Drug intelligence / Profile preview

ciclosporin

Development stage
Approved
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral, Intravenous, Ophthalmic
01

Overview

Ciclosporin is a calcineurin inhibitor immunosuppressant originally isolated from the fungus Tolypocladium inflatum. It acts by forming a complex with cyclophilin, which inhibits the phosphatase activity of calcineurin, leading to decreased production of inflammatory cytokines by T lymphocytes and suppression of immune responses. Ciclosporin is primarily used to prevent organ transplant rejection (kidney, liver, heart), and to treat autoimmune and inflammatory conditions such as rheumatoid arthritis, psoriasis, Crohn’s disease, nephrotic syndrome, eczema, ulcerative colitis, atopic dermatitis and keratoconjunctivitis sicca (dry eye) in ophthalmic formulations. It was first approved in 1983 and is available as oral capsules/solutions or intravenous infusions for systemic use; topical ophthalmic preparations are also widely used[1][2][3][4][5].

Brand names
NeoralSandimmuneGengrafCequaIkervisRestasisVerkaziaVevyeCapimuneCapsorinDeximune
Other names
cyclosporinecyclosporinciclosporinaciclosporinum
02

Targets

PPIA (Peptidyl-prolyl cis-trans isomerase A)PPIF (Cyclophilin D)CN (Calcineurin)ABCB1 (P-glycoprotein)

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