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.
Export Options
About this article
Cite this article as:
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 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
ERGIC3 Silencing Additively Enhances the Growth Inhibition of BFA on Lung Adenocarcinoma Cells
Current Cancer Drug Targets The Roles of Chromatin Remodeling Proteins in Cancer
Current Protein & Peptide Science Withdrawal Notice: Therapeutic Effect of Prdx1 on NAFLD Mice May be Related to the Activation of Nrf-2/HO-1 Pathway
Current Pharmaceutical Design SUBJECT INDEX TO VOLUME 1
Current Genomics Editorial (Mini Thematic Issue: Immunotherapy – A Pivotal Mechanism in the Fight of Cancer)
Reviews on Recent Clinical Trials Microsomal Prostaglandin E Synthase: A Key Enzyme in PGE2 Biosynthesis and Inflammation
Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents Real-Time PCR: Revolutionizing Detection and Expression Analysis of Genes
Current Genomics Volatile Organic Compounds Trapping from Gaseous Samples on the Basis of Co-Liquefaction with Organic Solvent for Gas Chromatographic Analysis
Current Analytical Chemistry The Anti-Cancer Activity of Noscapine: A Review
Recent Patents on Anti-Cancer Drug Discovery Recent Advances in PET Imaging for Skeletal Surgery Applications
Recent Patents on Medical Imaging Technology Whitespaces India Should Focus: A Comparative Anti-Cancer Patent Rational Analysis of Indian and International Public Funded Universities
Recent Patents on Anti-Cancer Drug Discovery Vitamin D Analogs- Drug Design Based on Proteins Involved in Vitamin D Signal Transduction
Current Drug Targets - Immune, Endocrine & Metabolic Disorders Targeting IAPs as An Approach to Anti-Cancer Therapy
Current Topics in Medicinal Chemistry Strategies Targeting DNA Topoisomerase I in Cancer Chemotherapy: Camptothecins, Nanocarriers for Camptothecins, Organic Non-Camptothecin Compounds and Metal Complexes
Current Drug Targets Recent Studies and Biological Aspects of Substantial Indole Derivatives with Anti-cancer Activity
Current Organic Chemistry Editorial (Thematic Issue: Antiangiogenic Agents in the Management of Solid Malignancies)
Current Angiogenesis (Discontinued) Prophylaxis of Cancer
Current Cancer Therapy Reviews Potential Non-coding RNAs from Microorganisms and their Therapeutic Use in the Treatment of Different Human Cancers
Current Gene Therapy NKT Cell Subsets Can Exert Opposing Effects in Autoimmunity, Tumor Surveillance and Inflammation
Current Immunology Reviews (Discontinued) Recent Development in [1,4]Benzodiazepines as Potent Anticancer Agents: A Review
Mini-Reviews in Medicinal Chemistry