Grage T B, Weiss A J, Wilson W, Reynolds V
J Surg Oncol. 1975;7(5):415-20. doi: 10.1002/jso.2930070513.
Porfiromycin was given to a group of patients with a variety of solid tumors. Of 114 patients admitted to the study, 103 yielded evaluable data. The following dosage schedules were used to determine the toxicity of porfiromycin when given in multiple doses by intravenous injection: 0.2 mg/kg x 5 days, 0.3 mg/kg x 5 days, 0.35 mg/kg x 5 days, 0.4 mg/kg x 5 days, 0.24 mg/kg x 10 days and 0.6 mg/kg weekly. Toxic effects noted were mainly leukopenia, thrombocytopenia, and, when injected paravenously, local tissue necrosis. Biological effects were noted at all dosage levels and were more severe at the higher dosages. The data suggest that profiromycin administered intravenously at a dose of 0.35 mg/kg daily for 5 days results in moderate hermatological toxicity and clinical evaluation in a Phase II study at this dosage level is indicated.
将甲基丝裂霉素给予一组患有多种实体瘤的患者。在纳入该研究的114名患者中，103名产生了可评估的数据。采用以下给药方案来确定静脉注射多次甲基丝裂霉素时的毒性：0.2毫克/千克×5天、0.3毫克/千克×5天、0.35毫克/千克×5天、0.4毫克/千克×5天、0.24毫克/千克×10天以及每周0.6毫克/千克。观察到的毒性作用主要是白细胞减少、血小板减少，静脉旁注射时会出现局部组织坏死。在所有剂量水平均观察到生物学效应，且在较高剂量时更为严重。数据表明，每天以0.35毫克/千克的剂量静脉注射甲基丝裂霉素，持续5天，会导致中度血液学毒性，因此表明在此剂量水平进行II期临床研究。
