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Product Details:

  • Product Name: Cyclosporin
  • CAS #: 59865-13-3
  • Mode of Action:

    Cyclosporin binds to cyclophilin. The complex then inhibits calcineurin which is normally responsible for activating transcription of interleukin 2. Cyclosporin also inhibits lymphokine production and interleukin release. In ophthalmic applications, the precise mechanism of action is not known. Cyclosporin emulsion is thought to act as a partial immunomodulator in patients whose tear production is presumed to be suppressed due to ocular inflammation associated with keratoconjunctivitis sicca.

  • Pharmacodynamics:

    Used in immunosuppression for prophylactic treatment of organ transplants, cyclosporin exerts specific and reversible inhibition of immunocompetent lymphocytes in the G0-or G1-phase of the cell cycle. T-lymphocytes are preferentially inhibited. The T1-helper cell is the main target, although the T1-suppressor cell may also be suppressed. Sandimmune (cyclosporin) also inhibits lymphokine production and release including interleukin-2.

  • Metabolism:

    Hepatic, extensively metabolized.

  • Toxicity:

    The oral LD50 is 2329 mg/kg in mice, 1480 mg/kg in rats, and > 1000 mg/kg in rabbits. The I.V. LD50 is 148 mg/kg in mice, 104 mg/kg in rats, and 46 mg/kg in rabbits.

  • IUPAC: (3S,6S,9S,12R,15S,18S,21S,24S,30S,33S)-30-ethyl-33-[(1R,2R,4E)-1-hydroxy-2-methylhex-4-en-1-yl]-1,4,7,10,12,15,19,25,28-nonamethyl-6,9,18,24-tetrakis(2-methylpropyl)-3,21-bis(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2,5,8,11,14,17,20,23,26,29,32-undecone
  • ATC: L04AD01, S01XA18
  • PubChem: 5284373
  • DrugBank: DB00091 (BIOD00003, BTD00003)
  • Formula: C22H26ClN7O2S
  • Molecular Mass: 1202.6112
  • Synonyms: Restasis, Sandimmune, Ciclosporin, Cyclosporine, Cyclosporin A
  • SMILES: CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C\C=C\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O)C(C)C
  • AHFS Code: 32:00.0
  • InChl: InChI=1S/C62H111N11O12/c1-25-27-28-40(15)52(75)51-56(79)65-43(26-2)58(81)67(18)33-48(74)68(19)44(29-34(3)4)55(78)66-49(38(11)12)61(84)69(20)45(30-35(5)6)54(77)63-41(16)53(76)64-42(17)57(80)70(21)46(31-36(7)8)59(82)71(22)47(32-37(9)10)60(83)72(23)50(39(13)14)62(85)73(51)24/h25,27,34-47,49-52,75H,26,28-33H2,1-24H3,(H,63,77)(H,64,76)(H,65,79)(H,66,78)/b27-25+/t40-,41+,42-,43+,44+,45+,46+,47+,49+,50+,51+,52-/m1/s1
  • Date Modified: 03-12-19
  • General Reference:

    1. Lichtiger S, Present DH, Kornbluth A, Gelernt I, Bauer J, Galler G, Michelassi F, Hanauer S: Cyclosporine in severe ulcerative colitis refractory to steroid therapy. N Engl J Med. 1994 Jun 30;330(26):1841-5. [PubMed:8196726]
    2. Husi H, Schorgendorfer K, Stempfer G, Taylor P, Walkinshaw MD: Prediction of substrate-specific pockets in cyclosporin synthetase. FEBS Lett. 1997 Sep 15;414(3):532-6. [PubMed:9323029]
    3. Forsythe P, Paterson S: Ciclosporin 10 years on: indications and efficacy. Vet Rec. 2014 Mar;174 Suppl 2:13-21. doi: 10.1136/vr.102484. [PubMed:24682697]
    4. Bunikowski R, Gerhold K, Brautigam M, Hamelmann E, Renz H, Wahn U: Effect of low-dose cyclosporin a microemulsion on disease severity, interleukin-6, interleukin-8 and tumor necrosis factor alpha production in severe pediatric atopic dermatitis. Int Arch Allergy Immunol. 2001 Aug;125(4):344-8. doi: 10.1159/000053836. [PubMed:11574757]
    5. Brazis P, Barandica L, Garcia F, Clough GF, Church MK, Puigdemont A: Dermal microdialysis in the dog: in vivo assessment of the effect of cyclosporin A on cutaneous histamine and prostaglandin D2 release. Vet Dermatol. 2006 Jun;17(3):169-74. doi: 10.1111/j.1365-3164.2006.00511.x. [PubMed:16674731]
    6. BuBmann C, Bieber T, Novak N: Systemic therapeutic options for severe atopic dermatitis. J Dtsch Dermatol Ges. 2009 Mar;7(3):205-19. doi: 10.1111/j.1610-0387.2008.06834.x. Epub 2008 Aug 26. [PubMed:18759739]
    7. Guaguere E, Steffan J, Olivry T: Cyclosporin A: a new drug in the field of canine dermatology. Vet Dermatol. 2004 Apr;15(2):61-74. doi: 10.1111/j.1365-3164.2004.00376.x. [PubMed:15030555]
    8. Cockerill GW, Bert AG, Ryan GR, Gamble JR, Vadas MA, Cockerill PN: Regulation of granulocyte-macrophage colony-stimulating factor and E-selectin expression in endothelial cells by cyclosporin A and the T-cell transcription factor NFAT. Blood. 1995 Oct 1;86(7):2689-98. [PubMed:7545467]
    9. Cirillo R, Triggiani M, Siri L, Ciccarelli A, Pettit GR, Condorelli M, Marone G: Cyclosporin A rapidly inhibits mediator release from human basophils presumably by interacting with cyclophilin. J Immunol. 1990 May 15;144(10):3891-7. [PubMed:1692065]
    10. Lallemand F, Schmitt M, Bourges JL, Gurny R, Benita S, Garrigue JS: Cyclosporine A delivery to the eye: A comprehensive review of academic and industrial efforts. Eur J Pharm Biopharm. 2017 Aug;117:14-28. doi: 10.1016/j.ejpb.2017.03.006. Epub 2017 Mar 14. [PubMed:28315447]
    11. Dehesa L, Abuchar A, Nuno-Gonzalez A, Vitiello M, Kerdel FA: The use of cyclosporine in dermatology. J Drugs Dermatol. 2012 Aug;11(8):979-87. [PubMed:22859244]
    12. Faulds D, Goa KL, Benfield P: Cyclosporin. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in immunoregulatory disorders. Drugs. 1993 Jun;45(6):953-1040. doi: 10.2165/00003495-199345060-00007. [PubMed:7691501]

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