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Ciclosporin, also known as cyclosporine or cyclosporin, is a medication primarily used as an immunosuppressant due to its calcineurin inhibitor properties. Administered either orally or intravenously, it is prescribed for various conditions including rheumatoid arthritis, psoriasis, Crohn's disease, nephrotic syndrome, eczema, and for preventing organ transplant rejection. Additionally, it is formulated as eye drops for treating keratoconjunctivitis sicca, or dry eyes. Common side effects of ciclosporin include high blood pressure, headaches, kidney issues, increased hair growth, and vomiting. More serious side effects can include a heightened risk of infection, liver complications, and an increased risk of lymphoma. To mitigate these risks, monitoring blood levels of the medication is recommended. While its use during pregnancy might lead to preterm birth, there is no evidence of it causing birth defects. The mechanism of action for ciclosporin involves decreasing lymphocyte function. It achieves this by forming a complex with cyclophilin, subsequently blocking the phosphatase activity of calcineurin. This action reduces the production of inflammatory cytokines by T-lymphocytes. Originally isolated in 1971 from the fungus Tolypocladium inflatum, ciclosporin was introduced into medical practice in 1983. It is listed on the World Health Organization's List of Essential Medicines and was one of the most prescribed medications in the United States in 2020, with over 2 million prescriptions. Available as a generic medication, its primary indications include treating and preventing graft-versus-host disease in bone marrow transplantation and preventing rejection in kidney, heart, and liver transplants. In the U.S., it is also approved for treating rheumatoid arthritis, psoriasis, persistent nummular keratitis following adenoviral keratoconjunctivitis, and as eye drops for dry eyes caused by Sjögren's syndrome and meibomian gland dysfunction. Beyond these applications, ciclosporin is used in treating severe atopic dermatitis, Kimura disease, pyoderma gangrenosum, chronic hives, acute systemic mastocytosis, and noninfective posterior or intermediate uveitis. It is occasionally used in severe cases of rheumatoid arthritis and related diseases. Moreover, ciclosporin has been employed in treating acute severe ulcerative colitis and steroid-resistant hives.

Chemical and Physical Properties

Source: PubChem