Tariful
Tariful Uses, Dosage, Side Effects, Food Interaction and all others data.
Tariful, 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 . In addition, it is used in inflammatory conditions such as rheumatoid arthritis. Phase I trials with talniflumate for the treatment of cystic fibrosis and COPD were completed in August 2001, and phase II trials were performed in Ireland for the treatment of cystic fibrosis but this research has now been discontinued . Tariful has been approved for approximately 20 years in Argentina other countries (excluding the United States, Europe, and Japan) .
Tariful 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.
Trade Name | Tariful |
Generic | Talniflumate |
Talniflumate Other Names | Talniflumate, Talniflumato, Talniflumatum |
Type | |
Formula | C21H13F3N2O4 |
Weight | Average: 414.34 Monoisotopic: 414.082741396 |
Protein binding | Niflumic acid, the active form of Talniflumate, is weak acid that is strongly bound to plasma proteins. Bioavailability was 100% in a study of 12 volunteers. It is a weak acid, strongly bound to plasma proteins . |
Groups | Experimental |
Therapeutic Class | |
Manufacturer | |
Available Country | |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
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 , and has also been studied for the management of cystic fibrosis .
How Tariful works
Tariful is a strong and selective inhibitor of core mucin-synthesizing enzyme GCNT3 (core 2 b-1,6 N-acetylglucosaminyltransferase). Tariful decreases gene expression of GCNT3 and production of mucins in vivo and in vitro. Tariful improves response of pancreatic tumors to gefitinib (chemotherapy drug). Tariful is a strong calcium-activated chloride channel (CaCC) blocker.
Toxicity
LD50 orally in rats: 12000 mg/kg
Volume of Distribution
In 12 subjects after a single oral administration, total plasma clearance of the main metabolite, niflumic acid, averaged 45 ml/min giving a distribution volume of 0.12 l/kg on average .
Half Life
Approximately 2h in 12 subjects
Clearance
This drug undergoes extensive first pass effect.
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