| Drug ID: | Drug60 |
|---|---|
| Drug Name: | Rosiglitazone |
| CID: | 77999 |
| DrugBank ID: | DB00412 |
| Modality: | Small Molecule |
| Groups: | approved|investigational |
| US Approved: | YES |
| Other Approved: | YES |
| Identifier: | NCT00065065, , NCT00309660 |
| Molecular Formula: | C18H19N3O3S |
| Molecular Weight: | 357.4 g/mol |
| Isomeric SMILES: | CN(CCOC1=CC=C(C=C1)CC2C(=O)NC(=O)S2)C3=CC=CC=N3 |
| Synonyms: | rosiglitazone; 122320-73-4; Rosiglizole; Rezult; rosiglitazona; Gaudil; Rosvel; TDZ 01; rosiglitazonum; DTXSID7037131 |
| Phase 0: | 0 |
| Phase 1: | 34 |
| Phase 2: | 39 |
| Phase 3: | 60 |
| Phase 4: | 53 |
| Description: | Rosiglitazone is an anti-diabetic drug in the thiazolidinedione class of drugs. It is marketed by the pharmaceutical company GlaxoSmithKline as a stand-alone drug (Avandia) and in combination with metformin (Avandamet) or with glimepiride (Avandaryl). Like other thiazolidinediones, the mechanism of action of rosiglitazone is by activation of the intracellular receptor class of the peroxisome proliferator-activated receptors (PPARs), specifically PPAR?. Rosiglitazone is a selective ligand of PPAR?, and has no PPAR?-binding action. Apart from its effect on insulin resistance, it appears to have an anti-inflammatory effect: nuclear factor kappa-B (NF?B) levels fall and inhibitor (I?B) levels increase in patients on rosiglitazone. Recent research has suggested that rosiglitazone may also be of benefit to a subset of patients with Alzheimer's disease not expressing the ApoE4 allele. This is the subject of a clinical trial currently underway. |
Molecular Structure
Knowledge Graph
| dtID | CID | Compound Name | Gene ID | Gene Name | Species | PubMed IDs | Action |
|---|---|---|---|---|---|---|---|
| dt540 | 77999 | Rosiglitazone | 8795 | TNFRSF10B | Homo sapiens (human) | 18164688 | Rosiglitazone results in increased expression of TNFRSF10B protein|glutathione inhibits the reaction [rosiglitazone results in increased expression of TNFRSF10B protein]|rosiglitazone results in increased expression of TNFRSF10B mRNA |
| dt541 | 77999 | Rosiglitazone | 8792 | TNFRSF11A | Mus musculus (house mouse) | 22286232 | Rosiglitazone inhibits the reaction [TNFSF11 protein results in increased expression of TNFRSF11A protein]|rosiglitazone inhibits the reaction [TNFSF11 protein results in increased expression of TNFRSF11A mrna] |
| dt542 | 77999 | Rosiglitazone | 4982 | TNFRSF11B | Mus musculus (house mouse) | 16054899 | Tetrachlorodibenzodioxin inhibits the reaction [[dexamethasone co-treated with rosiglitazone co-treated with 1-methyl-3-isobutylxanthine co-treated with INS1 protein] results in decreased expression of TNFRSF11B mrna]|egf protein inhibits the reaction [[d |
| dt543 | 77999 | Rosiglitazone | 27242 | TNFRSF21 | Homo sapiens (human) | 25572481 | Rosiglitazone results in increased expression of TNFRSF21 mRNA |
| dt544 | 77999 | Rosiglitazone | 8600 | TNFSF11 | Mus musculus (house mouse) | 22286232 | Rosiglitazone inhibits the reaction [TNFSF11 protein results in increased expression of TNFRSF11A protein]|[rosiglitazone co-treated with TNFSF11 protein] results in increased expression of PPARG mrna|rosiglitazone inhibits the reaction [TNFSF11 protein r |
| dt545 | 77999 | Rosiglitazone | 8742 | TNFSF12 | Homo sapiens (human) | 16982809 | Rosiglitazone results in decreased expression of TNFSF12 mRNA |
| dt546 | 77999 | Rosiglitazone | 9966 | TNFSF15 | Ovis aries (sheep) | 35504463 | [[biotin co-treated with pantothenic acid co-treated with INS protein co-treated with dexamethasone co-treated with 1-methyl-3-isobutylxanthine co-treated with rosiglitazone] results in increased susceptibility to bisphenol A] which results in decreased e |
| dt547 | 77999 | Rosiglitazone | 23043 | TNIK | Ovis aries (sheep) | 35504463 | [[biotin co-treated with pantothenic acid co-treated with INS protein co-treated with dexamethasone co-treated with 1-methyl-3-isobutylxanthine co-treated with rosiglitazone] results in increased susceptibility to bisphenol A] which results in decreased e |
| dt548 | 77999 | Rosiglitazone | 7137 | TNNI3 | Rattus norvegicus (Norway rat) | 21172411 | Rosiglitazone results in increased expression of TNNI3 protein |
| dt549 | 77999 | Rosiglitazone | 7139 | TNNT2 | Rattus norvegicus (Norway rat) | 31419397 | Rosiglitazone inhibits the reaction [citreoviridin results in increased secretion of TNNT2 protein] |
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 | |
|---|---|---|---|---|---|---|---|
| NCT00309660 | Treatment With Local PPARgamma Ligand in Distal Ulcerative Colitis | PHASE1|PHASE2 | UNKNOWN | Herlev Hospital | Ulcerative Colitis | DRUG: Rosiglitazone | Details |
| NCT00567593 | Gene Regulation by Thiazolidinediones | PHASE4 | Not recruiting | James Lewis | Inflammatory Bowel Disease;Inflammatory Bowel Dis… | Drug: Rosiglitazone;Drug: Rosiglitazone;Drug: Ros… | Details |
| NCT00065065 | A Trial of Rosiglitazone for Ulcerative Colitis | PHASE2 | COMPLETED | James Lewis | Ulcerative Colitis|Inflammatory Bowel Disease | DRUG: Rosiglitazone|DRUG: Placebo | Details |
| Disease ID | Disease Name | Definition | Category | Related Drugs | Mechanism | |
|---|---|---|---|---|---|---|
| No data available | ||||||
| Strategy ID | Therapeutic Strategy | Synonyms | Related Drugs | Mechanism | |
|---|---|---|---|---|---|
| S06 | Anti-fibrosis | fibrosis; tissue remodelling | GS-5745; STNM01 | Tissue remodelling and destruction in patients with IBD is … | Details |
Rosiglitazone Does Not Affect the Risk of Inflammatory Bowel Disease: A Retrosp…
PMID: 37242462
Year: 2023
Relationship Type:
Treatment
Score: 6.5
Human studies on the effect of rosiglitazone on inflammatory bowel disease (IBD) are still lacking. We investigated whether rosiglitazone might affec…
Comparison of anti-inflammatory properties of peroxisome proliferator-activated…
PMID: 24304573
Year: 2013
Relationship Type:
Treatment
Score: 6.1
Non-specific inflammatory bowel disease (IBD), including ulcerative colitis and Crohn;s disease, is a chronic noninfectious inflammatory disease whos…
Comparison of the anti-inflammatory and therapeutic actions of PPAR-gamma agoni…
PMID: 23388479
Year: 2012
Relationship Type:
Treatment
Score: 6.1
Non-specific inflammatory bowel diseases, including ulcerative colitis and Crohn;s disease, are chronic non-infectious diseases that showed an increa…