| 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 |
Endoscopic and histologic response to cyclosporine in ulcerative colitis and th…
PMID: 27052254
Year: 2016
Relationship Type:
Treatment
Score: 9.3
INTRODUCTION: Cyclosporine (CsA) is an effective agent for treating patients with acute steroid-refractory ulcerative colitis (UC). The aim was to as…
Cyclosporine in patients with severe steroid refractory ulcerative colitis in t…
PMID: 23110487
Year: 2013
Relationship Type:
Treatment
Score: 9.1
Corticosteroids are the mainstay of therapy for severe ulcerative colitis. However, at least a third of patients fail to respond and face a colectomy…
[A case of ulcerative colitis accompanied with myelodysplastic syndrome success…
PMID: 21817844
Year: 2011
Relationship Type:
Association
Score: 9.1
A 64-year-old man had been admitted to a previous hospital because of melena and a diagnosis of ulcerative colitis (UC, pancolitis type) had been mad…
Cyclosporine is safe and effective in patients with severe ulcerative colitis
PMID: 20679905
Year: 2011
Relationship Type:
Treatment
Score: 9.1
BACKGROUND: Cyclosporine (CSA) is effective in the short-term for severe, steroid refractory ulcerative colitis; but its use has been limited by conc…
Rescue therapy with oral cyclosporine after use of ustekinumab in ulcerative co…
PMID: 34082044
Year: 2022
Relationship Type:
Treatment
Score: 8.5
Infliximab is more effective than cyclosporine as a rescue therapy for acute se…
PMID: 33948062
Year: 2021
Relationship Type:
Treatment
Score: 8.5
The present study was aimed to evaluate the suitability of agro-wastes and crude vegetable oils for the cost-effective production of poly-β-hydroxyb…
Comparison of outcomes of cyclosporine A and infliximab for steroid-refractory …
PMID: 33880817
Year: 2021
Relationship Type:
Association
Score: 8.5
In vitro and in vivo amelioration of colitis using targeted delivery system of …
PMID: 32892648
Year: 2020
Relationship Type:
Association
Score: 8.5
Not found
Polymeric Nanocarriers With Mucus-Diffusive and Mucus-Adhesive Properties to Co…
PMID: 31697948
Year: 2020
Relationship Type:
Treatment
Score: 8.5
BACKGROUND AND AIMS: Familial mediterranean fever (FMF), an autoinflammatory disease, is characterized by periodic fever and serositis. An MEFV gene…
Superficial granulomatous pyoderma in a patient with ulcerative colitis success…
PMID: 30460989
Year: 2019
Relationship Type:
Association
Score: 8.5
Cyclosporine A-loaded lipid nanoparticles in inflammatory bowel disease
PMID: 26972380
Year: 2016
Relationship Type:
Association
Score: 8.3
BACKGROUND: There are very few studies and no consensus concerning the choice between two- and three-stage ileal pouch-anal anastomosis [IPAA] in in…
Cyclosporine A regulates pro-inflammatory cytokine production in ulcerative col…
PMID: 25155925
Year: 2015
Relationship Type:
Treatment
Score: 8.3
BACKGROUND: There is uncertain evidence of effectiveness of 5-aminosalicylates (5-ASA) to induce and maintain response and remission of active Crohn…
Long-term efficacy and safety of cyclosporine as a rescue therapy in acute, ste…
PMID: 21278580
Year: 2011
Relationship Type:
Treatment
Score: 8.1
Cyclosporine and infliximab as rescue therapy for each other in patients with s…
PMID: 18928936
Year: 2008
Relationship Type:
Treatment
Score: 8.1
BACKGROUND: The single nucleotide polymorphism (SNP) rs2542151 within the gene locus region encoding protein tyrosine phosphatase non-receptor type …
Combined use of cyclosporine and azathioprine or 6-mercaptopurine in pediatric …
PMID: 8708884
Year: 1996
Relationship Type:
Association
Score: 8.1
Human intestinal lamina propria T cells have a low expression of the CD45RA antigen and a high expression of the CD45RO antigen. This phenotype is …
Clinical Response and Complications are not Associated with Drug Levels in Pati…
PMID: 29506124
Year: 2018
Relationship Type:
Treatment
Score: 7.3
BACKGROUND: IV ciclosporin therapy is effective in steroid-refractory ulcerative colitis. The optimal drug level to achieve response and minimize com…
Target identification in Fusobacterium nucleatum by subtractive genomics approa…
PMID: 27176600
Year: 2016
Relationship Type:
Treatment
Score: 7.3
Cyclosporine A (CsA) is a well-known immunosuppressive agent used as rescue therapy in severe steroid-refractory ulcerative colitis (UC). However, t…
Remission of diabetes mellitus induced by prednisolone in combination with cycl…
PMID: 39042703
Year: 2024
Relationship Type:
Adverse Effect
Score: 6.5
The Mechanism and Potential Therapeutic Effects of Cyclosporin, Cyclophilin, Pr…
PMID: 38276500
Year: 2024
Relationship Type:
Treatment
Score: 6.5
Background: Inflammatory bowel diseases (IBDs) have several treatment modalities including immunoregulators, like cyclosporine A, an immunosuppressan…
Cyclosporine treatment for severe steroid refractory immune-mediated colitis in…
PMID: 36693590
Year: 2024
Relationship Type:
Treatment
Score: 6.5