叶酸类似物10-乙基-10-脱氮氨基蝶呤（10-EdAM）对人头颈癌异种移植瘤的活性。

Activity of the folate analog 10-ethyl, 10-deaza-aminopterin (10-EdAM) against human head and neck cancer xenografts.

作者信息

Brown D H, Braakhuis B J, van Dongen G A, van Walsum M, Bagnay M, Snow G B

机构信息

Department of Otolaryngology, Head and Neck Surgery, Free University Hospital, Amsterdam, The Netherlands.

出版信息

Anticancer Res. 1989 Nov-Dec;9(6):1549-52.

PMID:2627109

Abstract

In a previous study we established a markedly increased antitumour activity of 10-ethyl, 10-deaza-aminopterin (10-EdAM) as compared to methotrexate (MTX) when tested in vitro in squamous cell carcinoma cell lines from the head and neck (HNSCC). In this paper we describe the antitumour activity of these drugs in vivo in athymic nude mice bearing HNSCC xenografts. Using a schedule of 125 mg/kg i.p. for both drugs, injected on day 0 and 7, 10-EdAM caused a significant response in 2 out of 5 tumour lines, whereas MTX was completely inactive. These two lines moderately sensitive to 10-EdAM were not affected when the drug was given daily times 5 at an equitoxic dose of 0.75 mg/kg, indicating that the effect of the drug may be schedule dependent.

摘要

在先前的一项研究中，我们发现，在对头颈部鳞状细胞癌（HNSCC）细胞系进行体外测试时，与甲氨蝶呤（MTX）相比，10-乙基-10-脱氮氨基蝶呤（10-EdAM）的抗肿瘤活性显著增强。在本文中，我们描述了这些药物在携带HNSCC异种移植瘤的无胸腺裸鼠体内的抗肿瘤活性。两种药物均采用125mg/kg腹腔注射的给药方案，于第0天和第7天注射，10-EdAM在5种肿瘤细胞系中有2种产生了显著反应，而MTX则完全没有活性。当以0.75mg/kg的等效毒性剂量每日给药5次时，这两种对10-EdAM中度敏感的细胞系未受影响，这表明该药物的作用可能与给药方案有关。