Cyclosporin A

Synonyms

(R-(R*,R*-(E)))-Cyclic(L-alanyl-D-alanyl-N-methyl-L-leucyl-N-methyl-L-leucyl-N-methyl-L-valyl-3-hydroxy-N,4-dimethyl-L-2-amino-6-octenoyl-L-alpha-aminobutyryl-N-methylglycyl-N-methyl-L-leucyl-L-valyl-N-methyl-L-leucyl); Antibiotic S 7481F1; Ciclosporin; Ciclosporina [INN-Spanish]; Ciclosporine [INN-French]; Ciclosporine [INN]; Ciclosporinum [INN-Latin]; Cipol N; Consupren; Cyclo(((E)-(2S,3R,4R)-3-hydroxy-4-methyl-2-(methylamino)-6-octenoyl)-L-2-aminobutyryl-N-methylglycyl-N-methyl-L-leucyl-L-valyl-N-methyl-L-leucyl-L-alanyl-D-alanyl-N-methyl-L-leucyl-N-methyl-L-leucyl-N-methyl-L-valyl); Cyclo(L-alanyl-D-alanyl-N-methyl-L-leucyl-N-methyl-L-leucyl-N-methyl-L-valyl-((3R,4R,6E)-6,7-didehydro-3-hydroxy-N,4-dimethyl-L-2-aminooctanoyl-L-2-aminobutanoyl-N-methylglycyl-N-methyl-L-leucyl-L-valyl-N-methylleucyl); Cyclosporin; Cyclosporine; Cyclosporine A; DRG-0275; Gengraf; Neoplanta; Neoral; OL 27-400; Ramihyphin A; Restasis; S 7481F1; S-Neoral; Sandimmun; Sandimmun Neoral; Sandimmune; Sang 35; Sangcya; [ChemIDplus]

Category

Mycotoxins

Description

White solid; [Merck Index] White powder; [MSDSonline]

Sources/Uses

Produced by Tolypocladium inflatum and other fungi imperfecti; An immunosuppressant; Veterinary applications include control of immune-mediated dermatological diseases; [Merck Index] Used in organ transplantation; [HSDB] Used as an immunosuppressive drug since the 1980s; [IARC]

Comments

A nephrotoxin and hepatotoxin; [CAMEO] Directly toxic to the kidney; [Olson, p. 41] Causes chronic tubulointerstitial nephritis; [Ford, p. 194] In studies of rats, can cause male sterility and fetotoxicity at high doses; Enhances the development of lymphomas in animals and humans; [IARC] When used as a drug, nephrotoxicity occurs in all patients and is the limiting factor in its use. Nephrotoxicity is associated with trough plasma levels >250 ng/mL and hepatotoxicity with trough levels >1000 ng/mL; [HSDB]

Biomedical References

Hepatoxic (a) from occupational exposure (secondary effect) or (b) in animal studies or in humans after ingestion

Yes

Established

Human carcinogen

Other Information

No other related information on this agent was found.