Literature DB >> 26861027

Lesinurad: First Global Approval.

Sheridan M Hoy1.   

Abstract

Lesinurad (ZURAMPIC(®)) is an oral urate-anion exchanger transporter 1 (URAT1) inhibitor developed by Ardea Biosciences (a subsidiary of AstraZeneca) for the treatment of hyperuricaemia associated with gout. It reduces serum uric acid (sUA) levels by inhibiting the function of the transporter proteins (URAT1 and organic anion transporter 4) involved in uric acid reabsorption in the kidney. In December 2015, lesinurad was approved in the USA as combination therapy with a xanthine oxidase inhibitor for the treatment of hyperuricaemia associated with gout in patients who have not achieved sUA target levels with a xanthine oxidase inhibitor alone. Lesinurad has also received a positive opinion from the European Medicines Agency's Committee for Medicinal Products for Human Use for this indication and is in phase III development as a combination therapy in several other countries. This article summarizes the milestones in the development of lesinurad leading to this first approval for hyperuricaemia associated with gout.

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Year:  2016        PMID: 26861027     DOI: 10.1007/s40265-016-0550-y

Source DB:  PubMed          Journal:  Drugs        ISSN: 0012-6667            Impact factor:   9.546


  3 in total

Review 1.  Gout.

Authors:  Edward Roddy; Christian D Mallen; Michael Doherty
Journal:  BMJ       Date:  2013-10-01

Review 2.  Gout therapeutics: new drugs for an old disease.

Authors:  Christopher M Burns; Robert L Wortmann
Journal:  Lancet       Date:  2010-08-16       Impact factor: 79.321

3.  Lesinurad in combination with allopurinol: results of a phase 2, randomised, double-blind study in patients with gout with an inadequate response to allopurinol.

Authors:  Fernando Perez-Ruiz; John S Sundy; Jeffrey N Miner; Matthew Cravets; Chris Storgard
Journal:  Ann Rheum Dis       Date:  2016-01-07       Impact factor: 19.103

  3 in total
  10 in total

Review 1.  Application of triazoles as bioisosteres and linkers in the development of microtubule targeting agents.

Authors:  M Shaheer Malik; Saleh A Ahmed; Ismail I Althagafi; Mohammed Azam Ansari; Ahmed Kamal
Journal:  RSC Med Chem       Date:  2020-01-29

2.  Systematic Structure-Activity Relationship (SAR) Exploration of Diarylmethane Backbone and Discovery of A Highly Potent Novel Uric Acid Transporter 1 (URAT1) Inhibitor.

Authors:  Wenqing Cai; Jingwei Wu; Wei Liu; Yafei Xie; Yuqiang Liu; Shuo Zhang; Weiren Xu; Lida Tang; Jianwu Wang; Guilong Zhao
Journal:  Molecules       Date:  2018-01-27       Impact factor: 4.411

Review 3.  Reverse Translational Research of ABCG2 (BCRP) in Human Disease and Drug Response.

Authors:  Deanna J Brackman; Kathleen M Giacomini
Journal:  Clin Pharmacol Ther       Date:  2017-11-28       Impact factor: 6.875

4.  Lesinurad, a novel, oral compound for gout, acts to decrease serum uric acid through inhibition of urate transporters in the kidney.

Authors:  Jeffrey N Miner; Philip K Tan; David Hyndman; Sha Liu; Cory Iverson; Payal Nanavati; David T Hagerty; Kimberly Manhard; Zancong Shen; Jean-Luc Girardet; Li-Tain Yeh; Robert Terkeltaub; Barry Quart
Journal:  Arthritis Res Ther       Date:  2016-10-03       Impact factor: 5.156

5.  Determination of lesinurad in rat plasma by a UHPLC-MS/MS assay.

Authors:  Xiao-Yang Zhou; Ling-Jing Yuan; Zhe Chen; Peng-Fei Tang; Xiang-Yu Li; Guo-Xin Hu; Jian-Ping Cai
Journal:  Chem Cent J       Date:  2017-11-28       Impact factor: 4.215

6.  Discovery and characterization of verinurad, a potent and specific inhibitor of URAT1 for the treatment of hyperuricemia and gout.

Authors:  Philip K Tan; Sha Liu; Esmir Gunic; Jeffrey N Miner
Journal:  Sci Rep       Date:  2017-04-06       Impact factor: 4.379

7.  Individualized treatment strategies for hyperuricemia informed by a semi-mechanistic exposure-response model of uric acid dynamics.

Authors:  Sergey Aksenov; Carl C Peck; Ulf G Eriksson; Donald R Stanski
Journal:  Physiol Rep       Date:  2018-03

8.  Lesinurad: what the nephrologist should know.

Authors:  Maria Dolores Sanchez-Niño; Binbin Zheng-Lin; Lara Valiño-Rivas; Ana Belen Sanz; Adrian Mario Ramos; Jose Luño; Marian Goicoechea; Alberto Ortiz
Journal:  Clin Kidney J       Date:  2017-05-26

Review 9.  Physiology of Hyperuricemia and Urate-Lowering Treatments.

Authors:  Caroline L Benn; Pinky Dua; Rachel Gurrell; Peter Loudon; Andrew Pike; R Ian Storer; Ciara Vangjeli
Journal:  Front Med (Lausanne)       Date:  2018-05-31

10.  Impact of Lesinurad and allopurinol on experimental Hyperuricemia in mice: biochemical, molecular and Immunohistochemical study.

Authors:  Youssef Saeed Alghamdi; Mohamed Mohamed Soliman; Mohamed Abdo Nassan
Journal:  BMC Pharmacol Toxicol       Date:  2020-02-10       Impact factor: 2.483

  10 in total

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