Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review
. 2022 Jan;88(1):64-74.
doi: 10.1111/bcp.14964. Epub 2021 Jul 9.

Repurposing existing therapeutics, its importance in oncology drug development: Kinases as a potential target

Affiliations
Review

Repurposing existing therapeutics, its importance in oncology drug development: Kinases as a potential target

Saiful Islam et al. Br J Clin Pharmacol. 2022 Jan.

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.

Keywords: cancer; drug development; kinase; oncology; repurposing.

PubMed Disclaimer

Conflict of interest statement

The authors declare no conflict of interest.

Figures

FIGURE 1
FIGURE 1
A summary of the consequences of carcinogenesis and complexity illustrating a potential role for the repurposing of existing therapeutics
FIGURE 2
FIGURE 2
Possible pathways for identifying repurposed candidate drugs that target kinases in cancer. Shown are the potential approaches for the repurposing of non‐kinase drugs to kinase targets and the repurposing of existing kinase drugs to new targets within the kinome
FIGURE 3
FIGURE 3
A summary depicting the shift in focus with repurposing of existing drugs for new indications. The significance of the technical impacts with data generation and handling, contributing to technological scale as an approach to increase the portfolio of therapeutic agents for patients is illustrated

References

    1. Bray F, Ferlay J, Soerjomataram I, Siegel RL, Torre LA, Jemal A. Global cancer statistics 2018: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries. CA Cancer J Clin. 2018;68(6):394‐424. - PubMed
    1. Stewart B, Wild C (Eds). World Cancer Report 2014. France: Lyon‐International Agency for Research on Cancer; 2014.
    1. Mariotto AB, Yabroff KR, Shao Y, Feuer EJ, Brown ML. Projections of the cost of cancer care in the United States: 2010–2020. J Natl Cancer Inst. 2011;103(2):117‐128. - PMC - PubMed
    1. Bertolini F, Sukhatme VP, Bouche G. Drug repurposing in oncology—patient and health systems opportunities. Nat Rev Clin Oncol. 2015;12(12):732‐742. - PubMed
    1. Walker I, Newell H. Do molecularly targeted agents in oncology have reduced attrition rates? Nat Rev Drug Discov. 2009;8(1):15‐16. - PubMed

Publication types

MeSH terms

Substances