Gundersen S, Aamdal S, Fodstad O
Br J Cancer. 1987 Apr;55(4):433-5. doi: 10.1038/bjc.1987.85.
A phase II trial with mitozolomide was carried out in patients with malignant melanoma, since in preclinical studies this new imidazotetrazine had shown promising effects against human melanoma xenografts. Twenty-one evaluable patients with advanced malignant melanoma were treated with 115 mg m-2 of mitozolomide, given orally every 6 weeks. None of the patients had received prior chemotherapy. Two partial responses (10 and 7+ months) were observed. The responding patients had lung metastases, and one of them had, in addition, a huge (17 X 14 cm) lymph node metastasis in the groin. Also, one patient had a 48% tumour volume reduction of lung metastases. The dose limiting side effect of the treatment was bone marrow depression, with delayed leukopenia and thrombocytopenia. The median white blood cell counts and platelet nadirs were 2.5 X 10(9) 1(-1) (range 1.1-3.8) and 59 X 10(9) 1(-1) (range 14-95), respectively. Non-haematological adverse reactions were limited to mild or moderate nausea. It is concluded that orally administered mitozolomide is active against malignant melanoma and seems to have a response rate comparable to those of the most active established drugs.
对恶性黑色素瘤患者进行了一项使用米托唑胺的II期试验，因为在临床前研究中，这种新型咪唑并四嗪已显示出对人黑色素瘤异种移植有良好效果。21例可评估的晚期恶性黑色素瘤患者接受了每6周口服115mg/m²米托唑胺的治疗。所有患者均未接受过先前的化疗。观察到2例部分缓解（缓解期分别为10个月和7个多月）。有反应的患者有肺转移，其中1例此外在腹股沟还有一个巨大的（17×14cm）淋巴结转移。另外，1例患者肺转移灶的肿瘤体积缩小了48%。治疗的剂量限制性副作用是骨髓抑制，伴有延迟性白细胞减少和血小板减少。白细胞计数中位数和血小板最低点分别为2.5×10⁹/L（范围1.1 - 3.8）和59×10⁹/L（范围14 - 95）。非血液学不良反应仅限于轻度或中度恶心。结论是口服米托唑胺对恶性黑色素瘤有活性，且似乎具有与最有效的现有药物相当的缓解率。
