Department of Oncology and Neurosciences, Foundation University G. d'Annunzio Medical School, Chieti-Pescara, Italy.
Curr Cancer Drug Targets. 2010 Aug;10(5):462-83. doi: 10.2174/156800910791517208.
Over the last ten years, several new and therapeutically relevant cancer drugs targeting tyrosine kinases signaling pathways have been developed. Tyrosine kinase inhibitors (TKIs) are a pharmaceutical class of small molecules, orally available, well-tolerated, worldwide approved drugs for the treatment of several neoplasms, including lung, breast, kidney and pancreatic cancer as well as gastro-intestinal stromal tumors and chronic myeloid leukemia. This comprehensive review focuses on the most relevant members of the first and the second generation TKIs designed to interact with receptor and nonreceptor TKs. Attention is mainly focused on molecular mechanisms in in vitro and in vivo models related to the clinical activity of the drugs and to the development of resistance to treatment, still the major challenge in cancer research and care.
在过去的十年中，已经开发出了几种针对酪氨酸激酶信号通路的新的、有治疗意义的癌症药物。酪氨酸激酶抑制剂 (TKI) 是一类小分子药物，口服、耐受性好，已在全球批准用于治疗多种肿瘤，包括肺癌、乳腺癌、肾癌和胰腺癌，以及胃肠间质瘤和慢性髓性白血病。本综述重点介绍了旨在与受体和非受体 TKI 相互作用的第一代和第二代 TKI 中最相关的成员。主要关注与药物临床活性和治疗耐药性发展相关的体外和体内模型中的分子机制，这仍然是癌症研究和治疗的主要挑战。
