FDA (US): Approved (1983, Sandimmune; 1995, Neoral) for prevention of transplant rejection, and Neoral also for severe psoriasis and rheumatoid arthritis. Approved as eye drops (2002, Restasis; later Cequa and others) for dry eye
EMA (EU): Oral and intravenous forms authorized through national procedures (in Spain, Sandimmun Neoral and generics). Through the centralized route: Ikervis (2015) for severe keratitis in adult dry eye and Verkazia (2018) for severe vernal keratoconjunctivitis in children
Systemic: individual dose per kg of body weight depending on the indication, adjusted by blood levels (FDA/EMA label; e.g., psoriasis and rheumatoid arthritis starting at 2.5 mg/kg/day in two doses). Eye drops: 0.05% one drop twice a day (Restasis, FDA) or 0.1% one drop at bedtime (Ikervis, EMA).
Very many. It is metabolized by CYP3A4 and P-gp: grapefruit, ketoconazole, clarithromycin, or diltiazem raise its levels; rifampin, St. John's wort, or carbamazepine lower them. It raises levels of statins (myopathy risk), digoxin, and others. Greater kidney risk with NSAIDs and aminoglycosides and of high potassium with potassium-sparing diuretics.
Two phase 3 trials with 877 patients over 6 months. Cyclosporine eye drops at 0.05% and 0.1% twice a day improved corneal staining and tear production (Schirmer test) compared with vehicle. Stinging in 15–16% vs 6.5% with vehicle.
View the study (RCT) →It binds to a protein in the cell (cyclophilin) and together they block calcineurin. Without calcineurin, T cells do not activate the interleukin-2 gene and do not multiply. The result is a weaker immune response. In the eye, it reduces surface inflammation and improves tear production.
In people
Information, not medical advice. Prescription or unapproved peptides should only be used under medical supervision.