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Drugs & Therapy Perspectives

, Volume 34, Issue 10, pp 451–456 | Cite as

Fostamatinib in chronic immune thrombocytopenia: a profile of its use in the USA

  • Kate McKeage
  • Katherine A. Lyseng-Williamson
Adis Drug Q&A
  • 14 Downloads

Abstract

Oral fostamatinib is an orally administered small molecule spleen tyrosine kinase (SYK) inhibitor approved for the treatment of adults with chronic immune thrombocytopenia (ITP) who have an inadequate response to a previous treatment. Fostamatinib has a unique mechanism of action, whereby its active metabolite targets the SYK-mediated pathway of platelet destruction. In clinical trials, fostamatinib provided durable responses in adults with chronic ITP who had not responded or had relapsed following treatment with one or more prior ITP therapies, including corticosteroids, thrombopoietin receptor agonists, rituximab, and/or splenectomy. Most patients who respond to fostamatinib maintain platelet counts of > 50 × 109/L for periods of ≥ 12 months. The most common adverse events reported with fostamatinib in clinical trials were diarrhea, hypertension, nausea, and increased transaminase levels.

Notes

Acknowledgements

The manuscript was reviewed by: W. Homenda, Wojewódzki Szpital Specjalistyczny im. J. Korczaka i Akademia Pomorska w Słupsku, Slupsk, Poland; A. A. Khalafallah, Menzies Institute for Medical Research and Faculty of Health Sciences, University of Tasmania, Launceston, TAS, Australia. During the peer review process, Rigel Pharmaceuticals Inc., the marketing-authorization holder of fostamatinib, was also offered an opportunity to provide a scientific accuracy review of their data. Changes resulting from comments received were made on the basis of scientific and editorial merit.

Compliance with ethical standards

Funding

The preparation of this review was not supported by any external funding.

Conflict of interest

K. McKeage and K.A. Lyseng-Williamson are employees of Adis/Springer, are responsible for the article content and declare no conflicts of interest.

References

  1. 1.
    Niscola P, Scaramucci L, Giovannini M. Spleen tyrosine kinase inhibition: a new promising approach to chronic and refractory immune thrombocytopenia. Immunotherapy. 2018;10(1):5–7.CrossRefPubMedCentralGoogle Scholar
  2. 2.
    Zufferey A, Kapur R, Semple JW. Pathogenesis and therapeutic mechanisms in immune thrombocytopenia (ITP). J Clin Med. 2017;6(2):16.CrossRefGoogle Scholar
  3. 3.
    Cines DB, Bussel JB, Liebman HA, et al. The ITP syndrome: pathogenic and clinical diversity. Blood. 2009;113(26):6511–21.CrossRefPubMedCentralGoogle Scholar
  4. 4.
    Kistangari G, McCrae KR. Immune thrombocytopenia. Hematol Oncol Clin N Am. 2013;27(3):495–520.CrossRefGoogle Scholar
  5. 5.
    Terrell DR, Beebe LA, Vesely SK, et al. The incidence of immune thrombocytopenic purpura in children and adults: a critical review of published reports. Am J Hematol. 2010;85(3):174–80.Google Scholar
  6. 6.
    Braselmann S, Taylor V, Zhao H, et al. R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation. J Pharmacol Exp Ther. 2006;319(3):998–1008.CrossRefPubMedCentralGoogle Scholar
  7. 7.
    Baluom M, Grossbard EB, Mant T, et al. Pharmacokinetics of fostamatinib, a spleen tyrosine kinase (SYK) inhibitor, in healthy human subjects following single and multiple oral dosing in three phase I studies. Br J Clin Pharmacol. 2013;76(1):78–88.CrossRefPubMedCentralGoogle Scholar
  8. 8.
    Tavalisse™ (fostamatinib disodium hexahydrate): US prescribing information. South San Francisco: Rigel Pharmaceuticals Inc. 2018.Google Scholar
  9. 9.
    Martin P, Oliver S, Gillen M, et al. Pharmacokinetic properties of fostamatinib in patients with renal or hepatic impairment: results from 2 phase I clinical studies. Clin Ther. 2015;37(12):2823–36.CrossRefPubMedCentralGoogle Scholar
  10. 10.
    Bussel J, Arnold DM, Grossbard E, et al. Fostamatinib for the treatment of adult persistent and chronic immune thrombocytopenia: results of two phase 3, randomized, placebo-controlled trials. Am J Hematol. 2018;93(7):921–30.CrossRefPubMedCentralGoogle Scholar
  11. 11.
    Bussel JB, Arnold DM, Cooper N, et al. Long-term maintenance of platelet responses in adult patients with persistent/chronic immune thrombocytopenia treated with fostamatinib: 1-year efficacy and safety results [abstract]. Blood. 2017;130(Suppl 1):16.Google Scholar
  12. 12.
    Skinner M, Philp K, Lengel D, et al. The contribution of VEGF signalling to fostamatinib-induced blood pressure elevation. Br J Pharmacol. 2014;171(9):2308–20.CrossRefPubMedCentralGoogle Scholar

Copyright information

© Springer Nature Switzerland AG 2018

Authors and Affiliations

  1. 1.SpringerAucklandNew Zealand

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