[New antihyperuricemic medicine: febuxostat, Puricase, etc].
An inhibitor of xanthine dehydrogenase (XDH), allopurinol, and uricosuric agents, probenecid and benzbromarone, have been used for more than 20 years in the treatment of hyperuricemia and gout. However, they are inconvenient in some situations. With regard to allopurinol, the dosage reduction is recommended in patients with renal insufficiency for preventing from rare adverse effect, bone marrow depression. Benzbromarone also has quite rare adverse effect, fulminant hepatitis. Recently several new therapies have been developed such as new XDH inhibitors urate transporter (URAT) 1 inhibitor, and a modified recombinant uricase. The dosage reduction of the new XDH inhibitors, febuxostat and FYX-051, is not necessary in patients with renal insufficiency because renal excretion is not main excretory pathway. JTT-552 is a first medicine targeting on URAT1. Polyethylene glycol (PEG) conjugation with recombinant uricase sufficiently reduces the immunogenicity to permit repeated dosing and the clinical trials are ongoing for patients with treatment-failure gout and hyperuricemia.
Ichida
Kimiyoshi
K
Department of Pathophysiology, Tokyo University of Pharmacy and Life Sciences.
D000818:Animals; D002986:Clinical Trials as Topic; D015195:Drug Design; D000069465:Febuxostat; D006074:Gout Suppressants / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D009570:Nitriles; D027361:Organic Anion Transporters / Q000037:antagonists & inhibitors; D027701:Organic Cation Transport Proteins / Q000037:antagonists & inhibitors; D011092:Polyethylene Glycols; D011725:Pyridines; D013844:Thiazoles; D014503:Urate Oxidase; D014968:Xanthine Dehydrogenase / Q000037:antagonists & inhibitors
D006074:Gout Suppressants; D009570:Nitriles; D027361:Organic Anion Transporters; D027701:Organic Cation Transport Proteins; D011725:Pyridines; C491241:SLC22A12 protein, human; D013844:Thiazoles; C504882:FYX-051; D000069465:Febuxostat; D011092:Polyethylene Glycols; D014968:Xanthine Dehydrogenase; D014503:Urate Oxidase; C031545:Pegloticase