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Literature DB >> 31571162

Fedratinib: First Approval.

Abstract

Fedratinib (INREBIC®) is a JAK2-selective inhibitor that has been developed as an oral treatment for myelofibrosis. In August 2019, fedratinib received its first global approval in the USA for the treatment of adult patients with intermediate-2 or high-risk primary or secondary (post-polycythemia vera or post-essential thrombocythemia) myelofibrosis. Phase III clinical development for myelofibrosis is ongoing worldwide. This article summarizes the milestones in the development of fedratinib leading to this first approval for myelofibrosis.

Entities: Chemical

Mesh：

Substances：

Year: 2019 PMID： 31571162 DOI： 10.1007/s40265-019-01205-x

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

13 in total

1. Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera.

Authors: Gerlinde Wernig; Michael G Kharas; Rachel Okabe; Sandra A Moore; Dena S Leeman; Dana E Cullen; Maricel Gozo; Elizabeth P McDowell; Ross L Levine; John Doukas; Chi Ching Mak; Glenn Noronha; Michael Martin; Yon D Ko; Benjamin H Lee; Richard M Soll; Ayalew Tefferi; John D Hood; D Gary Gilliland
Journal: Cancer Cell Date: 2008-04 Impact factor: 31.743

2. Safety and efficacy of TG101348, a selective JAK2 inhibitor, in myelofibrosis.

Authors: Animesh Pardanani; Jason R Gotlib; Catriona Jamieson; Jorge E Cortes; Moshe Talpaz; Richard M Stone; Michael H Silverman; D Gary Gilliland; Jolene Shorr; Ayalew Tefferi
Journal: J Clin Oncol Date: 2011-01-10 Impact factor: 44.544

Review 3. JAK inhibitor therapy for myelofibrosis: critical assessment of value and limitations.

Authors: A Pardanani; A M Vannucchi; F Passamonti; F Cervantes; T Barbui; A Tefferi
Journal: Leukemia Date: 2010-11-16 Impact factor: 11.528

4. JAK inhibition induces silencing of T Helper cytokine secretion and a profound reduction in T regulatory cells.

Authors: Clodagh Keohane; Shahram Kordasti; Thomas Seidl; Pilar Perez Abellan; Nicholas S B Thomas; Claire N Harrison; Donal P McLornan; Ghulam J Mufti
Journal: Br J Haematol Date: 2015-06-15 Impact factor: 6.998

5. Specificity and mechanism-of-action of the JAK2 tyrosine kinase inhibitors ruxolitinib and SAR302503 (TG101348).

Authors: T Zhou; S Georgeon; R Moser; D J Moore; A Caflisch; O Hantschel
Journal: Leukemia Date: 2013-07-04 Impact factor: 11.528

6. The Janus kinase 2 inhibitor fedratinib inhibits thiamine uptake: a putative mechanism for the onset of Wernicke's encephalopathy.

Authors: Qiang Zhang; Yan Zhang; Sharon Diamond; Jason Boer; Jennifer J Harris; Yu Li; Mark Rupar; Elham Behshad; Christine Gardiner; Paul Collier; Phillip Liu; Timothy Burn; Richard Wynn; Gregory Hollis; Swamy Yeleswaram
Journal: Drug Metab Dispos Date: 2014-07-25 Impact factor: 3.922

7. High concordance in grading reticulin fibrosis and cellularity in patients with myeloproliferative neoplasms.

Authors: Olga Pozdnyakova; Kaida Wu; Abhay Patki; Scott J Rodig; Juergen Thiele; Robert P Hasserjian
Journal: Mod Pathol Date: 2014-04-25 Impact factor: 7.842

8. A randomized, placebo-controlled study of the pharmacokinetics, pharmacodynamics, and tolerability of the oral JAK2 inhibitor fedratinib (SAR302503) in healthy volunteers.

Authors: Meng Zhang; Christine R Xu; Elias Shamiyeh; Feng Liu; Jian Y Yin; Lisa L von Moltke; William B Smith
Journal: J Clin Pharmacol Date: 2013-11-16 Impact factor: 3.126

9. Effect of food on the bioavailability and tolerability of the JAK2-selective inhibitor fedratinib (SAR302503): Results from two phase I studies in healthy volunteers.

Authors: Meng Zhang; Christine Xu; Lei Ma; Elias Shamiyeh; Jianyun Yin; Lisa L von Moltke; William B Smith
Journal: Clin Pharmacol Drug Dev Date: 2014-10-27

10. A phase 2 randomized dose-ranging study of the JAK2-selective inhibitor fedratinib (SAR302503) in patients with myelofibrosis.

Authors: A Pardanani; A Tefferi; C Jamieson; N Y Gabrail; C Lebedinsky; G Gao; F Liu; C Xu; H Cao; M Talpaz
Journal: Blood Cancer J Date: 2015-08-07 Impact factor: 11.037

14 in total

1. Conversion of a False Virtual Screen Hit into Selective JAK2 JH2 Domain Binders Using Convergent Design Strategies.

Authors: Sean P Henry; Maria-Elena Liosi; Joseph A Ippolito; Kara J Cutrona; Stefan G Krimmer; Ana S Newton; Joseph Schlessinger; William L Jorgensen
Journal: ACS Med Chem Lett Date: 2022-04-21 Impact factor: 4.632

2. Fedratinib in myelofibrosis.

Authors: Ann Mullally; John Hood; Claire Harrison; Ruben Mesa
Journal: Blood Adv Date: 2020-04-28

Review 3. Baricitinib: From Rheumatoid Arthritis to COVID-19.

Authors: Sara Assadiasl; Yousef Fatahi; Banafsheh Mosharmovahed; Bahareh Mohebbi; Mohammad Hossein Nicknam
Journal: J Clin Pharmacol Date: 2021-06-12 Impact factor: 2.860

Review 4. Inside Perspective of the Synthetic and Computational Toolbox of JAK Inhibitors: Recent Updates.

Authors: Adriana Coricello; Francesco Mesiti; Antonio Lupia; Annalisa Maruca; Stefano Alcaro
Journal: Molecules Date: 2020-07-22 Impact factor: 4.411

5. Bioinformatics Data Mining Repurposes the JAK2 (Janus Kinase 2) Inhibitor Fedratinib for Treating Pancreatic Ductal Adenocarcinoma by Reversing the KRAS (Kirsten Rat Sarcoma 2 Viral Oncogene Homolog)-Driven Gene Signature.

Authors: Li-Wei Liu; Yao-Yu Hsieh; Pei-Ming Yang
Journal: J Pers Med Date: 2020-09-16

Review 6. Metabolic Vulnerabilities and Epigenetic Dysregulation in Myeloproliferative Neoplasms.

Authors: Vasundhara Sharma; Kenneth L Wright; Pearlie K Epling-Burnette; Gary W Reuther
Journal: Front Immunol Date: 2020-11-30 Impact factor: 7.561

Review 7. FDA-Approved Drugs for Hematological Malignancies-The Last Decade Review.

Authors: Aleksandra Sochacka-Ćwikła; Marcin Mączyński; Andrzej Regiec
Journal: Cancers (Basel) Date: 2021-12-24 Impact factor: 6.639

8. Blocking the JAK2/STAT3 and ERK pathways suppresses the proliferation of gastrointestinal cancers by inducing apoptosis.

Authors: Xi Wang; Chunyan Dai; Yifei Yin; Lin Wu; Weiyang Jin; Yufei Fu; Zhe Chen; Ke Hao; Bin Lu
Journal: J Zhejiang Univ Sci B Date: 2021-06-15 Impact factor: 3.066

Review 9. Downfalls of Chemical Probes Acting at the Kinase ATP-Site: CK2 as a Case Study.

Authors: Eleanor L Atkinson; Jessica Iegre; Paul D Brear; Elizabeth A Zhabina; Marko Hyvönen; David R Spring
Journal: Molecules Date: 2021-03-31 Impact factor: 4.411

Review 10. Restoring the Balance between Pro-Inflammatory and Anti-Inflammatory Cytokines in the Treatment of Rheumatoid Arthritis: New Insights from Animal Models.

Authors: Adrienn Markovics; Ken S Rosenthal; Katalin Mikecz; Roy E Carambula; Jason C Ciemielewski; Daniel H Zimmerman
Journal: Biomedicines Date: 2021-12-26