Carmichael J
CRC Department of Clinical Oncology, Nottingham City Hospital, Trust, UK.
Br J Cancer. 1998;78 Suppl 3(Suppl 3):21-5. doi: 10.1038/bjc.1998.750.
Gemcitabine (GEMZAR) is a novel nucleoside analogue with activity in a range of preclinical models both in vitro and in vivo. It is highly schedule dependent, with weekly x3 every 4 weeks being the recommended schedule for phase II/III studies. Early phase II trials identified activity against non-small-cell lung cancer and pancreatic cancers, tumour types for which gemcitabine has a licence for treatment in many countries. However, the preclinical models indicated that gemcitabine may be active against many other human solid tumours. In phase II studies, activity has been identified against breast cancer, both as a single agent and in combination. In bladder cancer, impressive single-agent activity of gemcitabine has also been seen, as well as in combination with cisplatin, initially in MVAC and platinum failures but more recently as first-line therapy both as a single agent and combined with cisplatin. Anti-tumour activity has also been seen in patients with ovarian cancer, head and neck cancer, small-cell lung cancer and cervical cancer, with minimal activity in renal carcinoma, prostate and colon cancer. In view of the excellent side-effect profile and the potential for gemcitabine to inhibit DNA repair after exposure to DNA-damaging agents, further developments of gemcitabine will include its use in combination chemotherapy and combined modality schedules.
吉西他滨（健择）是一种新型核苷类似物，在一系列临床前体外和体内模型中均具有活性。它高度依赖给药方案，每4周每周给药3次是II/III期研究的推荐方案。早期II期试验确定了其对非小细胞肺癌和胰腺癌的活性，在许多国家吉西他滨已获许可用于治疗这两种肿瘤类型。然而，临床前模型表明吉西他滨可能对许多其他人类实体瘤也有活性。在II期研究中，已确定其对乳腺癌有活性，无论是单药治疗还是联合治疗。在膀胱癌中，也观察到吉西他滨单药治疗有显著活性，以及与顺铂联合治疗的活性，最初用于甲氨蝶呤、长春碱、阿霉素和顺铂（MVAC）方案及铂类治疗失败的患者，但最近也作为一线治疗，单药或与顺铂联合使用。在卵巢癌、头颈癌、小细胞肺癌和宫颈癌患者中也观察到了抗肿瘤活性，而在肾癌、前列腺癌和结肠癌中活性最小。鉴于吉西他滨出色的副作用特征以及其在接触DNA损伤剂后抑制DNA修复的潜力，吉西他滨的进一步研发将包括其在联合化疗和综合治疗方案中的应用。
