Medically reviewed by Drugs.com. Last updated on May 21, 2020.
(le SIN ure ad)
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Zurampic: 200 mg [DSC]
Brand Names: U.S.
- Zurampic [DSC]
- Antigout Agent
- Uric Acid Transporter 1 (URAT1) Inhibitor
Lesinurad inhibits the function of transporter proteins involved in renal uric acid reabsorption (uric acid transporter 1 [URAT1] and organic anion transporter 4 [OAT4]), and lowers serum uric acid levels and increases renal clearance and fractional excretion of uric acid in patients with gout.
Extensive. Vdss: ~20 L
Metabolized oxidatively primarily via CYP2C9l plasma exposure to metabolites is minimal; metabolites are not known to contribute to activity
Urine (63%; ~30% as unchanged drug); feces (32%)
Time to Peak
Within 1 to 4 hours
>98%; primarily to albumin
Special Populations: Renal Function Impairment
Lesinurad exposure is increased by 30% in patients with estimated CrCl 60 to <90 mL/minute, 50% to 73% in patients with estimated CrCl 30 to <60 mL/minute, and 113% in patients with estimated CrCl <30 mL/minute; when compared with patients with normal renal function.
Special Populations: Hepatic Function Impairment
In patients with mild (Child-Pugh class A) and moderate (Child-Pugh class B), following administration of a single 400 mg dose, the AUC was 7% and 33% higher, respectively, when compared with patients with normal hepatic function.
Use: Labeled Indications
Hyperuricemia associated with gout: Treatment of hyperuricemia associated with gout (in combination with a xanthine oxidase inhibitor) in patients who have not achieved target serum uric acid levels with a xanthine oxidase inhibitor alone.
Limitations of use: Lesinurad is not recommended for the treatment of asymptomatic hyperuricemia. Lesinurad should not be used as monotherapy.
Severe renal impairment (CrCl <30 mL/minute), end-stage renal disease (ESRD), dialysis, kidney transplant recipients, tumor lysis syndrome, or Lesch-Nyhan syndrome
Hyperuricemia associated with gout: Oral: 200 mg once daily (in combination with a xanthine oxidase inhibitor, including allopurinol or febuxostat); maximum dose: 200 mg once daily. Note: If treatment with the xanthine oxidase inhibitor therapy is interrupted, lesinurad should also be withheld.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Refer to adult dosing.
Oral: Administer in the morning with food and water. Administer at the same time in the morning as the dose of xanthine oxidase inhibitor. Advise patients to stay well hydrated (eg 2 L of fluids/day).
Store at 20°C to 25°C (68°F to 77°F); excursions permitted from 15°C to 30°C (59°F to 86°F). Protect from light.
Alpelisib: May decrease the serum concentration of CYP2C9 Substrates (High risk with Inducers). Monitor therapy
Aspirin: May diminish the therapeutic effect of Lesinurad. Monitor therapy
CloZAPine: CYP3A4 Inducers (Weak) may decrease the serum concentration of CloZAPine. Monitor therapy
CYP2C9 Inducers (Moderate): May decrease the serum concentration of Lesinurad. Monitor therapy
CYP2C9 Inhibitors (Moderate): May increase the serum concentration of Lesinurad. Monitor therapy
Estrogen Derivatives (Contraceptive): Lesinurad may decrease the serum concentration of Estrogen Derivatives (Contraceptive). Management: Use of an additional, nonhormonal contraceptive is recommended in patients being treated with lesinurad who desire effective contraception. Consider therapy modification
Lumacaftor and Ivacaftor: May decrease the serum concentration of CYP2C9 Substrates (High Risk with Inhibitors or Inducers). Lumacaftor and Ivacaftor may increase the serum concentration of CYP2C9 Substrates (High Risk with Inhibitors or Inducers). Monitor therapy
NiMODipine: CYP3A4 Inducers (Weak) may decrease the serum concentration of NiMODipine. Monitor therapy
Progestins (Contraceptive): Lesinurad may decrease the serum concentration of Progestins (Contraceptive). Management: Use of an additional, nonhormonal contraceptive is recommended in patients being treated with lesinurad who desire effective contraception. Consider therapy modification
Rifapentine: May decrease the serum concentration of CYP2C9 Substrates (High risk with Inducers). Monitor therapy
Selpercatinib: CYP3A4 Inducers (Weak) may decrease the serum concentration of Selpercatinib. Monitor therapy
Tacrolimus (Systemic): CYP3A4 Inducers (Weak) may decrease the serum concentration of Tacrolimus (Systemic). Monitor therapy
Ubrogepant: CYP3A4 Inducers (Weak) may decrease the serum concentration of Ubrogepant. Management: Use an initial ubrogepant dose of 100 mg and second dose (if needed) of 100 mg when used with a weak CYP3A4 inducer. Consider therapy modification
Valproate Products: May increase the serum concentration of Lesinurad. Avoid combination
Incidence reported in combination with a xanthine oxidase inhibitor.
1% to 10%:
Central nervous system: Headache (5%)
Gastrointestinal: Gastroesophageal reflux disease (3%)
Infection: Influenza (5%)
Renal: Increased serum creatinine (≤6%; 1.5 x to <2.0 x baseline: 4%; ≥2.0 x baseline: 2%; most elevations were transient and resolved without therapy interruption), renal failure (2%)
Frequency not defined:
Cardiovascular: Cerebrovascular accident, myocardial infarction
Renal: Acute renal failure
<1%, postmarketing, and/or case reports: Nephrolithiasis
ALERT: U.S. Boxed WarningNephrotoxicity:
Acute renal failure has occurred with lesinurad and was more common when lesinurad was given alone.Appropriate use:
Lesinurad should be used in combination with a xanthine oxidase inhibitor.
Concerns related to adverse effects:
• Cardiovascular events: Major cardiac adverse events (cardiovascular deaths, non-fatal MI, or non-fatal strokes) were observed in clinical trials, although a causal relationship with lesinurad was not established.
• Gout flare: Following initiation of uric acid lowering therapy, gout may flare due to mobilization of urate from tissue deposits; gout flare prophylaxis is recommended when initiating lesinurad treatment. Lesinurad treatment may continue during gout flare and management of the flare.
• Nephrotoxicity: Lesinurad, when used concurrently with a xanthine oxidase inhibitor, is associated with an increased incidence of serum creatinine elevations (generally reversible). [US Boxed Warning]: Acute renal failure has occurred with lesinurad and was more common when lesinurad was given alone. Renal failure (acute and chronic) and nephrolithiasis have also been reported (when used in combination with a xanthine oxidase inhibitor). The incidence of renal-related adverse events was also higher with lesinurad dosed at 400 mg (which is higher than the approved dose).
• Renal impairment: Evaluate renal function prior to treatment initiation and periodically, as clinically indicated, thereafter (more frequently in patients with estimated CrCl <60 mL/minute or with serum creatinine elevations 1.5 to 2 times the baseline level). Lesinurad should not be initiated in patients with estimated CrCl <45 mL/minute and is contraindicated with estimated CrCl <30 mL/minute. Lesinurad is not expected to be effective in patients with estimated CrCl <30 mL/minute, end-stage renal disease (ESRD), and/or on dialysis. Interrupt treatment if serum creatinine is elevated to >2 times baseline level. Interrupt treatment and measure serum creatinine if symptoms indicative of acute uric acid nephropathy (including flank pain, nausea, or vomiting) occur; do not restart without determining the cause of the serum creatinine abnormality.
• Secondary hyperuricemia: Lesinurad has not been studied in patients with secondary hyperuricemia (including organ transplant recipients); use is contraindicated in patients with tumor lysis syndrome or Lesch-Nyhan syndrome, where the uric acid formation rate is greatly increased.
• CYP2C9 poor metabolizers: Lesinurad exposure is ~1.8 fold higher in CYP2C9 poor metabolizers; use with caution.
• Appropriate use: [US Boxed Warning]: Lesinurad should only be used in combination with a xanthine oxidase inhibitor; do not use as monotherapy. Lesinurad should be added when target serum uric acid levels are not achieved with a medically appropriate dose of single-agent xanthine oxidase inhibitor therapy. Lesinurad use is not recommended in patients taking allopurinol daily doses <300 mg (or <200 mg in patients with estimated CrCl <60 mL/minute).
Serum creatinine and estimated CrCl prior to treatment initiation and periodically, as clinically indicated, thereafter (more frequently in patients with estimated CrCl <60 mL/minute or with serum creatinine elevations 1.5 to 2 times the baseline level). Serum uric acid levels after every dose titration until desired level is achieved, then every 6 months (symptomatic patients) or every 12 months (all patients on urate-lowering therapy, regardless of symptoms) (FitzGerald 2018).
All forms of hormonal contraceptives (eg, oral, injectable, topical) may be less effective during therapy with lesinurad. Additional methods of contraception are recommended during therapy.
Adverse events were not observed in animal reproduction studies.
What is this drug used for?
• It is used to lower uric acid in the blood.
All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:
• Flu-like signs
WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:
• Kidney problems like unable to pass urine, blood in the urine, change in amount of urine passed, or weight gain
• Weakness on 1 side of the body, trouble speaking or thinking, change in balance, drooping on one side of the face, or blurred eyesight
• Chest pain
• Side pain
• Lower back pain
• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.
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More about lesinurad
- Side Effects
- During Pregnancy
- Dosage Information
- Drug Interactions
- En Español
- 2 Reviews
- Drug class: antihyperuricemic agents
Other brands: Zurampic