Lesinurad

404.28096

404.28

09ERP08I3W|Q59CAT99RS|73WY698HZ7

M04AA51|M04AB05|M - Musculo-skeletal system

93.3

4.7

1.72±0.1 g/cm3

643.7°C at 760 mmHg

343.1±34.3 °C

1.776

P264, P270, P301+P312, P330, P501

H302

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P264, P270, P301+P312, P330, and P501|Aggregated GHS information provided by 5 companies from 2 notifications to the ECHA C&L Inventory.

In large clinical trials, serum enzyme elevations were rare during lesinurad therapy and no more common than with placebo, and no instances of clinically apparent liver injury attributable to lesinurad were reported. Clinical experience with lesinurad therapy has been limited, but there have yet to be reports of clinically apparent liver injury attributable to its use.

Lesinurad is extensively bound to proteins in plasma (greater than 98%), mainly to albumin.

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.|FDA Label|Duzallo is indicated in adults for the treatment of hyperuricaemia in gout patients who have not achieved target serum uric acid levels with an adequate dose of allopurinol alone.|Zurampic, in combination with a xanthine oxidase inhibitor, is indicated in adults for the adjunctive treatment of hyperuricaemia in gout patients (with or without tophi) who have not achieved target serum uric acid levels with an adequate dose of a xanthine oxidase inhibitor alone.,|Treatment of hyperuricaemia|Prevention of hyperuricaemia, Treatment of hyperuricaemia

Lesinurad is a selective inhibitor of uric acid reabsorption which is used in combination with other agents in the therapy of gout. Lesinurad has had limited clinical use, but has not been associated with serum enzyme elevations during therapy or with instances of clinically apparent liver injury.

Antigout Agents

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.

Agents that increase uric acid excretion by the kidney (URICOSURIC AGENTS), decrease uric acid production (antihyperuricemics), or alleviate the pain and inflammation of acute attacks of gout. (See all compounds classified as Gout Suppressants.)|Gout suppressants that act directly on the renal tubule to increase the excretion of uric acid, thus reducing its concentrations in plasma. (See all compounds classified as Uricosuric Agents.)

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).|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.|The mean steady state volume of distribution of lesinurad was approximately 20 L following intravenous dosing.

Lesinurad undergoes oxidative metabolism mainly via the polymorphic cytochrome P450 CYP2C9 enzyme.

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.

((5-bromo-4-(4-cyclopropyl-1-naphthyl)-4H-1,2,4-triazol-3-yl)sulfanyl)acetic acid

Human drugs -> Duzallo -> EMA Drug Category|Antigout preparations -> Human pharmacotherapeutic group|Human drugs -> Zurampic -> EMA Drug Category|Human Drugs -> EU pediatric investigation plans|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients