Lesinurad
Lesinurad Uses, Dosage, Side Effects, Food Interaction and all others data.
Lesinurad is an oral uric acid transporter 1 (URAT1) inhibitor indicated for the treatment of hyperuricemia associated with gout. It reduces serum uric acid concentration through the inhibition of URAT1, an enzyme responsible for reuptake of uric acid from the renal tubule, and OAT4, another uric acid transporter associated with diuretic-induced hyperuricemia.
Marketed as the product Zurampic, it is indicated for use in combination with a xanthine oxidase inhibitor for the treatment of hyperuricemia associated with gout inpatients who have not achieved target serum uric acid levels with a xanthine oxidase inhibitor alone. In August 2017, a combination oral therapy consisting of lesinurad and Allopurinol was FDA-approved under the brand name Duzallo indicated for the treatment of gout-related hyperuricemia in patients with uncontrolled gout.
Dose-dependent reductions in serum uric acid levels and increases in urinary uric acid excretion have been observed following single and multiple oral doses of lesinurad.
| Trade Name | Lesinurad |
| Availability | Discontinued |
| Generic | Lesinurad |
| Lesinurad Other Names | Lesinurad |
| Related Drugs | allopurinol, febuxostat, Zyloprim, probenecid, Uloric, Krystexxa |
| Type | Oral |
| Formula | C17H14BrN3O2S |
| Weight | Average: 404.28 Monoisotopic: 402.999011 |
| Protein binding | Lesinurad is extensively bound to proteins in plasma (greater than 98%), mainly to albumin. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Lesinurad is a uric acid 1 transporter inhibitor typically used in combination with a xanthine oxidase inhibitor to treat hyperuricemia associated with gout in patients with inadequate control of uric acid levels with xanthine oxidase inhibitor monotherapy.
For use, in combination with a xanthine oxidase inhibitor, for the treatment of hyperuricemia associated with gout in patients who have not achieved target serum uric acid levels with a xanthine oxidase inhibitor alone.
Lesinurad is also used to associated treatment for these conditions: Hyperuricemia
How Lesinurad works
Lesinurad inhibits the activity of uric acid transporter 1 (URAT1) and organic anion transporter 4 (OAT4). URAT1 is a major transporter enzyme responsible for reuptake of uric acid from the renal tubules; inhibition of URAT1 function thereby increases excretion of uric acid.
Food Interaction
- Drink plenty of fluids.
- Take with a full glass of water.
- Take with food.
Lesinurad Drug Interaction
Moderate: ethinyl estradiol / norethindroneUnknown: amphotericin b lipid complex, isotretinoin, tocilizumab, corticotropin, alteplase, loxapine, fluticasone / salmeterol, theophylline, ketotifen ophthalmic, aluminum hydroxide, testosterone, umeclidinium / vilanterol, dolasetron, hydralazine, mesalamine, nebivolol, benazepril, hyoscyamine / methenamine / methylene blue / phenyl salicylate, piperacillin / tazobactam
Lesinurad Disease Interaction
Major: secondary hyperuricemia, severe renal impairmentModerate: CV disease, hepatic impairment
Volume of Distribution
The mean steady state volume of distribution of lesinurad was approximately 20 L following intravenous dosing.
Elimination Route
Oral lesinurad is rapidly absorbed, reaching maximum plasma concentrations (Cmax) within 1–4 h following the administration a single 200 mg dose (in either the fed or fasted state).
Elimination Route
Within 7 days following single dosing of radiolabeled lesinurad, 63% of administered radioactive dose was recovered in urine and 32% of administered radioactive dose was recovered in feces. Most of the radioactivity recovered in urine (> 60% of dose) occurred in the first 24 hours. Unchanged lesinurad in urine accounted for approximately 30% of the dose.
Innovators Monograph
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