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
-
Modulation of GSTP1-1 Oligomerization by Electrophilic Inflammatory Mediators and Reactive Drugs
Inflammation & Allergy - Drug Targets (Discontinued) Recent Advances in Multinuclear Complexes as Potential Anticancer and DNA Binding Agents
Anti-Cancer Agents in Medicinal Chemistry Impact of Splicing Factor Mutations on Pre-mRNA Splicing in the Myelodysplastic Syndromes
Current Pharmaceutical Design Benzamide Riboside, a Recent Inhibitor of Inosine 5-Monophosphate Dehydrogenase Induces Transferrin Receptors in Cancer Cells
Current Medicinal Chemistry uPAR as Anti-Cancer Target: Evaluation of Biomarker Potential, Histological Localization, and Antibody-Based Therapy
Current Drug Targets Damage and Recovery of the Bone Marrow Microenvironment Induced by Cancer Chemotherapy – Potential Regulatory Role of Chemokine CXCL12/Receptor CXCR4 Signalling
Current Molecular Medicine Natural Products Chemistry in Marine Ascidians of the Genus Aplidium
Mini-Reviews in Organic Chemistry Emerging Targeted Therapies for Pediatric Acute Myeloid Leukemia
Recent Patents on Anti-Cancer Drug Discovery Resveratrol, a Phytochemical Inducer of Multiple Cell Death Pathways: Apoptosis, Autophagy and Mitotic Catastrophe
Current Medicinal Chemistry The gp130 Receptor Cytokine Family: Regulators of Adipocyte Development and Function
Current Pharmaceutical Design Hypoxia-Inducible Factor (HIF): Fuel for Cancer Progression
Current Molecular Pharmacology Estrogen Receptors as Therapeutic Targets in Breast Cancer
Current Topics in Medicinal Chemistry Tolfenamic Acid Interrupts the De Novo Synthesis of the β-Amyloid Precursor Protein and Lowers Amyloid Beta Via a Transcriptional Pathway
Current Alzheimer Research Immunotherapy for Myeloproliferative Neoplasms (MPN)
Current Cancer Drug Targets Multidrug Resistance: Retrospect and Prospects in Anti-Cancer Drug Treatment
Current Medicinal Chemistry Epigenetically Active Drugs Inhibiting DNA Methylation and Histone Deacetylation
Current Pharmaceutical Design Quantization of Angiogenesis and Image Analysis
Current Angiogenesis (Discontinued) Prevention and Therapy of Prostate Cancer: An Update on Alternatives for Treatment and Future Perspectives
Current Drug Therapy Role of NF-κB and NF-κB-regulated Gene Products in Chemoresistance and Radioresistance
Current Cancer Therapy Reviews Phytochemical Profiles, Antioxidant and Antibacterial Activities of 11 Phellinus Mushrooms Collected in Thailand
The Natural Products Journal