Over the past two decades, tyrosine kinase inhibitors (TKIs) have rapidly emerged as pivotal targeted agents, offering promising therapeutic prospects for patients. However, as the cornerstone of targeted therapies, an increasing number of TKIs have been found to develop acquired resistance during treatment, making the challenge of overcoming this resistance a primary focus of current research. This review comprehensively examines the evolution of TKIs from multiple perspectives, with particular emphasis on the mechanisms underlying acquired resistance, innovative drug design strategies, inherent challenges, and future directions.

中文翻译：

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酪氨酸激酶靶向治疗的获得性耐药：机制和应对策略


在过去的二十年里，酪氨酸激酶抑制剂 （TKI） 迅速成为关键的靶向药物，为患者提供了广阔的治疗前景。然而，作为靶向治疗的基石，已发现越来越多的 TKI 在治疗过程中产生获得性耐药，这使得克服这种耐药性的挑战成为当前研究的主要重点。本综述从多个角度全面研究了 TKIs 的进化，特别强调了获得性耐药的机制、创新药物设计策略、固有挑战和未来方向。