| 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 |
Long-term comparative efficacy of cyclosporine- or infliximab-based strategies …
PMID: 25046008
Year: 2014
Relationship Type:
Treatment
Score: 10.0
BACKGROUND: The short-term efficacy of infliximab (IFX) and cyclosporine A (CsA) in steroid-refractory ulcerative colitis (SRUC) has been recently sh…
Rescue therapy with cyclosporine or infliximab is not associated with an increa…
PMID: 24297054
Year: 2014
Relationship Type:
Treatment
Score: 10.0
BACKGROUND: Cyclosporine and infliximab (IFX) are effective medical therapies for inducing remission in patients with steroid-refractory ulcerative c…
[Treatment of patients with severe glucocorticoid-refractory ulcerative colitis…
PMID: 24050446
Year: 2013
Relationship Type:
Treatment
Score: 10.0
Cyclosporine and infliximab are so-called 'rescue-therapies' as last resort for the treatment of patients with severe glucocorticoid-refractory ulcer…
Infliximab versus cyclosporine as rescue therapy in acute severe steroid-refrac…
PMID: 23114475
Year: 2013
Relationship Type:
Treatment
Score: 10.0
PURPOSE: Acute severe colitis affects 25 % of patients with ulcerative colitis (UC). Up to 30-40 % of these patients are resistant to intensive stero…
The effect of intravenous cyclosporine on rates of colonic surgery in hospitali…
PMID: 22751334
Year: 2012
Relationship Type:
Association
Score: 10.0
BACKGROUND: The role of intravenous (IV) cyclosporine in severe Crohn's colitis (CC) is poorly studied. AIM: Our primary aim was to determine the in-…
Cyclosporine or infliximab as rescue therapy in severe refractory ulcerative co…
PMID: 22398101
Year: 2012
Relationship Type:
Treatment
Score: 10.0
INTRODUCTION: About 30-40% of patients with acute severe ulcerative colitis (UC) fail to respond to intensive intravenous (iv) corticosteroid treatme…
Infliximab or cyclosporine for acute severe ulcerative colitis: a retrospective…
PMID: 22098019
Year: 2012
Relationship Type:
Treatment
Score: 10.0
BACKGROUND AND AIM: Medical treatment of steroid-refractory ulcerative colitis (UC) is limited to either cyclosporine or infliximab. Studies comparin…
Acute severe colitis: infliximab and/or cyclosporine?
PMID: 21466485
Year: 2011
Relationship Type:
Treatment
Score: 10.0
Acute severe ulcerative colitis is a serious condition that requires early hospitalization, with intensive monitoring and treatment. Despite the rece…
Infliximab or cyclosporine as rescue therapy in hospitalized patients with ster…
PMID: 21438096
Year: 2012
Relationship Type:
Treatment
Score: 10.0
BACKGROUND: Cyclosporine (CsA) or infliximab (IFX) are used as rescue therapies in steroid-refractory, severe attacks of ulcerative colitis (UC). The…
Colon salvage therapy for acute severe colitis: cyclosporine or infliximab?
PMID: 21423006
Year: 2011
Relationship Type:
Treatment
Score: 10.0
PURPOSE OF REVIEW: Steroid-refractory acute severe colitis (ASC) poses a significant clinical challenge to both physicians and surgeons alike. This r…
Successive treatment with cyclosporine and infliximab in steroid-refractory ulc…
PMID: 21386832
Year: 2011
Relationship Type:
Treatment
Score: 10.0
OBJECTIVES: Rescue therapy with either cyclosporine (CYS) or infliximab (IFX) is an effective option in patients with intravenous steroid-refractory …
Long-term outcome in patients with ulcerative colitis treated with intravenous …
PMID: 21122535
Year: 2010
Relationship Type:
Treatment
Score: 10.0
BACKGROUND AND AIM: Rescue therapy with intravenous cyclosporine A (CsA) helps to avoid colectomy in a substantial proportion of patients with severe…
Rapid endoscopic improvement is important for 1-year avoidance of colectomy but…
PMID: 20614157
Year: 2010
Relationship Type:
Treatment
Score: 10.0
BACKGROUND: Intravenous (IV) cyclosporine A (CSA) is one of the treatments of choice for patients with steroid-refractory severe ulcerative colitis (…
Ozanimod Maintenance Therapy After Cyclosporine Induction in Acute Severe Ulcer…
PMID: 35919406
Year: 2022
Relationship Type:
Treatment
Score: 9.5
Ozanimod has recently received US Food and Drug Administration approval for moderate-to-severe ulcerative colitis. Treatment of acute severe colitis …
Cyclosporine Therapy as a Rescue Treatment in Steroid Refractory Acute Severe U…
PMID: 35786613
Year: 2022
Relationship Type:
Treatment
Score: 9.5
BACKGROUND: Cyclosporine is a rescue treatment alternative to avoid colectomy in corticosteroid refractory acute severe ulcerative colitis. In this s…
PLA(2)-Triggered Activation of Cyclosporine-Phospholipid Prodrug as a Drug Targ…
PMID: 35336048
Year: 2022
Relationship Type:
Treatment
Score: 9.5
Oral medication with activity specifically at the inflamed sites throughout the gastrointestinal tract and limited systemic exposure would be a major…
Cyclosporine-Induced Kaposi Sarcoma in a Patient With Ulcerative Colitis
PMID: 34079842
Year: 2021
Relationship Type:
Association
Score: 9.5
Kaposi sarcoma (KS) is an angioproliferative neoplasm associated with human herpesvirus-8. Gastrointestinal KS has been well documented in immunosupp…
Penile pyoderma gangrenousm treated with cyclosporine: Case report
PMID: 30317330
Year: 2018
Relationship Type:
Treatment
Score: 9.3
Pyoderma gangrenosum (PG) of the penis is a very rare entity in medicine and it can be destructive. Generally, pyoderma gangrenosum is known to be co…
Long-Term Efficacy and Safety of Cyclosporine in a Cohort of Steroid-Refractory…
PMID: 28675163
Year: 2017
Relationship Type:
Treatment
Score: 9.3
OBJECTIVES: To determine the efficacy and safety of cyclosporine (CyA) in a large national registry-based population of patients with steroid-refract…
The Effective Treatment with Cyclosporine of a Ulcerative Colitis Patient with …
PMID: 28566594
Year: 2017
Relationship Type:
Treatment
Score: 9.3
Although extraintestinal manifestations of inflammatory bowel diseases are not uncommon, few reports have described concurrent idiopathic thrombocyto…