Von Hoff D D
Institute for Drug Development, Cancer Therapy and Research Center, San Antonio, TX, USA.
Invest New Drugs. 1996;14(3):265-70. doi: 10.1007/BF00194529.
2',2'-difluorodeoxycytidine (LY 188011, Gemcitabine, Gemzar) has recently been approved both in Europe for the treatment of patients with non-small cell lung cancer and in the United States for patients with pancreatic cancer. Since the initial discovery of the compound, we have been evaluating the in vitro activity of gemcitabine against human tumor colony-forming units taken directly from patients and growing in soft agar (in the human tumor cloning assay-HTCA). A total of 315 specimens have had gemcitabine tested against them with 44% giving evaluable results. Gemcitabine has been found to be active against colony-forming units from patients with non-small cell lung, breast, ovarian, and pancreatic cancers. A concentration-dependent in vitro response was noted with a higher in vitro response rate noted at 20 micrograms/ml than at 2.0 micrograms/ml. Based on subsequent clinical phase II data, the HTCA correctly predicted the wide spectrum of the clinical activity of gemcitabine.
2',2'-二氟脱氧胞苷（LY 188011，吉西他滨，健择）最近在欧洲被批准用于治疗非小细胞肺癌患者，在美国被批准用于治疗胰腺癌患者。自从该化合物最初被发现以来，我们一直在评估吉西他滨对直接取自患者并在软琼脂中生长的人肿瘤集落形成单位的体外活性（在人肿瘤克隆试验 - HTCA中）。共有315个标本接受了吉西他滨的测试，其中44%给出了可评估的结果。已发现吉西他滨对非小细胞肺癌、乳腺癌、卵巢癌和胰腺癌患者的集落形成单位有活性。观察到浓度依赖性的体外反应，在20微克/毫升时的体外反应率高于2.0微克/毫升时。基于随后的临床II期数据，HTCA正确地预测了吉西他滨临床活性的广泛范围。
