Investigational Drug Details
| Drug ID: | D318 |
| Drug Name: | Salsalate |
| Synonyms: | 2-Carboxyphenyl salicylate; Disalicylic acid; o-Salicylsalicylic acid; Salicylic acid bimolecular ester; Salicyloxysalicylic acid; Salicyloylsalicylic acid; Salicylsalicylic acid; Sasapyrin; Sasapyrine |
| Type: | Chemical drug |
| DrugBank ID: | DB01399 |
| DrugBank Description: | Salsalate is a nonsteroidal anti-inflammatory agent for oral administration. Salsalate's mode of action as an anti-inflammatory and antirheumatic agent may be due to inhibition of synthesis and release of prostaglandins. The usefulness of salicylic acid, the active in vivo product of salsalate, in the treatment of arthritic disorders has been established. In contrast to aspirin, salsalate causes no greater fecal gastrointestinal blood loss than placebo. Salsalate is readily soluble in the small intestine where it is partially hydrolyzed to two molecules of salicylic acid. A significant portion of the parent compound is absorbed unchanged and undergoes rapid esterase hydrolysis in the body. The parent compound has an elimination half-life of about 1 hour. Salicylic acid (the active metabolite) biotransformation is saturated at anti-inflammatory doses of salsalate. Such capacity limited biotransformation results in an increase in the half-life of salicylic acid from 3.5 to 16 or more hours. |
| PubChem ID: | 5161 |
| CasNo: | 552-94-3 |
| Repositioning for NAFLD: | Yes |
| SMILES: | O(C(=O)c1c(O)cccc1)c1c(C(=O)O)cccc1 |
| Structure: |
|
| InChiKey: | WVYADZUPLLSGPU-UHFFFAOYSA-N |
| Molecular Weight: | 258.229 |
| DrugBank Targets: | Prostaglandin G/H synthase 2 inhibitor; Prostaglandin G/H synthase 1 inhibitor |
| DrugBank MoA: | The mode of anti-inflammatory action of salsalate and other nonsteroidal anti-inflammatory drugs is not fully defined, but appears to be primarily associated with inhibition of prostaglandin synthesis. This inhibition of prostaglandin synthesis is done through the inactivation of cyclooxygenase-1 (COX-1) and COX-2, which are reponsible for catalyzing the formation of prostaglandins in the arachidonic acid pathway. Although salicylic acid (the primary metabolite of salsalate) is a weak inhibitor of prostaglandin synthesis in vitro, salsalate appears to selectively inhibit prostaglandin synthesis in vivo, providing anti-inflammatory activity equivalent to aspirin and indomethacin. Unlike aspirin, salsalate does not inhibit platelet aggregation. |
| DrugBank Pharmacology: | Salsalate is a nonsteroidal anti-inflammatory agent for oral administration. Salsalate's mode of action as an anti-inflammatory and antirheumatic agent may be due to inhibition of synthesis and release of prostaglandins. The usefulness of salicylic acid, the active in vivo product of salsalate, in the treatment of arthritic disorders has been established. In contrast to aspirin, salsalate causes no greater fecal gastrointestinal blood loss than placebo. |
| DrugBank Indication: | For relief of the signs and symptoms of rheumatoid arthritis, osteoarthritis and related rheumatic disorders. |
| Targets: | PTGS2 inhibitor; PTGS1 inhibitor |
| Therapeutic Category: | NSAID |
| Clinical Trial Progress: | Phase 4 completed (NCT03222206) |
| Latest Progress: | Under clinical trials |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L0527 | NCT03222206 | Phase 4 | Not recruiting | No Results Available | 08/07/2017 | 12 December 2020 | Details |
| L0814 | KCT0002441 | Not applicable | Recruiting | No Results Available | 01/09/2017 | 11 March 2019 | Details |
| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name |
|---|
| 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 |
| Article ID | PMID | Source | Title | |
|---|---|---|---|---|
| A05580 | 33200549 | Basic Clin Pharmacol Toxicol | Salsalate reverses metabolic disorders in a mouse model of non-alcoholic fatty liver disease through AMPK activation and caspase-6 activity inhibition. | Details |
| A17825 | 27554471 | Diabetes | Salsalate (Salicylate) Uncouples Mitochondria, Improves Glucose Homeostasis, and Reduces Liver Lipids Independent of AMPK-β1. | Details |
| A19872 | 26292849 | Br J Pharmacol | Salsalate attenuates diet induced non-alcoholic steatohepatitis in mice by decreasing lipogenic and inflammatory processes. | Details |
| A23218 | 23948064 | Biochem Pharmacol | Salsalate and adiponectin ameliorate hepatic steatosis by inhibition of the hepatokine fetuin-A. | Details |
| A25502 | 21764223 | Med Hypotheses | Full-spectrum antioxidant therapy featuring astaxanthin coupled with lipoprivic strategies and salsalate for management of non-alcoholic fatty liver disease. | Details |