- Therapeutic Category : Antigout
- CAS Number : 577778-58-6
- Molecular Formula : C13H8N6
- Molecular Weight : 248.24 g/mol
- Mesh Size : As per Customer Requirement
- Metrochem Development Status : Pipeline
Mechanism of Action:
Uric acid synthesis depends on the action of xanthine oxidase activity in the conversion of hypoxanthine to xanthine, followed by the conversion of xanthine to uric acid. Xanthine oxidase consists of a molybdenum ion as cofactor in the active center that has different redox states upon substrate binding.When a substrate such as hypoxanthine or xanthine binds, xanthine oxidase hydroxylates it and molybdenum ion is reduced from hexavalent, Mo(VI), to tetravalent form, Mo(IV). Molybdenum ion is reoxidized into hexavalent state once the hydroxylated substrate, xanthine or uric acid, dissociates from the active site. Topiroxostat is shown to interact with multiple amino acid residues of the solvent channel and additionally forms a reaction intermediate by covalent binding with molybdenum (IV) ion via an oxygen atom.It also forms hydrogen bonds with molybdenum (VI) ion, suggesting that it has multiple inhibition modes to xanthine oxidase.Enhanced binding interactions to xanthine oxidase achieves delayed dissociation of topiroxostat from the enzyme. 2-hydroxy-topiroxostat, the metabolite formed by primary hydroxylation of topiroxostat by xanthine oxidase, also causes time and concentration-dependent inhibition of the enzyme.Topiroxostat is shown to inhibit ATP-binding cassette transporter G2 (ABCG2) in vitro, which is a membrane protein responsible for recovering uric acid in the kidneys and secreting uric acid from the intestines.
Indicated for the treatment of gout and hyperurcemia.
Metrochem API Expertise:
Metrochem API Pvt Ltd is a leading manufacturer and supplier of Active Pharmaceutical Ingredients (APIs) through our manufacturing sites in Hyderabad and Vizag. Our API facilities have been inspected and approved by several global regulatory bodies including the US FDA, Japan PMDA, KFDA, and meet the cGMP compliance standards. Adapting quickly to the ever-evolving demands, we have emerged as one of the fastest growing organization in the pharmaceutical industry across the India. To cater our customer high volume requirements, we have dedicated each of our 6 manufacturing facilities to our 3 core product groups – APIs, Pelletization& Intermediates – reinforced by a well equipped, centralized Research & Development laboratory.
We have been successfully supplying APIs all over the globe for more than 15 years. Total reactor volume exceeds 1200 KL which includes pilot and multi-purpose units. We are capable of executing extensive API requirements for our customers. Metrochem API Pvt Ltd has an experienced team of highly skilled chemists, experienced regulatory professionals and supply chain experts, who are ready to handle your API manufacturing requirements with expert care. We also offer Contract Manufacturing, Contract Research, and Custom Synthesis services. We have a stand-alone R&D center located in Hyderabad with State-of-the-art analytical facilities and over 90 scientists.We have extensively worked on and delivered new products across a wide variety of therapeutic segments and as a company, we have built strong expertise in new product development.
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