Next Generation Tyrosine Kinase Inhibitor (TKI): Afatinib
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.
Keywords: Afatinib, gilotrif, product patent, polymorph, tyrosine kinase inhibitor, tyrosine phosphorylation inhibitor.
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.
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