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Investigational Drug Details

Drug ID: D253
Drug Name: Sirolimus
Synonyms:
Type: small molecule
DrugBank ID: DB00877
DrugBank Description: 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 ID: 5284616
CasNo: 53123-88-9
Repositioning for NAFLD: Yes
SMILES: [H][C@@]1(C[C@@H](C)[C@]2([H])CC(=O)[C@H](C)\C=C(C)\[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)\C=C\C=C\C=C(C)\[C@H](C[C@]3([H])CC[C@@H](C)[C@@](O)(O3)C(=O)C(=O)N3CCCC[C@@]3([H])C(=O)O2)OC)CC[C@@H](O)[C@@H](C1)OC
Structure:
InChiKey: QFJCIRLUMZQUOT-HPLJOQBZSA-N
Molecular Weight: 914.187
DrugBank Targets: Serine/threonine-protein kinase mTOR
DrugBank MoA: 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.
DrugBank Pharmacology: Sirolimus, a macrocyclic lactone produced by <i>Streptomyces hygroscopicus</i>, is an immunosuppressive agent indicated for the prophylaxis of organ rejection in patients receiving renal transplants. It is recommended that sirolimus be used in a regimen with cyclosporine and corticosteroids.
DrugBank Indication: For the prophylaxis of organ rejection in patients receiving renal transplants.
Targets:
Therapeutic Category:
Clinical Trial Progress:
Latest Progress: