Cyclosporine
Also known as: Ciclosporin, Sandimmune, Neoral, Gengraf, Restasis, Cequa
A cyclic peptide calcineurin inhibitor used to prevent transplant rejection and treat autoimmune and dry-eye disease. FDA-approved. Prescription only.
Last updated
Mechanism of Action
Cyclosporine is a cyclic peptide of 11 amino acids from the fungus Tolypocladium inflatum. Inside T cells it binds cyclophilin, and the complex inhibits calcineurin, a phosphatase needed to activate the transcription factor NFAT. This blocks interleukin-2 production and T-cell activation, suppressing the immune responses that drive organ rejection and some autoimmune diseases. Eye drop formulations act locally to reduce inflammation of the tear glands and ocular surface.
- Half-life
- ~8 hours on average, highly variable between patients
- Administration Routes
- Oral, Intravenous, Ophthalmic
- Research Status
- Clinical
Reported Benefits
- Prevents rejection of kidney, liver and heart transplants
- Treats severe rheumatoid arthritis and severe plaque psoriasis (Neoral/Gengraf)
- Ophthalmic forms increase tear production in chronic dry eye disease
Potential Side Effects
- Boxed warning: serious infections and malignancy, including lymphoma and skin cancer
- Boxed warning: kidney toxicity and high blood pressure
- Tremor, headache, excess hair growth and gum overgrowth
- Many drug interactions (CYP3A4 and P-glycoprotein)
- Eye burning (ophthalmic forms)
Common Dosing
Systemic cyclosporine is prescribed by transplant or specialist teams, dosed by weight and adjusted using blood levels, kidney function and blood pressure. Sandimmune and Neoral/Gengraf are not bioequivalent and should not be switched without monitoring. Eye drops follow a fixed labeled schedule. The prescribing clinician sets and supervises dosing.
The dosing information above is aggregated from research literature and anecdotal community reports for educational purposes only. It is not a recommendation, prescription, or medical advice. Peptides are sold as research chemicals only and are not intended for human use.
Contraindications
- Hypersensitivity to cyclosporine or formulation ingredients
- For psoriasis or rheumatoid arthritis: abnormal kidney function, uncontrolled hypertension or malignancy
- Avoid combining with PUVA, UVB therapy or other immunosuppressants for psoriasis
No documented stacking partners for Cyclosporine yet.