Related Experiment Video
Updated: May 22, 2026

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
Published on: October 23, 2019
Inhibitors of the anaplastic lymphoma kinase
1University of Milano-Bicocca, Monza, Italy. luca.mologni@unimib.it
Introduction:
Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase normally expressed in the developing nervous tissue. Genetic alterations of ALK are associated with a number of cancers, including anaplastic large cell lymphoma (ALCL) and a subset of non-small cell lung cancer (NSCLC). Standard therapies for these diseases include surgery plus unspecific cytotoxic agents, with a low therapeutic window and significant treatment-associated systemic toxicity. A few small-molecule inhibitors of ALK kinase activity have been described in the recent years, some of which are currently undergoing clinical evaluation.
Areas Covered:
Literature was searched for all ALK inhibitors that have entered clinical investigation, including published research articles and meeting abstracts. Data on pharmacokinetics, safety and efficacy of crizotinib, as well as preliminary clinical data for second-generation compounds, are reviewed. The issue of drug resistance is discussed.
Expert Opinion:
Understanding the specific genetic aberration that causes cancer development and progression allows major advances in cancer therapy. Along the same way shown by imatinib in chronic myeloid leukemia, compounds that selectively target ALK are bringing a revolution in the treatment of ALK-positive tumors. Crizotinib has just been approved, and new more potent ALK inhibitors will shortly follow. These molecules represent another excellent proof-of-principle for targeted therapy.
Insights
Targeted therapies like ALK inhibitors offer a revolutionary approach to treating anaplastic lymphoma kinase-positive cancers. Crizotinib and emerging potent inhibitors demonstrate significant promise for improved patient outcomes.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase implicated in cancers like ALCL and NSCLC.
- Current treatments for ALK-driven cancers involve surgery and cytotoxic agents with limited efficacy and high toxicity.
- Novel small-molecule ALK inhibitors are emerging as promising therapeutic options.
Purpose of the Study:
- To review ALK inhibitors that have entered clinical investigation.
- To summarize data on crizotinib's pharmacokinetics, safety, and efficacy.
- To discuss preliminary data for second-generation ALK inhibitors and address drug resistance.
Main Methods:
- Comprehensive literature search for ALK inhibitors in clinical trials.
- Review of published research articles and meeting abstracts.
- Analysis of pharmacokinetic, safety, and efficacy data for crizotinib and newer compounds.
Main Results:
- Crizotinib has been approved for ALK-positive tumors.
- Second-generation ALK inhibitors show increased potency and potential to overcome resistance.
- Targeted ALK inhibition represents a paradigm shift in cancer therapy.
Conclusions:
- Targeted therapies based on specific genetic alterations, like ALK inhibitors, are transforming cancer treatment.
- Crizotinib and upcoming ALK inhibitors offer a new era of precision medicine for ALK-positive malignancies.
- These targeted agents exemplify the success of personalized medicine in oncology.
Related Concept Videos
Inhibition of Cdk Activity
Inhibition of CDK Activity
Targeted Cancer Therapies
There are several types of targeted therapies against specific...
The Intrinsic Apoptotic Pathway
The JAK-STAT Signaling Pathway
Anaphase Promoting Complex
