Skip to main content
SpringerLink
Log in

Lesinurad: First Global Approval

  • AdisInsight Report
  • Published:
Drugs Aims and scope Submit manuscript

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.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Similar content being viewed by others

References

  1. Roddy E, Mallen CD, Doherty M. Gout. BMJ. 2013;347:f5648.

    Article  PubMed  Google Scholar 

  2. Burns CM, Wortmann RL. Gout therapeutics: new drugs for an old disease. Lancet. 2011;377(9760):165–77.

    Article  CAS  PubMed  Google Scholar 

  3. AstraZeneca AB. ZURAMPIC® (lesinurad) tablets, for oral use: US prescribing information. 2015. http://www.fda.gov/. Accessed 5 Jan 2016.

  4. Gliozzi M, Malara N, Muscoli S, et al. The treatment of hyperuricemia. Int J Cardiol. 2015. doi:10.1016/j.ijcard.2015.08.087.

    Google Scholar 

  5. Ardea Biosciences Inc. Ardea Biosciences announces expiration of HSR waiting period in connection with proposed merger. 2012. http://www.ardeabio.com/. Accessed 11 Jan 2016.

  6. US Food and Drug Administration. FDA approves Zurampic to treat high blood uric acid levels associated with gout. 2015. http://www.fda.gov/. Accessed 11 Jan 2016.

  7. European Medicines Agency. Zurampic (lesinurad): summary of opinion. 2015. http://www.ema.europa.eu. Accessed 21 Dec 2015.

  8. Yeh L, Shen Z, Kerr B, et al. RDEA594: a potent URAT1 inhibitor without affecting other important renal transporters, OAT1 and OAT3 [abstract no. THU0452]. Ann Rheum Dis. 2009;68(Suppl 3):320.

    Google Scholar 

  9. Terkeltaub R, Perez-Ruiz F, Kopicko J, et al. The safety and efficacy of lower serum urate levels: a pooled analysis of gout subjects receiving lesinurad and xanthine oxidase inhibitors [abstract no. 2354]. Arthritis Rheumatol. 2015;67(Suppl 10):2839–40.

  10. Terkeltaub R, Perez-Ruiz F, Storgard C, et al. Relationship between sustained lowering of serum urate levels and improvements in gout flares and tophus area: pooled exploratory analysis of gout subjects receiving lesinurad and xanthine oxidase inhibitor combination therapy [abstract no. SAT0313]. Ann Rheum Dis. 2015;74(Suppl 2):771–2.

    Article  Google Scholar 

  11. Yeh LT, Shen Z, Kerr B, et al. No clinically meaningful drug interactions expected between lesinurad, a novel oral uricosuric agent, and drugs most commonly used by gout patients [abstract no. AB1064]. Ann Rheum Dis. 2012;71(Suppl 3):699.

  12. Tausche AK, Alten R, Dalbeth N, et al. Lesinurad monotherapy in gout patients intolerant to xanthine oxidase inhibitors (LIGHT): a randomized, double-blind, placebo-controlled, 6-month phase III clinical trial [abstract no. SAT0307]. Ann Rheum Dis. 2015;74(Suppl 2):769.

    Article  Google Scholar 

  13. Saag K, Fitz-Patrick D, Kopicko J, et al. Lesinurad, a selective uric acid reabsorption inhibitor, in combination with allopurinol: results from a phase III study in gout patients having an inadequate response to standard of care (CLEAR 1) [abstract no. FRI0320]. Ann Rheum Dis. 2015;74(Suppl 2):540.

    Google Scholar 

  14. Bardin T, Keenan R, Khanna P, et al. Lesinurad, a selective uric acid reabsorption inhibitor, in combination with allopurinol: results from a phase III study in gout patients having an inadequate response to standard of care (CLEAR 2) [abstract no. FRI0333]. Ann Rheum Dis. 2015;74(Suppl 2):545.

    Article  Google Scholar 

  15. Saag KG, Bardin T, So A, et al. Analysis of gout subjects receiving lesinurad and allopurinol combination therapy by baseline renal function [abstract no. 2112]. Arthritis Rheumatol. 2015;67(Suppl 10):2524–5.

  16. Perez-Ruiz F, Sundy JS, Miner JN, et al. Lesinurad in combination with allopurinol: results of a phase 2, randomised, double-blind study in patients with gout with an inadequate response to allopurinol. Ann Rheum Dis. 2016. doi:10.1136/annrheumdis-2015-207919.

    Google Scholar 

  17. Perez-Ruiz F, Sundy J, Krishnan E, et al. Efficacy and safety of lesinurad (RDEA594), a novel URAT1 inhibitor, in combination with allopurinol in allopurinol-refractory gout patients: results from a randomized, blinded, placebo-controlled, phase 2b extension study [abstract no. FRI0370]. Ann Rheum Dis. 2012;71(Suppl 3):439.

  18. Dalbeth N, Jones G, Terkeltaub R, et al. Lesinurad, a novel selective uric acid reabsorption inhibitor, in combination with febuxostat, in patients with tophaceous gout: the CRYSTAL phase III clinical trial [abstract no. SAT0329]. Ann Rheum Dis. 2015;74(Suppl 2):778.

    Google Scholar 

  19. Dalbeth N, Jones G, Terkeltaub R, et al. Lesinurad and febuxostat combination therapy: analysis of treatment based on patient baseline renal function [abstract no. 2353]. Arthritis Rheumatol. 2015;67(Suppl 10):2837–9.

  20. Ardea Biosciences Inc. Lesinurad in combination with a xanthine oxidase inhibitor for treatment of hyperuricemia associated with gout: briefing document for the arthritis advisory committee. 2015. http://www.fda.gov/. Accessed 3 Feb 2016.

  21. Dalbeth N, Jones G, Terkeltaub R, et al. Efficacy and safety in patients with tophaceous gout receiving lesinurad and febuxostat combination therapy: interim analysis of an extension study [abstract no. 2352]. Arthritis Rheumatoly. 2015;67(Suppl 10):2836–7.

Download references

Disclosure

The preparation of this review was not supported by any external funding. During the peer review process the manufacturer of the agent under review was offered an opportunity to comment on the article. Changes resulting from any comments received were made by the author on the basis of scientific completeness and accuracy. S. M. Hoy is a salaried employee of Adis, Springer SBM.

Author information

Authors and Affiliations

  1. Springer, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand

    Sheridan M. Hoy

Authors
  1. Sheridan M. Hoy
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Sheridan M. Hoy.

Additional information

This profile has been extracted and modified from the AdisInsight database. AdisInsight tracks drug development worldwide through the entire development process, from discovery, through pre-clinical and clinical studies to market launch and beyond.

Rights and permissions

Reprints and permissions

About this article

Check for updates. Verify currency and authenticity via CrossMark

Cite this article

Hoy, S.M. Lesinurad: First Global Approval. Drugs 76, 509–516 (2016). https://doi.org/10.1007/s40265-016-0550-y

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s40265-016-0550-y

Keywords

Search

Navigation