Literature DB >> 29869203

Fostamatinib: First Global Approval.

Anthony Markham1.   

Abstract

Rigel Pharmaceuticals are developing the spleen tyrosine kinase (SYK) inhibitor fostamatinib (TAVALISSE™) as a treatment for immune thrombocytopenia (ITP), autoimmune haemolytic anaemia and IgA nephropathy. Based on positive results in the phase III FIT clinical trial program, the drug was recently approved in the US as a treatment for thrombocytopenia in adult patients with chronic ITP who have had an insufficient response to a previous treatment. This article summarizes the milestones in the development of fostamatinib leading to this first approval.

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Year:  2018        PMID： 29869203     DOI： 10.1007/s40265-018-0927-1

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


  9 in total

1.  R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation.

Authors:  Sylvia Braselmann; Vanessa Taylor; Haoran Zhao; Su Wang; Catherine Sylvain; Muhammad Baluom; Kunbin Qu; Ellen Herlaar; Angela Lau; Chi Young; Brian R Wong; Scott Lovell; Thomas Sun; Gary Park; Ankush Argade; Stipo Jurcevic; Polly Pine; Rajinder Singh; Elliott B Grossbard; Donald G Payan; Esteban S Masuda
Journal:  J Pharmacol Exp Ther       Date:  2006-08-31       Impact factor: 4.030

2.  Effects of Fostamatinib on the Pharmacokinetics of the CYP2C8 Substrate Pioglitazone: Results From In Vitro and Phase 1 Clinical Studies.

Authors:  Paul Martin; Michael Gillen; David Millson; Stuart Oliver; Clive Brealey; Dominic Surry; David Sweeny; David Lau; Philip Leese
Journal:  Clin Pharmacol Drug Dev       Date:  2016-03-23

3.  Pharmacokinetic Properties of Fostamatinib in Patients With Renal or Hepatic Impairment: Results From 2 Phase I Clinical Studies.

Authors:  Paul Martin; Stuart Oliver; Michael Gillen; Thomas Marbury; David Millson
Journal:  Clin Ther       Date:  2015-10-27       Impact factor: 3.393

4.  Effects of Fostamatinib on the Pharmacokinetics of Digoxin (a P-Glycoprotein Substrate): Results From in Vitro and Phase I Clinical Studies.

Authors:  Paul Martin; Michael Gillen; David Millson; Stuart Oliver; Clive Brealey; Robert Elsby; Muhammad Baluom; David Lau; Tim Mant
Journal:  Clin Ther       Date:  2015-10-26       Impact factor: 3.393

5.  Effects of ranitidine (antacid), food, and formulation on the pharmacokinetics of fostamatinib: results from five phase I clinical studies.

Authors:  Talia Flanagan; Paul Martin; Michael Gillen; David Mathews; Eleanor Lisbon; Martin Kruusmägi
Journal:  Eur J Clin Pharmacol       Date:  2016-11-17       Impact factor: 2.953

6.  Of mice and men: an open-label pilot study for treatment of immune thrombocytopenic purpura by an inhibitor of Syk.

Authors:  Anna Podolanczuk; Alan H Lazarus; Andrew R Crow; Elliot Grossbard; James B Bussel
Journal:  Blood       Date:  2008-12-18       Impact factor: 22.113

7.  Effects of Fostamatinib on the Pharmacokinetics of Oral Contraceptive, Warfarin, and the Statins Rosuvastatin and Simvastatin: Results From Phase I Clinical Studies.

Authors:  P Martin; M Gillen; J Ritter; D Mathews; C Brealey; D Surry; S Oliver; V Holmes; P Severin; R Elsby
Journal:  Drugs R D       Date:  2016-03

8.  Effects of CYP3A4 Inhibitors Ketoconazole and Verapamil and the CYP3A4 Inducer Rifampicin on the Pharmacokinetic Parameters of Fostamatinib: Results from In Vitro and Phase I Clinical Studies.

Authors:  Paul Martin; Michael Gillen; David Millson; Stuart Oliver; Clive Brealey; Elliott B Grossbard; Muhammad Baluom; David Lau; David Sweeny; Tim Mant; Kelli Craven
Journal:  Drugs R D       Date:  2016-03

9.  Fostamatinib for the treatment of adult persistent and chronic immune thrombocytopenia: Results of two phase 3, randomized, placebo-controlled trials.

Authors:  James Bussel; Donald M Arnold; Elliot Grossbard; Jiří Mayer; Jacek Treliński; Wojciech Homenda; Andrzej Hellmann; Jerzy Windyga; Liliya Sivcheva; Alhossain A Khalafallah; Francesco Zaja; Nichola Cooper; Vadim Markovtsov; Hany Zayed; Anne-Marie Duliege
Journal:  Am J Hematol       Date:  2018-05-15       Impact factor: 10.047
  9 in total
  20 in total

1.  Discovery of Lanraplenib (GS-9876): A Once-Daily Spleen Tyrosine Kinase Inhibitor for Autoimmune Diseases.

Authors:  Peter Blomgren; Jayaraman Chandrasekhar; Julie A Di Paolo; Wanchi Fung; Guoju Geng; Carmen Ip; Randall Jones; Jeffrey E Kropf; Eric B Lansdon; Seung Lee; Jennifer R Lo; Scott A Mitchell; Bernard Murray; Chris Pohlmeyer; Aaron Schmitt; Kimberly Suekawa-Pirrone; Sarah Wise; Jin-Ming Xiong; Jianjun Xu; Helen Yu; Zhongdong Zhao; Kevin S Currie
Journal:  ACS Med Chem Lett       Date:  2020-02-12       Impact factor: 4.345

2.  Fungal Infections with Ibrutinib and Other Small-Molecule Kinase Inhibitors.

Authors:  Marissa A Zarakas; Jigar V Desai; Georgios Chamilos; Michail S Lionakis
Journal:  Curr Fungal Infect Rep       Date:  2019-07-05

3.  R406 elicits anti-Warburg effect via Syk-dependent and -independent mechanisms to trigger apoptosis in glioma stem cells.

Authors:  Shuxin Sun; Dongdong Xue; Zhijie Chen; Ying Ou-Yang; Ji Zhang; Jialuo Mai; Jiayv Gu; Wanjun Lu; Xincheng Liu; Wenfeng Liu; Longxiang Sheng; Bingzheng Lu; Yuan Lin; Fan Xing; Zhongping Chen; Yonggao Mou; Guangmei Yan; Wenbo Zhu; Ke Sai
Journal:  Cell Death Dis       Date:  2019-05-01       Impact factor: 8.469

4.  SYK Targeting Represents a Potential Therapeutic Option for Relapsed Resistant Pediatric ETV6-RUNX1 B-Acute Lymphoblastic Leukemia Patients.

Authors:  Valentina Serafin; Elena Porcù; Giuliana Cortese; Elena Mariotto; Giulia Veltri; Silvia Bresolin; Giuseppe Basso; Benedetta Accordi
Journal:  Int J Mol Sci       Date:  2019-12-07       Impact factor: 5.923

5.  Comparison of SYK Signaling Networks Reveals the Potential Molecular Determinants of Its Tumor-Promoting and Suppressing Functions.

Authors:  Marion Buffard; Aurélien Naldi; Gilles Freiss; Marcel Deckert; Ovidiu Radulescu; Peter J Coopman; Romain M Larive
Journal:  Biomolecules       Date:  2021-02-18

6.  Identification of four key prognostic genes and three potential drugs in human papillomavirus negative head and neck squamous cell carcinoma.

Authors:  Guocai Tian; You Fu; Dahe Zhang; Jiang Li; Zhiyuan Zhang; Xi Yang
Journal:  Cancer Cell Int       Date:  2021-03-12       Impact factor: 5.722

7.  Drug Repurposing for COVID-19 Treatment by Integrating Network Pharmacology and Transcriptomics.

Authors:  Dan-Yang Liu; Jia-Chen Liu; Shuang Liang; Xiang-He Meng; Jonathan Greenbaum; Hong-Mei Xiao; Li-Jun Tan; Hong-Wen Deng
Journal:  Pharmaceutics       Date:  2021-04-14       Impact factor: 6.321

8.  Cytokine Production and NET Formation by Monosodium Urate-Activated Human Neutrophils Involves Early and Late Events, and Requires Upstream TAK1 and Syk.

Authors:  Olga Tatsiy; Thomas Z Mayer; Vanessa de Carvalho Oliveira; Stéphanie Sylvain-Prévost; Marilyn Isabel; Claire M Dubois; Patrick P McDonald
Journal:  Front Immunol       Date:  2020-01-15       Impact factor: 7.561

Review 9.  Kinase inhibition in autoimmunity and inflammation.

Authors:  Ali A Zarrin; Katherine Bao; Patrick Lupardus; Domagoj Vucic
Journal:  Nat Rev Drug Discov       Date:  2020-10-19       Impact factor: 84.694

10.  Drugs and Epigenetic Molecular Functions. A Pharmacological Data Scientometric Analysis.

Authors:  Dario Kringel; Sebastian Malkusch; Jörn Lötsch
Journal:  Int J Mol Sci       Date:  2021-07-06       Impact factor: 5.923
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