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.
Recent Patents on Anti-Cancer Drug Discovery
Title:Next Generation Tyrosine Kinase Inhibitor (TKI): Afatinib
Volume: 9 Issue: 3
Author(s): Suresh Kumar and Ritesh Agrawal
Affiliation:
Keywords: Afatinib, gilotrif, product patent, polymorph, tyrosine kinase inhibitor, tyrosine phosphorylation inhibitor.
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.
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Kumar Suresh and Agrawal Ritesh, Next Generation Tyrosine Kinase Inhibitor (TKI): Afatinib, Recent Patents on Anti-Cancer Drug Discovery 2014; 9 (3) . https://dx.doi.org/10.2174/1574892809666140520114928
DOI https://dx.doi.org/10.2174/1574892809666140520114928 |
Print ISSN 1574-8928 |
Publisher Name Bentham Science Publisher |
Online ISSN 2212-3970 |
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