Related Experiment Video
Updated: Dec 27, 2025
Establishment and Characterization of Patient-Derived Xenograft Models of Anaplastic Thyroid Carcinoma and Head and Neck Squamous Cell Carcinoma
Published on: June 2, 2023
Anaplastic lymphoma kinase inhibitors: an updated patent review (2014-2018)
Yi-Min Liu1,2, Chun-Nan Kuo3,4, Jing-Ping Liou1,3
1TMU Biomedical Commercialization Center, Taipei Medical University, Taipei, Taiwan.
Abstract:
Introduction: Anaplastic lymphoma kinase (ALK), a receptor tyrosine kinase, has been discovered in several cancers, including anaplastic large-cell lymphoma, non-small cell lung cancer, and inflammatory myofibroblastic tumors. The deregulation of ALK activities, such as translocation and point mutation, results in human carcinogenesis. The use of ALK inhibitors in clinical cancer treatment has been shown to be efficacious, and the issue of resistance to ALK inhibitors has been reported. Consequently, the development of a new generation of ALK inhibitors is necessary.Areas covered: This paper provides a comprehensive review of the patent literature from 2014 to 2018 including small molecule ALK inhibitors and their use as anticancer agents. The approved and developing ALK inhibitors are described.Expert commentary: The available three generations of ALK inhibitors have shown a good anticancer effect in ALK-positive non-small cell lung cancer. An urgent issue in this field is ALK resistance development. The development of new ALK inhibitors through structure modification of currently available ALK inhibitors is proceeding, such as the synthesis of macrocyclic compounds. This article arranges the ALK inhibitors that have published in the patent in recent years. It may help in the investigation of a new generation of ALK inhibitors, which can overcome the resistance issue and development of novel drug candidates in the future.
Insights
New generations of anaplastic lymphoma kinase (ALK) inhibitors are needed to overcome resistance in cancer treatment. This review covers recent patents on small molecule ALK inhibitors for improved anticancer therapies.
Area of Science:
- Oncology
- Medicinal Chemistry
- Drug Discovery
Background:
- Anaplastic lymphoma kinase (ALK) is implicated in various cancers, including non-small cell lung cancer.
- Dysregulation of ALK, through mutations or translocations, drives carcinogenesis.
- Existing ALK inhibitors show efficacy but face resistance challenges, necessitating new therapeutic strategies.
Purpose of the Study:
- To comprehensively review patent literature (2014-2018) on small molecule ALK inhibitors.
- To describe approved and developing ALK inhibitors for anticancer applications.
- To identify trends and potential avenues for next-generation ALK inhibitor development.
Main Methods:
- Systematic review of patent literature focusing on small molecule ALK inhibitors.
- Analysis of approved and investigational ALK inhibitors within the specified patent period.
- Categorization of inhibitors based on chemical structure and therapeutic application.
Main Results:
- The review covers numerous small molecule ALK inhibitors patented between 2014 and 2018.
- Approved and emerging ALK inhibitors demonstrate significant anticancer effects in ALK-positive cancers.
- Ongoing research focuses on structural modifications, such as macrocyclic compounds, to address resistance.
Conclusions:
- Three generations of ALK inhibitors are effective against ALK-positive non-small cell lung cancer.
- Development of resistance to current ALK inhibitors is a critical clinical challenge.
- Future research, guided by patent literature, aims to create novel ALK inhibitors that overcome resistance and lead to new drug candidates.
Related Concept Videos
02:57Targeted Cancer Therapies
There are several types of targeted therapies against...
02:34Inhibition of Cdk Activity