Kamei H, Takenaka K, Goto T, Suga S, Fugiwara A, Nakao I, Agatsuma T, Fujita K, Isurugi K, Kubota T
Gan To Kagaku Ryoho. 1986 Jun;13(6):2208-15.
A phase I study was performed on a newly developed antitumor agent, Bestrabucil (KM 2210). The study was started at an initial dose of 1 n 25 mg/body, and gradually increased up to 32n 800 mg/body. With single (35 patients) and five-consecutive-day (36 patients) administration, the dose-limiting factor was found to be tarry stool, remarkable decrease in hemoglobin content, and strong nipple and breast pain. The maximum tolerated dose (MTD) was concluded to be around 700 to 800 mg/body. With long-term administration (the longest term, 20 weeks, 36 patients), the dose-limiting factor was concluded to be a decrease in the peripheral leukocyte count when the total amount administered reached about 10 g. Side effects on the alimentary system due to this agent, such as vomiting, nausea and anorexia, were observed. In addition, mastalgia and genital bleeding due to released estrogen were also seen, especially in the case of long-term administration.
对一种新开发的抗肿瘤药物Bestrabucil（KM 2210）进行了一项I期研究。该研究起始剂量为1×25mg/体，并逐渐增加至32×800mg/体。单次给药（35例患者）和连续五天给药（36例患者）时，剂量限制因素为柏油样便、血红蛋白含量显著降低以及强烈的乳头和乳房疼痛。最大耐受剂量（MTD）被确定为约700至800mg/体。长期给药（最长20周，36例患者）时，当给药总量达到约10g时，剂量限制因素被确定为外周白细胞计数减少。观察到该药物对消化系统的副作用，如呕吐、恶心和厌食。此外，还出现了因雌激素释放引起的乳房疼痛和生殖器出血，尤其是在长期给药的情况下。
