Ciklosporin

Ciklosporin
(IUPAC) ime
	(E)-14,17,26,32-tetrabutyl-5-ethyl-8-(1-hydroxy-2-methylhex-4-enyl) -1,3,9,12,15,18,20,23,27-nonamethyl-11,29-dipropyl-1,3,6,9,12,15,18,21,24,27,30- undecaazacyclodotriacontan-2,4,7,10,13,16,19,22,25,28,31-undecaone
Klinički podaci
Identifikatori
CAS broj	59865-13-3
ATC kod	L04AD01 S01XA18
PubChem	2909
DrugBank	DB00091
ChemSpider	4447449
Hemijski podaci
Formula	C62H111N11O12
Mol. masa	1202.61
InChI
	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; Key: PMATZTZNYRCHOR-CGLBZJNRSA-N
Farmakokinetički podaci
Bioraspoloživost	promenljiva
Metabolizam	hepatički
Poluvreme eliminacije	promenljivo (oko 24 sata)
Izlučivanje	bilijarno
Farmakoinformacioni podaci
Trudnoća	C(AU) C(US)
Pravni status	Samo na recept (S4) (AU) POM (UK) ℞-only (SAD)
Način primene	oralno, IV, oftalmički

Ciklosporin (INN, cyklosporine (USAN), cyclosporin (bivši BAN) ili cyclosporin A, je imunosupresantni lek koji se široko koristi nakon alotransplantacije organa da be umanjila aktivnost pacijentovog imunskog sistema, i time rizik neprihvatanja organa. On je bio studiran kod transplanta kože, srca, bubrega, jetre, pluća, pankreasa, koštane srži, i tankih creva. Inicijalno je izolovan iz jednog Norveškog uzorka humusa. Ciklosporin je ciklični ne-ribozomski peptid sa 11 aminokiselina koji proizvodi gljiva Beauveria nivea, i sadrži jednu D-aminokiselinu, što se retko sreće u prirodi.^[4]

↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit
↑ Borel JF (2002). „History of the discovery of cyclosporin and of its early pharmacological development”. Wien. Klin. Wochenschr. 114 (12): 433–7. PMID 12422576.
Neki izvori navode ovu gljivu pod alternativnim imenom vrste Hypocladium inflatum gams, npr. Pritchard i Sneader 2005:
* Pritchard DI (2005). „Sourcing a chemical succession for cyclosporin from parasites and human pathogens”. Drug Discov. Today 10 (10): 688–91. DOI:10.1016/S1359-6446(05)03395-7. PMID 15896681.
* „Ciclosporin”. Drug Discovery - A History. John Wiley & Sons. str. 298–299 (refs. page 315).
However, the name, "Beauveria nivea", also appears in several other articles including in a 2001 online publication by Harriet Upton entitled "Origin of drugs in current use: the cyclosporin story Arhivirano 2005-03-08 na Wayback Machine-u" (retrieved June 19, 2005). Mark Plotkin states in his book Medicine Quest, Penguin Books 2001, pages 46-47, that in 1996 mycology researcher Kathie Hodge found that it is in fact a species of Cordyceps.

[1] Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit

[2] Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.

[3] Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit

[pmid12422576-4] Borel JF (2002). „History of the discovery of cyclosporin and of its early pharmacological development”. Wien. Klin. Wochenschr. 114 (12): 433–7. PMID 12422576.
Neki izvori navode ovu gljivu pod alternativnim imenom vrste Hypocladium inflatum gams, npr. Pritchard i Sneader 2005:
* Pritchard DI (2005). „Sourcing a chemical succession for cyclosporin from parasites and human pathogens”. Drug Discov. Today 10 (10): 688–91. DOI:10.1016/S1359-6446(05)03395-7. PMID 15896681.
* „Ciclosporin”. Drug Discovery - A History. John Wiley & Sons. str. 298–299 (refs. page 315).
However, the name, "Beauveria nivea", also appears in several other articles including in a 2001 online publication by Harriet Upton entitled "Origin of drugs in current use: the cyclosporin story Arhivirano 2005-03-08 na Wayback Machine-u" (retrieved June 19, 2005). Mark Plotkin states in his book Medicine Quest, Penguin Books 2001, pages 46-47, that in 1996 mycology researcher Kathie Hodge found that it is in fact a species of Cordyceps.

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Ciklosporin

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