Ciclosporine

CAS 59865-13-3

About the API

Systematic name (3S,6S,9S,12R,15S,18S,21S,24S,30S,33S)-30-Ethyl-33-[(1R,2R,4E)-1-hydroxy-2-methyl-4-hexen-1-yl]-6,9,18,24-tetraisobutyl-3,21-diisopropyl-1,4,7,10,12,15,19,25,28-nonamethyl-1,4,7,10,13,16,19,22,25,28,3 1-undecaazacyclotritriacontane-2,5,8,11,14,17,20,23,26,29,32-undecone
Trade name(s) Gengraf, Neoral, Sandimmune
Molecular Formula C62H111N11O12
Molecular Weight 1202.61 g/mol
Physical properties white to off-white crystalline powder
Therapeutic category Immunology
Available formulations Injectables Opthalmic Oral Liquid Oral Solid
Regulations Canada DMF Flag Canada DMF CEP Flag CEP EU DMF Flag EU DMF Japan DMF Flag Japan DMF Korea DMF Flag Korea DMF Other Flag Other US DMF Flag US DMF

General Information

Ciclosporine is an immunosuppressant isolated from the fungus Tolypocladium inflatum. It is prescribed to prevent rejection of newly transplanted organs and tissues. Specifically, ciclosporin is a calcineurin inhibitor that targets the activity of T-cells, a type of white blood cell involved in fighting foreign substances the body is exposed to. It is also used in the treatment of rheumatoid arthritis when methotraxate treatment alone is not effective, Crohn’s disease, and other autoimmune disorders.

 

The immunosuppressive activity of ciclosporin was first discovered in 1976 and approved by the FDA for clinical use in 1983. Ciclosporin is manufactured by large-scale aerobic fermentation of various fungi and then extracted and purified from cultures using chromatographic techniques.