Lesinurad is an orally active selective uric acid reabsorption inhibitor used in the management of hyperuricemia associated with gout. It belongs to the uricosuric class of medicines and works primarily by inhibiting renal uric acid transporters involved in the reabsorption of uric acid.
Lesinurad selectively inhibits URAT1 (urate transporter 1) and OAT4 (organic anion transporter 4) in the renal proximal tubule. By reducing the reabsorption of uric acid, Lesinurad increases urinary uric acid excretion and lowers serum uric acid concentrations.
Lesinurad has been used in combination with a xanthine oxidase inhibitor, such as allopurinol or febuxostat, in appropriate patients whose serum uric acid target is not adequately achieved with xanthine oxidase inhibitor therapy alone.
Lesinurad is a synthetic small-molecule pharmaceutical compound with the molecular formula C17H14BrN3O2S and a molecular weight of approximately 404.28 g/mol. Its CAS Number is 878672-00-5.
Lesinurad is a selective uric acid transporter inhibitor developed for oral administration and pharmaceutical formulation.
Lesinurad inhibits URAT1, a major transporter responsible for renal uric acid reabsorption. It also inhibits OAT4, another transporter involved in urate reabsorption.
Inhibition of these transporters reduces renal tubular reabsorption of uric acid, increases urinary uric acid excretion and lowers circulating serum uric acid levels.
Lesinurad has been used as an adjunctive urate-lowering therapy for hyperuricemia associated with gout in patients who do not achieve adequate serum uric acid control with a xanthine oxidase inhibitor alone.
Its approved status and availability vary by market because the regulatory status of Lesinurad-containing products has changed in some regions.
Lesinurad API can be evaluated using validated analytical procedures for identification, assay, related substances, water content, residual solvents, elemental impurities and other applicable quality attributes.
HPLC and suitable spectroscopic and chromatographic techniques may be used for identity, assay and purity determination. Control of related substances and degradation products is important for pharmaceutical-grade Lesinurad.
Acceptance criteria should be based on the applicable manufacturer's drug-substance specification, Certificate of Analysis and relevant regulatory requirements.
Lesinurad should be stored in a tightly closed pharmaceutical-grade container under controlled storage conditions. The material should be protected from excessive heat, moisture, direct light and contamination. Specific storage requirements should follow the applicable manufacturer's approved specification.
Lesinurad API may be supplied for qualified pharmaceutical manufacturing, formulation development, analytical and research applications, subject to applicable quality and regulatory requirements.
Lesinurad API is available for qualified pharmaceutical development and manufacturing requirements subject to applicable quality and regulatory requirements. Customers can request product specifications, Certificate of Analysis, analytical documentation, packaging information and commercial details according to their requirements.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 2.0% |
| Residue on Ignition | NMT 0.5% |
| Individual Impurity | NMT 0.5% |
| Total Impurities | ≤ 1.5% |
| Water Content | NMT 1.0% |