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Updated: Oct 31, 2025

A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors
Published on: December 7, 2014
Repurposing existing therapeutics, its importance in oncology drug development: Kinases as a potential target
Saiful Islam1, Shudong Wang1, Nikola Bowden2
1Drug Discovery and Development, Clinical and Health Sciences, University of South Australia, Adelaide, SA, 500, Australia.
Abstract:
Repurposing the large arsenal of existing non-cancer drugs is an attractive proposition to expand the clinical pipelines for cancer therapeutics. The earlier successes in repurposing resulted primarily from serendipitous findings, but more recently, drug or target-centric systematic identification of repurposing opportunities continues to rise. Kinases are one of the most sought-after anti-cancer drug targets over the last three decades. There are many non-cancer approved drugs that can inhibit kinases as "off-targets" as well as many existing kinase inhibitors that can target new additional kinases in cancer. Identifying cancer-associated kinase inhibitors through mining commercial drug databases or new kinase targets for existing inhibitors through comprehensive kinome profiling can offer more effective trial-ready options to rapidly advance drugs for clinical validation. In this review, we argue that drug repurposing is an important approach in modern drug development for cancer therapeutics. We have summarized the advantages of repurposing, the rationale behind this approach together with key barriers and opportunities in cancer drug development. We have also included examples of non-cancer drugs that inhibit kinases or are associated with kinase signalling as a basis for their anti-cancer action.
Insights
Drug repurposing offers a strategic approach to cancer therapeutics by identifying existing non-cancer drugs that inhibit kinases. This method accelerates the development of novel cancer treatments, leveraging known drug safety profiles.
Area of Science:
- Oncology
- Pharmacology
- Drug Discovery
Background:
- Drug repurposing is a valuable strategy for expanding cancer therapeutics pipelines.
- Historically, drug repurposing relied on serendipity, but systematic approaches are now prevalent.
- Kinases are critical anti-cancer targets, with many existing drugs exhibiting kinase inhibitory off-target effects.
Purpose of the Study:
- To review the advantages, rationale, barriers, and opportunities of drug repurposing in cancer therapy.
- To highlight the potential of repurposing non-cancer drugs and existing kinase inhibitors for oncology.
- To provide examples of drugs with anti-cancer kinase-related activity.
Main Methods:
- Systematic identification of repurposing opportunities through drug- or target-centric approaches.
- Mining commercial drug databases for kinase inhibitors.
- Comprehensive kinome profiling to identify new kinase targets for existing inhibitors.
Main Results:
- Drug repurposing accelerates the identification of trial-ready cancer therapeutics.
- Systematic approaches enhance the efficiency of finding repurposed drugs.
- Kinase inhibition is a key mechanism for many repurposed anti-cancer agents.
Conclusions:
- Drug repurposing is a vital component of modern cancer drug development.
- Leveraging off-target kinase inhibition and kinome profiling can yield effective cancer treatments.
- Repurposing existing drugs offers a faster, more cost-effective route to clinical validation.
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