Abstract

Efficacy and Toxicity Assessment of Different Clinically Used Small Molecular Tyrosine Kinase Inhibitors by Computational Molecular Docking Method

Highlights

  • Though angiogenesis is a physiological process; almost all types of solid tumors survive by utilizing this process

  • Among the studied small molecular AAG drugs we have found that gefitinib most strongly binds to the VEGF receptor (-11.6 kcal/mol); whereas erlotinib has less binding affinity to the VEGF (Table 3 and Figure 1)

  • Among the studied drugs our results indicate that binding affinities of the drugs to the tyrosine kinase (TK) receptor are in following order: imatinib ≤ gefitinib < sunitinib < soratinib < erlotinib < lapatinib

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Summary

Introduction

Though angiogenesis is a physiological process; almost all types of solid tumors survive by utilizing this process. Development of different therapeutic strategies that can control of tumor angiogenesis becomes an important aspect in clinical oncology [1,2]. For several types of cancer, different antiangiogenic (AAG) drugs are generally used as an adjuvant therapy that is, in combination with the conventional MTD (maximal tolerable dosing strategy) chemotherapy. Such applications have shown positive results with reduced (chemotherapy related) toxicities [3]. Therapy with different AAG drugs are supplement the ongoing chemotherapy (with docetaxel, platinum based therapies, paclitaxel, vinorelbine and gemcitabine) and becomes important when the conventional chemotherapies have failed or are not tolerated [4]. Different AAG drugs are targeted towards receptors that are involved with tyrosine kinase (TK) mediated cell proliferation [5,6,7]

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