Cancer Management by Tyrosine Kinase Inhibitors: Efficacy, Limitation, and Future Strategies

Abstract

Tyrosine kinase inhibitors are taking up an increasingly significant role in treating cancers. There are different types of TKIs currently used in clinical settings. However, TKI-associated limitations such as resistance and adverse effects are frequently reported. In this chapter, we would comprehensively review the clinical efficacy of current TKIs using the currently available clinical trial data. Significant limitations of TKIs on cancer treatment will be further summarized and discussed. The strategies on overcoming the limitations of TKIs to maximize their clinical effectiveness and efficiency, such as complementary use of Chinese medicine or development of novel TKIs, will be proposed. In conclusion, an overall picture of the clinical use and limitation of the current TKIs will be drawn and the prospective development in overcoming the limitations will be discussed. Evaluation of clinical efficacy of TKIs, evaluation of limitations of TKIs, strategies in overcoming the limitations of TKIs, and conclusion (including prospective development of TKIs) are discussed below.

Cancer Therapeutic siRNA Delivery and Imaging by Nitrogen- and Neodymium-Doped Graphene Quantum Dots

“…One of the major types of RNAi technology includes the delivery of small interfering RNAs (siRNAs), noncoding double-stranded oligos roughly 20–24 nucleotides in length. Unlike tyrosine kinase inhibitors that can act on multiple targets and may lack specificity, siRNA binds to a specific complementary mRNA sequence, inducing its cleavage and inhibiting corresponding protein synthesis . To date, the FDA has already approved four siRNA-based treatments, making RNAi technology a prospective tool in gene silencing .…”

Molecular Modeling Studies on Biochanin-A as a Potential Dual inhibitor for VEGFR-2 and Cyclin D1-CDK-4 Complex

“…Sorafenib is one of the famous multi-tyrosine kinase inhibitors that target VEGFR-2 as well as other tyrosine kinases and is highly efficient in the management of HCC [9, 10]. Treatment with agents from either class imposes several dose-limiting adverse reactions that undermine the quality of life of cancer patients [11]. Therefore, we performed in silico molecular docking studies for Biochanin-A as a potential dual hit for the VEGFR-2 and Cyclin-D1-CDK4 complex to validate the utility of Biochanin-A as a scaffold for the synthesis of efficient anticancer agents.…”