Comis R L, Issell B F, Pittman K, Ginsberg S J, Rudolph A, Aust J C, DiFino S M, Tinsley R W, Poiesz B J, Crooke S T
Cancer Res. 1982 Jul;42(7):2944-8.
Carminomycin (CMN) was administered i.v. to 44 patients with a variety of nonhematological cancers every 4 weeks at doses of 15, 20, 22.5, and 25 mg/sq m. Granulocytopenia was the dose-limiting toxicity. The median granulocyte count for previously untreated patients receiving 22.5 mg/sq m was 0.962 cells/microliters, and for previously treated patients receiving 20 mg/sq m it was 0.420 cell/microliters. Moderate to severe phlebitis was associated with drug administration in 50% of cases. Nausea, vomiting, and alopecia were mild. Three of nine patients who received a total CMN dose of greater than or equal to 100 mg/sq m (mean, 132 mg/sq m) developed unexplained decreases in radionuclide cardiac ejection fraction, with one patient developing decreased QRS amplitude and congestive heart failure at a total dose of 160 mg/sq m. CMN is rapidly metabolized to carminomycinol. The elimination half-lives of CMN and carminomycinol are 6 to 10 and 50 hr, respectively. CMN was found to be a more potent inhibitor of human granulocyte-macrophage colony-forming units than was carminomycinol. Objective partial responses were seen in two of seven previously untreated patients with non-small cell lung cancer and one of three patients with squamous cell carcinoma of the head and neck previously untreated with chemotherapy.
对44例患有各种非血液系统癌症的患者静脉注射卡米诺霉素（CMN），每4周一次，剂量分别为15、20、22.5和25mg/m²。粒细胞减少是剂量限制性毒性。接受22.5mg/m²的既往未治疗患者的粒细胞计数中位数为0.962细胞/微升，接受20mg/m²的既往治疗患者的粒细胞计数中位数为0.420细胞/微升。50%的病例中，药物给药与中度至重度静脉炎有关。恶心、呕吐和脱发症状较轻。9例接受CMN总剂量大于或等于100mg/m²（平均132mg/m²）的患者中有3例出现放射性核素心脏射血分数 unexplained下降，1例患者在总剂量为160mg/m²时出现QRS波幅降低和充血性心力衰竭。CMN迅速代谢为卡米诺霉素醇。CMN和卡米诺霉素醇的消除半衰期分别为6至10小时和50小时。发现CMN比卡米诺霉素醇更有效地抑制人粒细胞-巨噬细胞集落形成单位。7例既往未治疗的非小细胞肺癌患者中有2例出现客观部分缓解，3例既往未接受化疗的头颈部鳞状细胞癌患者中有1例出现客观部分缓解。
