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Several chemotherapeutic agents remain mainstays in cancer treatment. However, their limited efficacy underscores the need for therapies that target tumor cells while minimizing adverse effects. Combination therapies have emerged as promising alternatives. Among these, small molecule inhibitors (SMIs) represent a pivotal class of agents implicated in combination with chemotherapy or radiation therapy. Receptor tyrosine kinases (RTKs), key molecular targets for many SMIs, and the increasing number of effective RTK inhibitors (RTKIs) highlight their growing role in oncology. However, only a few RTKIs have progressed to clinical trials. Several approved RTKIs are multi-targeted inhibitors, which often result in significant off-target effects and toxicity when compared to selective RTKIs. However, their development and clinical application remain limited. This chapter highlights the characteristic features of various RTKIs, advances in the development of selective RTKIs in combination with other well-established therapies in cancer, and their targets that could drive the next generation of targeted therapeutics.

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Receptor Tyrosine Kinase Inhibitors in Combination Therapies: Integrating Chemotherapy and Radiation Therapy for Improved Cancer Treatment

  • 章节

  • 发表日期：

    2025年

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  • Rohit Patel,
  • Johnna Francis Varghese

摘要

Several chemotherapeutic agents remain mainstays in cancer treatment. However, their limited efficacy underscores the need for therapies that target tumor cells while minimizing adverse effects. Combination therapies have emerged as promising alternatives. Among these, small molecule inhibitors (SMIs) represent a pivotal class of agents implicated in combination with chemotherapy or radiation therapy. Receptor tyrosine kinases (RTKs), key molecular targets for many SMIs, and the increasing number of effective RTK inhibitors (RTKIs) highlight their growing role in oncology. However, only a few RTKIs have progressed to clinical trials. Several approved RTKIs are multi-targeted inhibitors, which often result in significant off-target effects and toxicity when compared to selective RTKIs. However, their development and clinical application remain limited. This chapter highlights the characteristic features of various RTKIs, advances in the development of selective RTKIs in combination with other well-established therapies in cancer, and their targets that could drive the next generation of targeted therapeutics.