Lesinurad

DB11560

small molecule approved investigational

Deskripsi

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 in
patients 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 DB00437 was FDA-approved under the brand name Duzallo indicated for the treatment of gout-related hyperuricemia in patients with uncontrolled gout.

Struktur Molekul 2D

Berat 404.28
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) -
Volume Distribusi The mean steady state volume of distribution of lesinurad was approximately 20 L following intravenous dosing.
Klirens (Clearance) -

Absorpsi

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).

Metabolisme

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

Rute Eliminasi

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.

Interaksi Makanan

3 Data
  • 1. Drink plenty of fluids.
  • 2. Take with a full glass of water.
  • 3. Take with food.

Interaksi Obat

1085 Data
Nitrofurantoin The serum concentration of Nitrofurantoin can be increased when it is combined with Lesinurad.
Pegloticase The risk or severity of adverse effects can be increased when Lesinurad is combined with Pegloticase.
Fluvoxamine The metabolism of Lesinurad can be decreased when combined with Fluvoxamine.
Troglitazone The metabolism of Lesinurad can be decreased when combined with Troglitazone.
Fluoxetine The metabolism of Lesinurad can be decreased when combined with Fluoxetine.
Nabilone The metabolism of Lesinurad can be decreased when combined with Nabilone.
Efavirenz The metabolism of Lesinurad can be decreased when combined with Efavirenz.
Mifepristone The metabolism of Lesinurad can be decreased when combined with Mifepristone.
Felbamate The metabolism of Lesinurad can be decreased when combined with Felbamate.
Sulfinpyrazone The metabolism of Lesinurad can be decreased when combined with Sulfinpyrazone.
Iproniazid The metabolism of Lesinurad can be decreased when combined with Iproniazid.
Medical Cannabis The metabolism of Lesinurad can be decreased when combined with Medical Cannabis.
Imatinib The metabolism of Lesinurad can be decreased when combined with Imatinib.
Valproic acid The metabolism of Lesinurad can be decreased when combined with Valproic acid.
Fluconazole The metabolism of Lesinurad can be decreased when combined with Fluconazole.
Floxuridine The metabolism of Lesinurad can be decreased when combined with Floxuridine.
Nicardipine The metabolism of Lesinurad can be decreased when combined with Nicardipine.
Delavirdine The metabolism of Lesinurad can be decreased when combined with Delavirdine.
Miconazole The metabolism of Lesinurad can be decreased when combined with Miconazole.
Gemfibrozil The metabolism of Lesinurad can be decreased when combined with Gemfibrozil.
Sulfaphenazole The metabolism of Lesinurad can be decreased when combined with Sulfaphenazole.
Icosapent Icosapent may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Cefotiam Cefotiam may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Mesalazine Mesalazine may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Cefmenoxime Cefmenoxime may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Cefmetazole Cefmetazole may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Pamidronic acid Pamidronic acid may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Tenofovir disoproxil Tenofovir disoproxil may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Indomethacin Indomethacin may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Cidofovir Cidofovir may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Cefpiramide Cefpiramide may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Ceftazidime Ceftazidime may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Loracarbef Loracarbef may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Cefalotin Cefalotin may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Nabumetone Nabumetone may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Ketorolac Ketorolac may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Tenoxicam Tenoxicam may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Celecoxib Celecoxib may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Cefotaxime Cefotaxime may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Tolmetin Tolmetin may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Foscarnet Foscarnet may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Rofecoxib Rofecoxib may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Piroxicam Piroxicam may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Fenoprofen Fenoprofen may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Valaciclovir Valaciclovir may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Valdecoxib Valdecoxib may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Diclofenac Diclofenac may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Sulindac Sulindac may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Bacitracin Bacitracin may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Amphotericin B Amphotericin B may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Cephaloglycin Cephaloglycin may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Flurbiprofen Flurbiprofen may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Adefovir dipivoxil Adefovir dipivoxil may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Pentamidine Pentamidine may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Etodolac Etodolac may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Mefenamic acid Mefenamic acid may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Acyclovir Acyclovir may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Naproxen Naproxen may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Meloxicam Meloxicam may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Carprofen Carprofen may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Cefaclor Cefaclor may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Diflunisal Diflunisal may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Ceforanide Ceforanide may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Salicylic acid Salicylic acid may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Meclofenamic acid Meclofenamic acid may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Carboplatin Carboplatin may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Oxaprozin Oxaprozin may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Ketoprofen Ketoprofen may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Balsalazide Balsalazide may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Ibuprofen Ibuprofen may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Cefditoren Cefditoren may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Colistimethate Colistimethate may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Cefuroxime Cefuroxime may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Cefapirin Cefapirin may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Cefadroxil Cefadroxil may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Cefprozil Cefprozil may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Ceftriaxone Ceftriaxone may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Olsalazine Olsalazine may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Lumiracoxib Lumiracoxib may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Cefamandole Cefamandole may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Cefazolin Cefazolin may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Cefonicid Cefonicid may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Cefoperazone Cefoperazone may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Cefotetan Cefotetan may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Cefoxitin Cefoxitin may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Ceftizoxime Ceftizoxime may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Cefradine Cefradine may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Magnesium salicylate Magnesium salicylate may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Salsalate Salsalate may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Choline magnesium trisalicylate Choline magnesium trisalicylate may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Cefepime Cefepime may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Cefacetrile Cefacetrile may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Ceftibuten Ceftibuten may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Cefpodoxime Cefpodoxime may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Antrafenine Antrafenine may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Aminophenazone Aminophenazone may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Antipyrine Antipyrine may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Tiaprofenic acid Tiaprofenic acid may decrease the excretion rate of Lesinurad which could result in a higher serum level.
Hydrolyzed Cephalothin Hydrolyzed Cephalothin may decrease the excretion rate of Lesinurad which could result in a higher serum level.

Target Protein

Solute carrier family 22 member 12 SLC22A12
Solute carrier family 22 member 11 SLC22A11

Referensi & Sumber

Artikel (PubMed)
  • PMID: 26861027
    Hoy SM: Lesinurad: First Global Approval. Drugs. 2016 Mar;76(4):509-16. doi: 10.1007/s40265-016-0550-y.

Contoh Produk & Brand

Produk: 9 • International brands: 0
Produk
  • Duzallo
    Tablet, film coated • - • Oral • US • Approved
  • Duzallo
    Tablet, film coated • - • Oral • US • Approved
  • Zurampic
    Tablet, film coated • 200 mg/1 • Oral • US • Approved
  • Zurampic
    Tablet, film coated • 200 mg/1 • Oral • US • Approved
  • Zurampic
    Tablet, film coated • 200 mg • Oral • EU
  • Zurampic
    Tablet, film coated • 200 mg • Oral • EU
  • Zurampic
    Tablet, film coated • 200 mg • Oral • EU
  • Zurampic
    Tablet, film coated • 200 mg • Oral • EU
Menampilkan 8 dari 9 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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