Eagan R T, Ingle J N, Rubin J, Frytak S, Moertel C G
J Natl Cancer Inst. 1978 Jan;60(1):93-6. doi: 10.1093/jnci/60.1.93.
Maytansine, an ansa macrolide, was evaluated in an early clinical trial in 40 adult patients with various solid tumors. Severe nausea and vomiting, sometimes associated with watery diarrhea and abdominal cramps, and liver function abnormalities, mainly elevation of serum glutamic--oxaloacetic transaminase levels, together constituted what we considered dose-limiting toxicity. Mild hematologic toxicity (mainly thrombocytopenia), neurotoxicity, and possibly cardiac toxicity were also noted. No antitumor effect was seen. An iv dose of 0.750 mg/m2 on days 1, 3, and 5 (total dose, 2.25 mg/m2) repeated every 4 weeks is recommended for Phase II trials.
美登素，一种安莎大环内酯类药物，在一项针对40名患有各种实体瘤的成年患者的早期临床试验中进行了评估。严重的恶心和呕吐，有时伴有水样腹泻和腹部绞痛，以及肝功能异常，主要是血清谷草转氨酶水平升高，共同构成了我们认为的剂量限制性毒性。还观察到轻度血液学毒性（主要是血小板减少症）、神经毒性以及可能的心脏毒性。未观察到抗肿瘤效果。推荐在II期试验中每4周重复一次，于第1、3和5天静脉注射剂量为0.750 mg/m²（总剂量为2.25 mg/m²）。
