Tsuda H, Hara H, Eriguchi N, Nishida H, Yoshida H, Kumabe T, Sugita Y
Department of Anesthesiology, Kurume University School of Medicine, Japan.
Kurume Med J. 1995;42(4):241-9. doi: 10.2739/kurumemedj.42.241.
Antineoplastons, which were firstly described by Burzynski, are naturally occurring peptides and amino acid derivatives which control neoplastic growth. We conducted a toxicological study of the Antineoplastons A-10 and AS2-1 in combination with other anticancer agents or radiation in 42 patients, 46 tumors with terminal stage cancer. Antineoplaston A-10 oral formulation and A-10 injectable formulation was administered in 14 and 25 patients respectively. The maximum daily dose was 10 g and 40 g, respectively and the longest term of administration was 610 days and 67 days, respectively. Antineoplaston AS2-1 oral formulation and AS2-1 injectable formulation was administered in 33 and 10 patients, respectively, the maximum daily dose was 12 g and 30 g, respectively, and the longest term was 1070 days and 25 days, respectively. The major adverse effects that may have been related to these agents as used in combination with other conventional chemotherapeutic agents or radiation were general weakness, myelosuppression, and liver dysfunction, but these effects were not seen when either Antineoplaston was administered alone. The minor adverse effects observed in single use of either Antineoplaston A-10 or AS2-1 were excess gas, maculopapullar rash, fingers rigidity, reduced cholesterol, reduced albumin, increased amylase, eosinophilia, increased alkaline phosphatase, headache, hypertension, palpitation, peripheral edema but these adverse effects did not limit to continuation of either agent. The evaluation of the usefulness of the Antineoplastons in combination therapy based on the imaging findings during the course of treatment revealed disappearance or measurable shrinkage of the tumor lasting more than one months as visualized by magnetic resonance imaging or computed tomography was seen in 15 tumors (32.6%). No increase in size of tumor for more than 3 months was observed in 8 (17.4%). The mean survival time of these patients was significantly longer than that in patients with tumors showing progressive increasing (17.52 + 3.31 months vs 4.80 + 0.65 months, p < 0.005). Antineoplaston A-10 and AS2-1 are less toxic than conventional chemotherapeutics and they were useful in maintenance therapy for cancer patients.
抗瘤酮最早由布尔津斯基描述，是天然存在的肽和氨基酸衍生物，可控制肿瘤生长。我们对42例患有晚期癌症的患者、46个肿瘤进行了抗瘤酮A - 10和AS2 - 1与其他抗癌药物或放疗联合使用的毒理学研究。抗瘤酮A - 10口服制剂和注射制剂分别给予14例和25例患者。最大日剂量分别为10克和40克，最长给药期限分别为610天和67天。抗瘤酮AS2 - 1口服制剂和注射制剂分别给予33例和10例患者，最大日剂量分别为12克和30克，最长给药期限分别为1070天和25天。与这些药物与其他传统化疗药物或放疗联合使用可能相关的主要不良反应为全身虚弱、骨髓抑制和肝功能障碍，但单独使用任何一种抗瘤酮时均未出现这些效应。单独使用抗瘤酮A - 10或AS2 - 1观察到的轻微不良反应为胃肠胀气、斑丘疹、手指僵硬、胆固醇降低、白蛋白降低、淀粉酶升高、嗜酸性粒细胞增多、碱性磷酸酶升高、头痛、高血压、心悸、外周水肿，但这些不良反应并未限制任何一种药物的继续使用。基于治疗过程中的影像学检查结果对抗瘤酮在联合治疗中的有效性进行评估发现，15个肿瘤（32.6%）经磁共振成像或计算机断层扫描显示肿瘤消失或可测量的缩小持续超过1个月。8个肿瘤（17.4%）观察到肿瘤大小3个月以上未增加。这些患者的平均生存时间显著长于肿瘤呈进行性增大的患者（17.52±3.31个月对4.8±0.65个月，p<0.005）。抗瘤酮A - 10和AS2 - 1的毒性低于传统化疗药物，对癌症患者的维持治疗有用。
