| 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 |
An Old Bridge to the Newer Biologics: Cyclosporine for Rescue Therapy in Acute …
PMID: 36125593
Year: 2022
Relationship Type:
Treatment
Score: 6.5
Response to the Letter to the Editor: "Pyoderma Gangrenosum in An Ulcerative Co…
PMID: 34003266
Year: 2021
Relationship Type:
Treatment
Score: 6.5
Pyoderma Gangrenosum in An Ulcerative Colitis Pediatric Patient During Vedolizu…
PMID: 34003258
Year: 2021
Relationship Type:
Treatment
Score: 6.5
One of the most common complications of Crohn's disease (CD) is the formation of strictures. Endoscopy plays a vital role not only in the diagnosis,…
Still the Joker in the Pack: When to Take Out Cyclosporine in the Game?
PMID: 33742654
Year: 2021
Relationship Type:
Association
Score: 6.5
Cyclosporine modulates neutrophil functions via the SIRT6-HIF-1α-glycolysis axi…
PMID: 33634990
Year: 2021
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Ozanimod is an oral sphingosine 1-phosphate (S1P) receptor modulator selectively targeting S1P1 and S1P5, which reduces migration of lym…
Cyclosporine protects from intestinal epithelial injury by modulating butyrate …
PMID: 33102812
Year: 2020
Relationship Type:
Association
Score: 6.5
Gut homeostasis is a process that requires a prudent balance of host responses to the beneficial enteric microbial community and the pathogenic stim…
Evolution of Endoscopic Lesions in Steroid-Refractory Acute Severe Ulcerative C…
PMID: 32777552
Year: 2021
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Patients with ulcerative colitis (UC) often face complex treatment decisions. Although shared decision making (SDM) is considered import…
Phospholipid Cyclosporine Prodrugs Targeted at Inflammatory Bowel Disease (IBD)…
PMID: 32618133
Year: 2020
Relationship Type:
Treatment
Score: 6.5
With the increase of incidence, inflammatory bowel diseases (IBD), which are chronic diseases affecting the gastrointestinal tract, impose a conside…
Successful management of refractory immune-mediated enterocolitis with cyclospo…
PMID: 32278241
Year: 2020
Relationship Type:
Association
Score: 6.5
INTRODUCTION: Although the landmark of Crohn's Disease (CD) is the transmural inflammation, mucosal healing (MH), which is assessed by colonoscopy, …
Colon targeted bioadhesive pellets of curcumin and cyclosporine for improved ma…
PMID: 32277353
Year: 2020
Relationship Type:
Treatment
Score: 6.5
A key role of the gut microbiota in the establishment and maintenance of health, as well as in the pathogenesis of disease, has been identified over…
[Three cases of severe and fulminating ulcerative colitis with megacolon treate…
PMID: 32037361
Year: 2020
Relationship Type:
Association
Score: 6.5
Comment on United European Gastroenterol J. 2021 Dec;9(10):1193-1196. United European Gastroenterol J. 2022 Feb;10(1):126-127.
A novel player: cyclosporine therapy in the management of inflammatory bowel di…
PMID: 31620649
Year: 2019
Relationship Type:
Treatment
Score: 6.5
Genome-wide association studies have identified over 200 loci associated with IBD. We and others have recently shown that, in addition to variants i…
Hypoxia-inducible factor hydroxylase inhibition enhances the protective effects…
PMID: 31070931
Year: 2019
Relationship Type:
Treatment
Score: 6.5
Decreased levels of Faecalibacterium prausnitzii (F. prausnitzii), whose supernatant plays an anti-inflammatory effect, are frequently found in inf…
Cyclosporine for severe steroid-refractory ulcerative colitis: commenting the c…
PMID: 29327818
Year: 2018
Relationship Type:
Association
Score: 6.3
New Promising Combo Therapy in Inflammatory Bowel Diseases Refractory to Anti-T…
PMID: 29272353
Year: 2018
Relationship Type:
Treatment
Score: 6.3
Impact of Infliximab and Cyclosporine on the Risk of Colectomy in Hospitalized …
PMID: 28590343
Year: 2017
Relationship Type:
Treatment
Score: 6.3
BACKGROUND: Immunosuppressed patients are at risk of severe viral infections-related complications. National and international vaccination guidelin…
The use of Cyclosporin A in acute steroid-refractory ulcerative colitis: long t…
PMID: 21453876
Year: 2011
Relationship Type:
Treatment
Score: 6.1
BACKGROUND AND AIMS: Approximately 15% of patients with ulcerative colitis will have a severe flare requiring hospitalisation at some stage. For thos…
Factors affecting the efficacy of cyclosporin A therapy for refractory ulcerati…
PMID: 20370728
Year: 2010
Relationship Type:
Treatment
Score: 6.1
BACKGROUND AND AIMS: Cyclosporin A (CSA), an immunosuppressive agent, is highly efficacious in patients with refractory ulcerative colitis (UC). We r…
What is the importance of infliximab and cyclosporine in the treatment of corti…
PMID: 23576083
Year: 2012
Relationship Type:
Treatment
Score: 6.1
Ciclosporin use during pregnancy
PMID: 23516008
Year: 2013
Relationship Type:
Treatment
Score: 6.1
Ciclosporin (cyclosporine) is an immunosuppressive drug first approved for use in organ transplantation to prevent rejection. Ciclosporin is also kno…