Open AccessLesinurad: A significant advancement or just another addition to existing therapies of gout?
Author(s) -
Ajay Gupta,
Pramod Kumar Sharma,
Arup Kumar Misra,
Surjit Singh
Publication year - 2016
Publication title -
journal of pharmacology and pharmacotherapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.301
H-Index - 34
eISSN - 0976-5018
pISSN - 0976-500X
DOI - 10.4103/0976-500x.195897
Subject(s) - gout , probenecid , uric acid , hyperuricemia , biopharmaceutical , medicine , organic anion transporter 1 , pharmacology , xanthine oxidase , clinical trial , transporter , chemistry , biochemistry , microbiology and biotechnology , enzyme , biology , gene
Gout is a metabolic disorder that usually presents as recurrent episodes of acute arthritis due to deposition of crystals in joints and cartilages. Despite the availability of several drugs for gout, its management is still less than adequate. There is always a search for newer, safer, and more potent urate-lowering therapies for treating patients inadequately controlled with available drugs. Lesinurad in combination with a xanthine oxidase inhibitor provides an effective mode of therapy in the management of hyperuricemia associated with gout. Lesinurad is a selective uric acid transporter 1 (URAT1) inhibitor. URAT1 is responsible for the majority of uric acid absorption from kidneys to the circulation. Lesinurad was granted marketing approval based on three randomized, double-blind, placebo-controlled; phase III clinical trials. It is devoid of interaction with organic anion transporters (OATs) such as OAT1 and 3, responsible for drug-drug interactions, an undesirable property associated with probenecid. On-going research is more focused on reducing inflammation consequent to deposition of crystals rather than production and excretion of urate. Various targets are being explored, and interleukin-1 beta inhibition seems to be one of the most promising approaches.