Rodriguez V, Gottlieb J, Burgess M A, Livingston R, Wheeler W, Spitzer G, Bodey G P, Blumenschein G R, Freireich E J
Cancer. 1976 Aug;38(2):690-4. doi: 10.1002/1097-0142(197608)38:2<690::aid-cncr2820380212>3.0.co;2-x.
Phase I studies were conducted in 58 adult cancer patients with Baker's Antifol (BAF), a new active-site directed inhibitor of dihydrofolate reductase. Dose escalation ranged from 10 to 250 mg/m2/day X 5 days and courses of treatment were repeated every 2-3 weeks. Biologic effects were observed mostly at doses greater than 100 mg/m2/day X 5 days. The patients developed myelosuppression during 19% of the trials. Other types of toxicity were dermatitis in 12 to 30% and stomatitis in 7 to 38% of the trials. Toxicity was directly related to the impairment of the patient's liver function. Two partial responses (in a patient with adenocarcinoma of the lung and a patient with transitional cell carcinoma of the bladder) occurred. BAF is an active new chemotherapeutic agent which deserves further clinical trials in patients with various malignancies.
对58例成年癌症患者开展了I期研究，使用了一种新型的二氢叶酸还原酶活性位点定向抑制剂——贝克抗叶酸（BAF）。剂量递增范围为10至250毫克/平方米/天，持续5天，每2至3周重复一个疗程。生物效应大多在剂量大于100毫克/平方米/天且持续5天的情况下观察到。在19%的试验中，患者出现了骨髓抑制。在12%至30%的试验中出现了其他类型的毒性反应，即皮炎，在7%至38%的试验中出现了口腔炎。毒性反应与患者肝功能受损直接相关。出现了两例部分缓解（一例为肺腺癌患者，另一例为膀胱移行细胞癌患者）。BAF是一种有效的新型化疗药物，值得在各类恶性肿瘤患者中进一步开展临床试验。
