |
| Target | Calcineurin (protein phosphatase 2B) |
| Modality | Small molecule |
| Therapeutic area | Immunology |
| Phase | FDA-approved |
Mechanism of action
Cyclosporine binds to cyclophilin and forms a complex that inhibits calcineurin, a phosphatase essential for dephosphorylating NFAT (nuclear factor of activated T cells). This prevents NFAT translocation to the nucleus and subsequent IL-2 and other cytokine gene transcription, thereby suppressing T-cell mediated immune responses. The microemulsion formulation improves oral bioavailability and reduces food-dependent variability compared to conventional formulations.
Approved indications
- Organ transplant rejection prophylaxis (kidney, heart, liver, pancreas)
- Rheumatoid arthritis
- Psoriasis
- Atopic dermatitis
- Nephrotic syndrome (minimal change disease)
- Uveitis
- Graft-versus-host disease
Common side effects
- Nephrotoxicity/renal dysfunction
- Hypertension
- Tremor
- Headache
- Gingival hyperplasia
- Hirsutism
- Hyperkalemia
- Infections
- Neurotoxicity/encephalopathy
- Hepatotoxicity
Key clinical trials
- Mycophenolate Mofetil in Patients With Progressive Idiopathic Membranous Nephropathy (PHASE3)
- The Effect of Cyclosporin Before Cataract Surgery (PHASE4)
- Nordic Study in Cardiac and Lung Transplantation: Outcome in Relation to Cyclosporine Microemulsion C2 Levels (PHASE4)
- Everolimus in a Cyclosporine Microemulsion-free Regimen Compared to a Low-dose Cyclosporine Microemulsion Regimen, in de Novo Kidney Transplant Patients (PHASE3)
- Efficacy and Safety of Cyclosporine Microemulsion in Diabetic Adult Stable Liver Transplant Recipients (PHASE4)
- Efficacy and Safety of Everolimus in Combination With Cyclosporine Microemulsion Versus Everolimus in Combination With Enteric-coated Mycophenolate Sodium (EC-MPS), in Adult Renal Transplant Patients in Maintenance. (PHASE3)
- Efficacy and Safety of Enteric-coated Mycophenolate Sodium (EC-MPS) in a Cyclosporine Microemulsion Based Regimen in de Novo Living Donor Kidney Transplant Recipients (PHASE4)
- Study of Enteric-coated Mycophenolate Sodium (EC-MPS) With Cyclosporine Microemulsion and Steroids in Pediatric de Novo Renal Transplant Patients (PHASE4)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Cyclosporine - cyclosporine microemulsion CI brief — competitive landscape report
- Cyclosporine - cyclosporine microemulsion updates RSS · CI watch RSS
- Novartis portfolio CI
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Related
- Drug class: All Calcineurin inhibitor drugs
- Target: All drugs targeting Calcineurin (protein phosphatase 2B)
- Manufacturer: Novartis — full pipeline
- Therapeutic area: All drugs in Immunology
- Indication: Drugs for Organ transplant rejection prophylaxis (kidney, heart, liver, pancreas)
- Indication: Drugs for Rheumatoid arthritis
- Indication: Drugs for Psoriasis
- Compare: Cyclosporine - cyclosporine microemulsion vs similar drugs
- Pricing: Cyclosporine - cyclosporine microemulsion cost, discount & access