Next Generation Tyrosine Kinase Inhibitor (TKI): Afatinib

ISSN: 2212-3970 (Online)
ISSN: 1574-8928 (Print)


Volume 9, 3 Issues, 2014


Download PDF Flyer




Recent Patents on Anti-Cancer Drug Discovery

Aims & ScopeAbstracted/Indexed in

Ranking and Category:
  • 86th of 254 in Pharmacology & Pharmacy
  • 91st of 202 in Oncology

Submit Abstracts Online Submit Manuscripts Online

Editor-in-Chief:
Khurshid Zaman
Bentham Science Publishers
USA


View Full Editorial Board

Subscribe Purchase Articles Order Reprints

Current: 2.863
5 - Year: 2.512

Next Generation Tyrosine Kinase Inhibitor (TKI): Afatinib

Author(s): Suresh Kumar and Ritesh Agrawal

Affiliation: Department of Chemistry, Shrimant Madhavrao Scindia, Government Model Science College, Jhansi Road, Gwalior, Madhya Pradesh, PIN No. 474001, India.

Abstract

Afatinib is a recently introduced new tyrosine kinase inhibitor, approved by the USFDA on July 12, 2013. Afatinib is marketed under the trade name Gilotrif and developed by Boehringer Ingelheim GmbH. It is indicated for the first-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) carrying EGFR exon 19 deletions or exon 21 (L858R) mutations. Afatinib is a covalent, irreversible inhibitor of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2) and HER4. Chemically afatinib is a 4-anilinoquinazoline derivative, having an acrylamide warhead. Gilotrif is the formulation of Afatinib di-meleate salt. Presently, afatinib has been approved in the USA, the European Union, Taiwan and Mexico. In this review, we have summarized the chemical characterization of afatinib, its synthesis, patent status, marketed formulation, available crystalline form and current clinical trials.

Keywords: Afatinib, gilotrif, product patent, polymorph, tyrosine kinase inhibitor, tyrosine phosphorylation inhibitor.

Purchase Online Rights and Permissions

  
  



Article Details

Volume: 9
Issue Number: 3
First Page: 382
Last Page: 393
Page Count: 12
DOI: 10.2174/1574892809666140520114928
Advertisement

Related Journals




Webmaster Contact: urooj@benthamscience.org Copyright © 2014 Bentham Science