. . . . "A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to immunophilins. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties. [PubChem]"@en . . . "For the prophylaxis of organ rejection in patients receiving renal transplants."@en . "Sirolimus inhibits T lymphocyte activation and proliferation that occurs in response to antigenic and cytokine (Interleukin IL-2, IL-4, and IL-15) stimulation by a mechanism that is distinct from that of other immunosuppressants. Sirolimus also inhibits antibody production. In cells, sirolimus binds to the immunophilin, FK Binding Protein-12 (FKBP-12), to generate an immunosuppressive complex. The sirolimus:FKBP-12 complex has no effect on calcineurin activity. This complex binds to and inhibits the activation of the mammalian Target Of Rapamycin (mTOR), a key regulatory kinase. This inhibition suppresses cytokine-driven T-cell proliferation, inhibiting the progression from the G1 to the S phase of the cell cycle."@en . . "92%"@en . . "53123-88-9"@en . . . . . . "Madhup K. Dhaon, Chi-nung Hsiao, Subhash R. Patel, Peter J. Bonk, Sanjay R. Chemburkar, Yong Y. Chen, \"One pot synthesis of tetrazole derivatives of sirolimus.\" U.S. Patent US20080167335, issued July 10, 2008."@en . . . . . "# Pritchard DI: Sourcing a chemical succession for cyclosporin from parasites and human pathogens. Drug Discov Today. 2005 May 15;10(10):688-91. \"Pubmed\":http://www.ncbi.nlm.nih.gov/pubmed/15896681 # Shuchman M: Trading restenosis for thrombosis? New questions about drug-eluting stents. N Engl J Med. 2006 Nov 9;355(19):1949-52. \"Pubmed\":http://www.ncbi.nlm.nih.gov/pubmed/17093244 # Sun SY, Rosenberg LM, Wang X, Zhou Z, Yue P, Fu H, Khuri FR: Activation of Akt and eIF4E survival pathways by rapamycin-mediated mammalian target of rapamycin inhibition. Cancer Res. 2005 Aug 15;65(16):7052-8. \"Pubmed\":http://www.ncbi.nlm.nih.gov/pubmed/16103051 # Chan S: Targeting the mammalian target of rapamycin (mTOR): a new approach to treating cancer. Br J Cancer. 2004 Oct 18;91(8):1420-4. \"Pubmed\":http://www.ncbi.nlm.nih.gov/pubmed/15365568 # Graziani EI: Recent advances in the chemistry, biosynthesis and pharmacology of rapamycin analogs. Nat Prod Rep. 2009 May;26(5):602-9. Epub 2009 Mar 5. \"Pubmed\":http://www.ncbi.nlm.nih.gov/pubmed/19387497"@en . . . . . . . "Sirolimus"@en . . . . . . "Humans and other mammals"@en . . "approved"@en . . . . . . . . . . . . . . . . . . . . . . . . . "Rapamycin"@en . . . . . "investigational"@en . "57-63 hours"@en . "(-)-Rapamycin"@en . . . . . . " "@en . . . . .