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 |
Call for Papers in Thematic Issues
Novel anti-cancer drugs in photoimmunotherapy management: from bench to translational research
In recent years, traditional cancer treatments, such as surgery, chemotherapy, and radiation treatment, etc., may damage the pathological tissue and normal cells. The ideal tumor treatment should be noninvasive, eliminating the primary tumor, making the body produce systemic tumor-specific immunity, eliminating metastases, and having less /no side effects. Recent Patents ...read more
- 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
-
The Combination of the CIGB-300 Anticancer Peptide and Cisplatin Modulates Proteins Related to Cell Survival, DNA Repair and Metastasis in a Lung Cancer Cell Line Model
Current Proteomics Nanoparticle-Based Drugs: A Potential Armamentarium of Effective Anti-Cancer Therapies
Current Drug Metabolism Clinical Importance of Assessment of Type 2 Diabetes Mellitus with Visceral Obesity. A Japanese Perspective
Current Diabetes Reviews Pharmacogenomics of Nicotine Dependence and Impact on Smoking Cessation
Current Pharmacogenomics Rheumatoid Nodules and Lung
Current Respiratory Medicine Reviews Synthesis, Cytotoxic Evaluation, and Molecular Docking Studies of New Oxadiazole Analogues
Letters in Organic Chemistry Impact of Renin-Angiotensin System in Hepatocellular Carcinoma
Current Cancer Drug Targets Destabilizing Aneuploidy by Targeting Cell Cycle and Mitotic Checkpoint Proteins in Cancer Cells
Current Drug Targets Inhaled Dry Powder Formulations for Treating Tuberculosis
Current Drug Delivery Biomarkers Linking PCB Exposure and Obesity
Current Pharmaceutical Biotechnology Cabozantinib in Thyroid Cancer
Recent Patents on Anti-Cancer Drug Discovery Triterpene Derivatives as Inhibitors of Protein Involved in the Inflammatory Process: Molecules Interfering with Phospholipase A2, Cycloxygenase, and Lipoxygenase
Current Drug Targets Recent Advances of Small Molecule Focal Adhesion Kinase (FAK) Inhibitors as Promising Anticancer Therapeutics
Current Medicinal Chemistry Novel Implications for Lysophospholipids, Lysophosphatidic Acid and Sphingosine 1-Phosphate, as Drug Targets in Cancer
Anti-Cancer Agents in Medicinal Chemistry The Current Status of Novel PET Radio-Pharmaceuticals in Radiotherapy Treatment Planning of Glioma
Current Pharmaceutical Biotechnology The Application of Fungal Beta-glucans for the Treatment of Colon Cancer
Anti-Cancer Agents in Medicinal Chemistry Deep Learning in the Quest for Compound Nomination for Fighting COVID-19
Current Medicinal Chemistry DNA Fragmentation, Cell Cycle Arrest, and Docking Study of Novel Bis Spiro-cyclic 2-oxindole of Pyrimido[4,5-b]quinoline-4,6-dione Derivatives Against Breast Carcinoma
Current Cancer Drug Targets STAT3: A Potential Drug Target for Tumor and Inflammation
Current Topics in Medicinal Chemistry Development of Specific New ELISA for Bioanalysis of Cetuximab: A Monoclonal Antibody Used for Cancer Immunotherapy
Current Pharmaceutical Analysis