Repositioning Candidate Details
| Candidate ID: | R1229 |
| Source ID: | DB09121 |
| Source Type: | approved; withdrawn |
| Compound Type: | small molecule |
| Compound Name: | Aurothioglucose |
| Synonyms: | Auromyose; Aurothioglucose; Gold thioglucose |
| Molecular Formula: | C6H11AuO5S |
| SMILES: | OC[C@H]1O[C@H](S[Au])[C@H](O)[C@@H](O)[C@@H]1O |
| Structure: |
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| DrugBank Description: | Aurothioglucose, also known as gold thioglucose, was formerly used to treat rheumatoid arthritis. Contemporary research on the effect of gold salts treatment began in 1935, primarily to reduce inflammation and to slow disease progression in patients with rheumatoid arthritis . The use of gold compounds has decreased since the 1980s owing to numerous side effects, limited efficacy, and slow onset of action. Many if not most gold compounds that were indicated for rheumatoid arthritis therapy have since been replaced with the use of various current disease modifying anti-rheumatic drugs (DMARDs) like methotrexate and others, which are far more effective. |
| CAS Number: | 12192-57-3 |
| Molecular Weight: | 392.18 |
| DrugBank Indication: | Aurothioglucose is indicated for the adjunctive treatment of early active adult and juvenile type rheumatoid arthritis that is not adequately controlled by other anti-inflammatory agents and conservative measures like salicylate, glucocorticoids, etc. . In chronic, advanced cases of rheumatoid arthritis, such gold therapy is not demonstrated to be as valuable . Antirheumatic measures such as salicylate and other anti-inflammatory drugs (both steroidal and non steroidal) may be continued after initiation of gold therapy . After improvement commences, these measures may be discontinued slowly as symptoms permit . |
| DrugBank Pharmacology: | After administration, patient serum levels of gold rise sharply but decline over the following week . Peak levels with aqueous preparations are higher and decline faster than those with oily preparations . Regular weekly administration produces a continuous rise in the basal value for several months, after which the serum level becomes relatively stable . After a standard weekly dose, considerable individual variation in the levels of gold can be observed . A steady decline in gold levels occurs when the interval between injections is lengthened, and small amounts may be found in the serum for months after discontinuation of therapy . The incidence of toxic reactions is seemingly unrelated to the plasma level of gold, but may perhaps be more associated with the total cumulative content of gold in the body . |
| DrugBank MoA: | Rheumatoid arthritis is an autoimmune disease in which the body's immune system mistakenly attacks the lining of various skeletal bone joints of the body . These attacks are facilitated by various pro-inflammatory immune cells and agents like cytokines, histamines, mast cells, macrophages, monocytes, lymphocytes, leukocytes, and many others . The longterm result of this unwanted immune response is chronic inflammation and painful tissue damage . The cause of the malfunctioning immune system in rheumatoid arthritis is unknown and there is no definitive cure for the condition . Similarly, the mechanism of action of aurothioglucose is also not well elucidated. Nevertheless, some studies have suggested that the combination of both the sulfhydryl ligand and aureus cation present in aurothioglucose elicits an inhibitory effect on adenylyl cyclase activity in human lymphocyte membranes and in membranes of T and B lymphocyte subsets . In particular, such inhibition of the activity of adenylyl cyclase and its various isoforms would theoretically also limit the cyclases' ability to induce mast cell degranulation and histamine release, to enhance respiratory burst effects, to stimulate the action of resting macrophages, to induce and activate phagocytes, to induce neutrophil chemotaxis, etc. - all of which are pro-inflammatory actions . |
| Targets: | Adenylate cyclase type 1; Adenylate cyclase type 2; Adenylate cyclase type 5 |
| Inclusion Criteria: | Therapeutic strategy associated |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs | |
|---|---|---|---|---|---|
| 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 |
| Diseases ID | DO ID | Disease Name | Definition | Class | |
|---|---|---|---|---|---|
| I15 | 1290 | Bone disease | A connective tissue disease that affects the structure or development of bone or causes an impairment of normal bone function. http://en.wikipedia.org/wiki/Bone_disease | disease of anatomical entity/ musculoskeletal system disease/connective tissue disease | Details |