Basic information of drug: DB09295
| Drug id | DB09295 |
| Drug name | Talniflumate |
| Description | Talniflumate, is an anti-inflammatory molecule studied and used as a mucin regulator in the treatment of cystic fibrosis, chronic obstructive pulmonary disease (COPD) and asthma [L1400]. In addition, it is used in inflammatory conditions such as rheumatoid arthritis. Phase I trials with talniflumate... |
| State | solid |
| Cas number | 66898-62-2 |
| Synonyms | Talniflumate Talniflumato Talniflumatum |
| Sequences | None |
| Indication | Talnifumate is a phthalidyl ester of nifumic acid, which has potent analgesic and anti-inflammatory effects and is widely used to treat inflammatory disorders, such as rheumatoid arthritis and osteoarthritis [L1409], and has also been studied for the management of cystic fibrosis [L1403]. |
| Pharmacodynamics | Talniflumate is metabolized to its prodrug, niflumic acid, which has several pharmacodynamic effects. Firstly, it blocks synthesis of mucin. Secondly, talniflumate blocks prostaglandin synthesis by cyclooxygenases, which aids in pain and inflammation management. |
| Mechanism of action | Talniflumate is a strong and selective inhibitor of core mucin-synthesizing enzyme GCNT3 (core 2 b-1,6 N-acetylglucosaminyltransferase). Talniflumate decreases gene expression of GCNT3 and production of mucins in vivo and in vitro. Talniflumate improves response of pancreatic tumors to gefitinib (ch... |
| Metabolism | Extensive liver metabolism. |
| Toxicity | LD50 orally in rats: 12000 mg/kg [L1410] |