Capdeville Renaud, Silberman Sandra
Novartis Oncology, Novartis Pharma AG, Basel, Switzerland; and Novartis Oncology, Novartis Pharmaceutical Corp, Florham Park, NJ, USA.
Semin Hematol. 2003 Apr;40(2 Suppl 2):15-20. doi: 10.1053/shem.2003.50037.
Imatinib (Gleevec) (formerly STI571) is an orally bioavailable rationally developed inhibitor of the tyrosine kinases Bcr-Abl, Kit, and platelet-derived growth factor receptor (PDGFR). In 4 years of clinical development, more than 12,000 patients have been treated in the clinical development program. Imatinib was first shown to be highly effective in the treatment of all stages of chronic myelogenous leukemia (CML). Moreover, preliminary results of a randomized study have demonstrated superior efficacy and safety of first-line imatinib therapy compared with a combination of interferon and cytarabine. Imatinib has also been shown to be the only effective drug therapy in the treatment of patients with metastatic gastrointestinal stromal tumors expressing the stem cell factor (SCF) receptor Kit. This review outlines the successive steps in the clinical development of this new, targeted anticancer agent.
伊马替尼（格列卫）（原称STI571）是一种口服生物利用度良好的、经过合理研发的酪氨酸激酶抑制剂，可抑制Bcr-Abl、Kit和血小板衍生生长因子受体（PDGFR）。在4年的临床研发过程中，超过12000名患者参与了临床研发项目。伊马替尼首次被证明在治疗慢性粒细胞白血病（CML）的各个阶段均具有高效性。此外，一项随机研究的初步结果表明，与干扰素和阿糖胞苷联合使用相比，一线伊马替尼治疗具有更高的疗效和安全性。伊马替尼还被证明是治疗表达干细胞因子（SCF）受体Kit的转移性胃肠道间质瘤患者的唯一有效药物疗法。本综述概述了这种新型靶向抗癌药物临床研发的连续步骤。
