Braakhuis B J, van Dongen G A, van Walsum M, Leyva A, Snow G B
Department of Otolaryngology, Free University Hospital, Amsterdam, The Netherlands.
Invest New Drugs. 1988 Dec;6(4):299-304. doi: 10.1007/BF00173648.
The antitumor activity of 5-aza-2'-deoxycytidine (5-aza-dCyd), a nucleoside analog, was established in human head and neck cancer xenografts, transplanted in nude mice. A significant response was noted in 3 of 5 lines, when the drug was injected intraperitoneally at a maximum tolerated dose of 2 mg/kg every four days for three doses. In two most sensitive lines 1 out of 6 tumors regressed completely. The antitumor activity of the drug may depend on the schedule used, as illustrated by the fact that just one of these two lines appeared to be sensitive when treated with low daily doses (0.25 mg/kg). In two lines, 5-aza-dCyd showed equal or better antitumor activity when compared to the conventional drugs known to produce remissions in patients with head and neck cancer (cisplatin, methotrexate, bleomycin, 5-fluorouracil and cyclophosphamide). 5-Aza-dCyd is a drug with potential value in the chemotherapeutic treatment of patients with head and neck cancer [corrected].
核苷类似物5-氮杂-2'-脱氧胞苷（5-aza-dCyd）在移植于裸鼠的人头颈癌异种移植模型中显示出抗肿瘤活性。当以2mg/kg的最大耐受剂量每四天腹腔注射给药三次时，5个细胞系中有3个出现了明显反应。在两个最敏感的细胞系中，6个肿瘤中有1个完全消退。药物的抗肿瘤活性可能取决于用药方案，这一点从以下事实可以看出：当用低剂量每日给药（0.25mg/kg）时，这两个细胞系中只有一个似乎敏感。在两个细胞系中，与已知对头颈癌患者有缓解作用的传统药物（顺铂、甲氨蝶呤、博来霉素、5-氟尿嘧啶和环磷酰胺）相比，5-aza-dCyd显示出同等或更好的抗肿瘤活性。5-aza-dCyd是一种在头颈癌患者化疗中具有潜在价值的药物[校正后]
