Investigational Drug Details
| Drug ID: | D107 |
| Drug Name: | Diacerein |
| Synonyms: | Diacerein |
| Type: | Chemical drug |
| DrugBank ID: | DB11994 |
| DrugBank Description: | Diacerein is a prodrug which is metabolized to rhein. It is currently approved in France for the treatment of osteoarthritis although the use of diacerein is restricted due to the side effects including severe diarrhea . Diacerein is under investigation for the treatment of Insulin Resistance, Diabetes Mellitus (Type 2), and Diabetes-Related Complications. |
| PubChem ID: | 26248 |
| CasNo: | 13739-02-1 |
| Repositioning for NAFLD: | Yes |
| SMILES: | O(C(=O)C)c1c2c(C(=O)c3c(C2=O)c(OC(=O)C)ccc3)cc(c1)C(=O)O |
| Structure: |
|
| InChiKey: | TYNLGDBUJLVSMA-UHFFFAOYSA-N |
| Molecular Weight: | 368.297 |
| DrugBank Targets: | Oxysterols receptor LXR-alpha inhibitor; Oxysterols receptor LXR-beta inhibitor; Arylamine N-acetyltransferase inhibitor; Arachidonate 5-lipoxygenase inhibitor; Cytochrome P450 1A2 inhibitor; Cytochrome P450 3A Subfamily inhibitor; Cytochrome P450 2E1 inh |
| DrugBank MoA: | Diacerein's active metabolite rhein reduces cartilage destruction by decreasing expression of matrix metalloproteinase (MMP)-1 and -3 as well as upregulating tissue inhibitor of matrix metalloproteinases which serve to reduce the activity of several MMPs . The anti-inflammatory action of rhein reduces the level of interleukin-1beta activity which plays a large role in reduction of extracellular matrix production, MMP activity, and continued inflammation . Rhein reduces abnormal osteoblast synthetic activity through an unknown mechanism . |
| DrugBank Pharmacology: | Decreases inflammation and cartilage destruction and also corrects altered osteoblast acitivity . |
| DrugBank Indication: | For the treatment of osteoarthritis affecting the hip or knee . |
| Targets: | ALOX5 inhibitor |
| Therapeutic Category: | Antiarthritic drug; antiinflammatory agent |
| Clinical Trial Progress: | Phase 3 completed (NCT02242149: Diacerein reduced mean HbA1c levels, with peak of effect at the 24th week of treatment. The drug was well tolerated and may be indicated as adjunct treatment in patients with type 2 diabetes, particularly in those with osteoarthritis.) |
| Latest Progress: | Under clinical trials |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L0142 | NCT02242149 | Phase 3 | Completed | No Results Available | October 14, 2014 | May 3, 2018 | Details |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs | |
|---|---|---|---|---|---|
| S01 | Improve insulin resistance | insulin sensitizer; insulin resistance; glucose tolerance | Biguanide: increases 5-AMP activated protein kinase signaling; SGLT-2 inhibitor; Thiazalidinedione: selective PPAR-γ agonists; GLP-1 agonist | Metformin; Empagliflozin; Canagliflozin; Rosiglitazone; Pioglitazone; Liraglutide | Details |
| S05 | Anti-inflammatory | inflammatory | Bile acid; TNF-a inhibitor; Dual PPAR-α and -δ agonists; Toll-Like Receptor; (TLR)-4 antagonist; Caspase inhibitor; ASK-1 inhibitor | Ursodeoxycholic Acid; Pentoxifylline; Elafibranor; JKB-121; Emricasan; Selonsertib; | Details |
| Article ID | PMID | Source | Title | |
|---|---|---|---|---|
| A11901 | 30687994 | Diabetes Obes Metab | Efficacy of diacerein in reducing liver steatosis and fibrosis in patients with type 2 diabetes and non-alcoholic fatty liver disease: A randomized, placebo-controlled trial. | Details |
| A49396 | 35765026 | J Transl Med | Rhubarb free anthraquinones improved mice nonalcoholic fatty liver disease by inhibiting NLRP3 inflammasome. | Details |