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: |
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| 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: |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L1116 | NCT01750294 | PHASE4 | COMPLETED | YES | 2012-08 | 2016-06-13 | Details |
| L2517 | NCT01358929 | PHASE1 | COMPLETED | NO | 2011-04 | 2016-11-02 | Details |
| L2559 | NCT00879710 | COMPLETED | YES | 2008-08 | 2020-07-29 | Details | |
| L2564 | NCT00476710 | COMPLETED | NO | 2007-05 | 2015-04-01 | Details | |
| L2577 | NCT01217112 | PHASE2 | COMPLETED | YES | 2010-10 | 2022-10-18 | Details |
| L2596 | NCT03485092 | PHASE4 | COMPLETED | NO | 2018-03-16 | 2020-09-18 | Details |
| L2797 | NCT00036504 | PHASE4 | COMPLETED | NO | 2001-08 | 2010-10-13 | Details |
| L3203 | NCT00118963 | PHASE4 | COMPLETED | NO | 2003-01 | 2008-12-08 | Details |
| L3307 | NCT06362265 | PHASE1 | RECRUITING | NO | 2024-10-10 | 2025-03-28 | Details |
| L3430 | NCT00715663 | COMPLETED | NO | 2007-02 | 2016-12-13 | Details | |
| L3479 | NCT04314622 | PHASE2 | COMPLETED | NO | 2020-04-14 | 2021-09-17 | Details |
| L3838 | NCT00325910 | PHASE3 | TERMINATED | NO | 2006-05 | 2008-05-14 | Details |
| L4174 | NCT04218734 | PHASE3 | COMPLETED | NO | 2020-01-14 | 2021-06-28 | Details |
| L4176 | NCT04937816 | COMPLETED | YES | 2021-06-01 | 2024-02-08 | Details | |
| L4224 | NCT03604224 | COMPLETED | NO | 2018-09-05 | 2020-08-19 | Details | |
| L4227 | NCT01650324 | PHASE1 | COMPLETED | YES | 2012-07 | 2014-08-28 | Details |
| L4240 | NCT01569841 | PHASE3 | COMPLETED | YES | 2012-04 | 2016-02-18 | Details |
| L5817 | NCT01752985 | PHASE2 | TERMINATED | YES | 2013-03-18 | 2019-07-30 | Details |
| L6712 | NCT04510493 | PHASE3 | COMPLETED | NO | 2020-10-23 | 2021-09-08 | Details |
| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name |
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| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
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