Shibata H, Ueda T, Kanakura Y, Mitsui H, Nakagawa M, Yakura H, Taoka T, Tejima H, Hiraoka A, Masaoka T
Gan To Kagaku Ryoho. 1986 Oct;13(10):2974-80.
K 18, an IgG-Melphalan conjugate was administered to 30 patients, who had recurrent hematopoietic malignancy. Ten out of the 30 patients received single doses of 1 to 20 enteric tablets containing 10 mg of K 18, as a phase I study. No side effects were observed. K 18 was administered every day to the remaining 20 patients in order to evaluate the side effects and therapeutic effects, as a phase II study. One patient attained partial remission. Although no remission effect was obtained in 14 of the 20 patients, antitumor effects such as a decrease in leukemia cells, were observed in 4 of 20 patients. As to side effects, neither recurrence of tumor nor cumulative toxicity were shown in one patient with NHL who received only K 18 for 14 months as maintenance therapy. Evaluation of antitumor effect was difficult in the case of the remaining 4 patients. In the 20 cases who entered the phase II study, a decrease in neutrophils was observed in 2 patients, a slight decrease in platelets in 3 patients and increased transaminase activity in one patient as side effects of K 18. In brief, compared with Melphalan, K 18 has between 1.3 and 2 times a more potent therapeutic effect, with extremely low side effects.
K18（一种免疫球蛋白-美法仑结合物）被给予30例复发性造血系统恶性肿瘤患者。作为I期研究，30例患者中有10例接受了单剂量的1至20片含10毫克K18的肠溶片剂，未观察到副作用。作为II期研究，为了评估副作用和治疗效果，每天给其余20例患者使用K18。1例患者获得部分缓解。虽然20例患者中有14例未获得缓解效果，但20例患者中有4例观察到了抗肿瘤效果，如白血病细胞减少。关于副作用，1例接受K18作为维持治疗仅14个月的非霍奇金淋巴瘤患者既未出现肿瘤复发也未出现累积毒性。其余4例患者的抗肿瘤效果评估较为困难。在进入II期研究的20例患者中，有2例患者出现中性粒细胞减少，3例患者血小板略有减少，1例患者转氨酶活性升高，这些都是K18的副作用。简而言之，与美法仑相比，K18的治疗效果强1.3至2倍，且副作用极低。
