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Updated: Jun 28, 2026

A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors
Published on: December 7, 2014
Recent advances in the development of multi-kinase inhibitors
Martin Krug1, Andreas Hilgeroth
1Martin Luther University Halle-Wittenberg, Institute of Pharmacy, Wolfgang-Langenbeck-Strasse 4, 06120 Halle (Saale), Germany.
Abstract:
During the last two decades, protein kinases have emerged as a major target for cancer therapy and a large number of selective kinase inhibitors have been developed as potential anticancer drugs. To avoid unpredictable toxic effects, researchers usually aim at designing highly selective inhibitors. But since the formation and progression of a tumor has to be considered as a multifactorial process, which is dependent on different signalling pathways, it seems reasonable to establish anticancer therapies that target several kinases associated with tumor growth. In general, this can be achieved by two different strategies, either by concomitantly using a combination of a set of selective kinase inhibitors or by administering a single agent, which simultaneously inhibits several kinases, a so called multi-kinase inhibitor. In this review, benefits and obstacles of both strategies are discussed. An overview over recently approved and newly upcoming multi-kinase inhibitors is given.
Insights
Targeting protein kinases with inhibitors is key for cancer therapy. This review explores dual-action multi-kinase inhibitors versus combinations of selective inhibitors, discussing their benefits and drawbacks for cancer treatment.
Area of Science:
- Oncology
- Pharmacology
- Molecular Biology
Background:
- Protein kinases are crucial targets in cancer therapy, with numerous selective inhibitors developed.
- Tumorigenesis is a multifactorial process involving various signaling pathways, necessitating broader therapeutic strategies.
- Current approaches include using multiple selective kinase inhibitors or single multi-kinase inhibitors.
Purpose of the Study:
- To review the benefits and obstacles of using combinations of selective kinase inhibitors versus multi-kinase inhibitors.
- To provide an overview of recently approved and emerging multi-kinase inhibitors in cancer therapy.
Main Methods:
- Literature review of scientific publications and drug development data.
- Analysis of therapeutic strategies involving kinase inhibitors for cancer treatment.
- Comparative assessment of single-agent multi-kinase inhibition versus combination therapy.
Main Results:
- Both combination therapy and multi-kinase inhibitors offer strategies to target complex cancer signaling pathways.
- Multi-kinase inhibitors present a single-agent approach to simultaneously inhibit multiple kinases involved in tumor growth.
- The review details approved and upcoming multi-kinase inhibitors, highlighting their therapeutic potential.
Conclusions:
- Targeting multiple kinases is a rational approach for cancer therapy due to the multifactorial nature of tumorigenesis.
- Both combination therapy and multi-kinase inhibitors have distinct advantages and disadvantages that need careful consideration.
- Multi-kinase inhibitors represent a significant advancement in anticancer drug development, offering a streamlined therapeutic option.
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