| Drug ID: | Drug92 |
|---|---|
| Drug Name: | Cyclosporine |
| CID: | 5284373 |
| DrugBank ID: | DB00091 |
| Modality: | Small Molecule |
| Groups: | approved|investigational |
| US Approved: | YES |
| Other Approved: | YES |
| Identifier: | NCT05112263, , NCT05219656, , NCT00542152 |
| Molecular Formula: | C62H111N11O12 |
| Molecular Weight: | 1202.6 g/mol |
| Isomeric SMILES: | CC[C@H]1C(=O)N(CC(=O)N([C@H](C(=O)N[C@H](C(=O)N([C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N([C@H](C(=O)N([C@H](C(=O)N([C@H](C(=O)N([C@H](C(=O)N1)[C@@H]([C@H](C)C/C=C/C)O)C)C(C)C)C)CC(C)C)C)CC(C)C)C)C)C)CC(C)C)C)C(C)C)CC(C)C)C)C |
| Synonyms: | cyclosporin A; Ciclosporin; cyclosporine; Cyclosporin; 59865-13-3; Sandimmune; Neoral; Cyclosporine A; Sandimmun; Ciclosporine |
| Phase 0: | 7 |
| Phase 1: | 163 |
| Phase 2: | 373 |
| Phase 3: | 184 |
| Phase 4: | 175 |
| Description: | A cyclic undecapeptide from an extract of soil fungi. It is a powerful immunosupressant with a specific action on T-lymphocytes. It is used for the prophylaxis of graft rejection in organ and tissue transplantation. Cyclosporine is produced as a metabolite by the fungus species Cordyceps militaris. (From Martindale, The Extra Pharmacopoeia, 30th ed). |
Molecular Structure
Knowledge Graph
| dtID | CID | Compound Name | Gene ID | Gene Name | Species | PubMed IDs | Action |
|---|---|---|---|---|---|---|---|
| dt775 | 5284373 | cyclosporin A | 8435 | SOAT2 | Homo sapiens (human) | 25562108 | Cyclosporine results in decreased expression of SOAT2 mRNA |
| dt776 | 5284373 | cyclosporin A | 55084 | SOBP | Homo sapiens (human) | Cyclosporine results in decreased expression of SOBP mRNA | |
| dt777 | 5284373 | cyclosporin A | 8651 | SOCS1 | Homo sapiens (human) | 25562108 | Cyclosporine results in decreased expression of SOCS1 mRNA |
| dt778 | 5284373 | cyclosporin A | 8651 | SOCS1 | Homo sapiens (human) | 27989131 | Cyclosporine results in decreased methylation of SOCS1 promoter |
| dt779 | 5284373 | cyclosporin A | 445073 | socs1a | Danio rerio (zebrafish) | 25064622 | Cyclosporine affects the expression of SOCS1A mRNA |
| dt780 | 5284373 | cyclosporin A | 8835 | SOCS2 | Danio rerio (zebrafish) | 25064622 | Cyclosporine affects the expression of SOCS2 mRNA |
| dt781 | 5284373 | cyclosporin A | 8835 | SOCS2 | Homo sapiens (human) | 27989131 | Cyclosporine results in decreased expression of SOCS2 mRNA |
| dt782 | 5284373 | cyclosporin A | 8835 | SOCS2 | Homo sapiens (human) | Cyclosporine results in increased expression of SOCS2 mRNA | |
| dt783 | 5284373 | cyclosporin A | 122809 | SOCS4 | Homo sapiens (human) | 25562108 | Cyclosporine results in increased expression of SOCS4 mRNA |
| dt784 | 5284373 | cyclosporin A | 9306 | SOCS6 | Homo sapiens (human) | Cyclosporine results in increased expression of SOCS6 mRNA |
- No data available
Phase Distribution
Phase Description
- Phase 0: Exploratory trials to assess drug behavior in humans
- Phase 1: Safety trials to determine safe dosage range
- Phase 2: Efficacy trials to evaluate therapeutic effects
- Phase 3: Large-scale trials to confirm efficacy and safety
- Phase 4: Post-marketing surveillance for long-term safety and efficacy
| Trial ID | Title | Phase | Status | Sponsor | Indications | Interventions | |
|---|---|---|---|---|---|---|---|
| NCT05112263 | Tofacitinib Versus Cyclosporine for Steroid Refractory Acute Severe Ulcerative Colitis | None | NOT_YET_RECRUITING | Post Graduate Institute of Medical Education and Research, Chandigarh | Ulcerative Colitis | DRUG: Tofacitinib|DRUG: Cyclosporine | Details |
| NCT00542152 | Study Comparing Cyclosporine With Infliximab in Steroid-refractory Severe Attacks of Ulcerative Colitis | PHASE4 | COMPLETED | Groupe d'Etude Therapeutique des Affections Inflammatoires Digestives | Ulcerative Colitis|Steroid Refractory | DRUG: CYCLOSPORINE VS INFLIXIMAB | Details |
| CTRI/2021/10/037641 | An open label study to compare the efficacy and safety of tofacitinib compared to corticosteroids for inducing remission in moderately severe active ulcerative colitis | PHASE4 | Recruiting | Dayanand Medical College and Hospital Ludhiana | Disease.2. Total mayo clinic score <6 or >9. 3.… | Health Condition 1: K51- Ulcerative colitis | Details |
| NCT05867329 | A Trial for Acute Severe Ulcerative Colitis | PHASE4 | RECRUITING | Berinstein, Jeffrey | Ulcerative Colitis Acute | DRUG: Cyclosporine Injection (IV)|DRUG: Cyclospor… | Details |
| NCT05219656 | Efficacy of Cyclosporine Rescue Therapy in Acute Ulcerative Colitis. | None | COMPLETED | Tampere University Hospital | Ulcerative Colitis Acute | DRUG: Cyclosporine A | Details |
| Disease ID | Disease Name | Definition | Category | Related Drugs | Mechanism | |
|---|---|---|---|---|---|---|
| 1.0 | Crohn's disease | An intestinal disease that involves inflammation located_in intestine. | disease of anatomical entity gastrointestinal system disease, intestinal disease, inflammatory bowel disease | Obiltoxaximab; Budesonide; Hydrocortisone acetate; Sulfasalazine; Ursodeoxycholic acid; Pegunigalsidase alfa; Imiglucerase; Bictegravir; Taliglucerase alfa; Etelcalcetide; Cimetidine; Desonide | Crohn's disease is a relapsing systemic inflammatory diseas… | Details |
| 2.0 | ulcerative colitis | A colitis that is predominantly confined to the mucosa located_in colon and includes characteristic ulcers, or open sores. | disease of anatomical entity, gastrointestinal system disease, autoimmune disease of gastrointestinal tract; intestinal disease, inflammatory bowel disease, colitis; disease, primary immunodeficiency disease, autoimmune disease, autoimmune disease of gastrointestinal tract | Mirikizumab; Olsalazine; Balsalazide; Sulfasalazine; Budesonide; Hydrocortisone acetate; Tixocortol; Kappadione; Teicoplanin; Atezolizumab; Gamolenic acid; Upadacitinib | No abstract available | Details |
| Strategy ID | Therapeutic Strategy | Synonyms | Related Drugs | Mechanism | |
|---|---|---|---|---|---|
| S01 | Anti-inflammatory | inflammatory | 5-Aminosalicylates (5-ASAs); corticosteroids | Crohn's disease and ulcerative colitis are the two main com… | Details |
| S02 | Immunosuppression | Classic immunosuppressive drugs | azathioprine; 6-mercaptopurine; methotrexate; ciclosporin-A; tacrolimus | Ciclosporin-A and tacrolimus bind to specific intracellular… | Details |
| S03 | Anti-TNF agents | Tumor necrosis factor | infliximab; adalimumab; golimumab; certolizumab pegol | TNF is produced by various immune and non-immune cells in t… | Details |
| S04 | T-cell homing and retention | T-cell trafficking | vedolizumab; anti-MAdCAM1 antibodies ; etrolizumab | Inhibition of the interaction between α4β7 integrins on T c… | Details |
| S05 | Angiogenesis | cell proliferation; vascular permeability | ozanimod | The bioactive lipid S1P has been shown to activate NF-κB an… | Details |
| S07 | Blockade of cytokine | Cytokine signalling | apremilast; roflumilast; filgotinib; tofacitinib; ABT494; ABT-874; ustekinumab; isankizumab; LY-2525623; AMG139; MEDI2079; guselkumab | Various T-cell subsets, their differentiation pathways and … | Details |
| S08 | Strengthening barrier function | Modulation of barrier function | phosphatidylcholine (lecithin); imiquimod; mongersen | Escherichia coli Nissle (EcN) is a nonpathogenic Gram-negat… | Details |
| S11 | Improveming Intestinal Microecology | the intestinal microbiota | antibiotics; probiotics; prebiotics; postbiotics; synbiotics; fecal microbiota transplantation (FMT) | The imbalance between beneficial bacteria and harmful patho… | Details |
Extended abstract: Tacrolimus and cyclosporine in inflammatory bowel disease
PMID: 23295702
Year: 2012
Relationship Type:
Association
Score: 6.1
[Effect of immunosuppressants on inflammatory bowel disease: tacrolimus and cyc…
PMID: 23126111
Year: 2012
Relationship Type:
Association
Score: 6.1
Cyclosporine: does it matter if it is given for Crohn's colitis or ulcerative c…
PMID: 22955259
Year: 2012
Relationship Type:
Association
Score: 6.1
Cyclosporine in the management of severe ulcerative colitis while breast-feeding
PMID: 21538721
Year: 2011
Relationship Type:
Association
Score: 6.1
Adverse events associated with the use of cyclosporine in patients with inflamm…
PMID: 18177449
Year: 2008
Relationship Type:
Mechanism
Score: 6.1
Data indicate that appendicectomy for intra-abdominal inflammation protects against inflammatory bowel disease (IBD). This suggests an important rol…
Pharmacokinetics and clinical efficacy of cyclosporine treatment of dogs with s…
PMID: 16594578
Year: 2006
Relationship Type:
Treatment
Score: 6.1
Evidence from four independent linkage studies and two meta-analyses of genome-wide data support the existence of a locus conferring susceptibility …
Cyclosporine for severe ulcerative colitis
PMID: 16368919
Year: 2006
Relationship Type:
Treatment
Score: 6.1
BACKGROUND: There are limited data on factors predicting response to azathioprine and uncertainty regarding the optimal duration of treatment. PATIE…
Cyclosporine, or cyclosporine not, for severe ulcerative colitis
PMID: 11720331
Year: 2001
Relationship Type:
Mechanism
Score: 6.1
Sustained damage to the mucosal lining in patients with inflammatory bowel disease (IBD) facilitates translocation of intestinal microbes to submuco…
Cyclosporine therapy in inflammatory bowel disease: short-term and long-term re…
PMID: 10478875
Year: 1999
Relationship Type:
Treatment
Score: 6.1
OBJECTIVES: Immunologic studies have characterized the numbers and types of inflammatory cells in diseased inflammatory bowel disease (IBD) mucosa b…
More evidence of the failure of oral cyclosporine to maintain remission due to …
PMID: 10478868
Year: 1999
Relationship Type:
Association
Score: 6.1
Not found
Success of Cyclosporin and Tofacitinib Combination Therapy in a Patient With Se…
PMID: 34398196
Year: 2021
Relationship Type:
Treatment
Score: 5.5
At present, the conventional therapies for acute severe ulcerative colitis (ASUC) mainly include corticosteroids, cyclosporin, and biological agents.…