Khayat D, Giroux B, Berille J, Cour V, Gerard B, Sarkany M, Bertrand P, Bizzari J P
Hôpital Pitié Salpétrière, Service d'Oncologie Médicale, France.
Cancer Invest. 1994;12(4):414-20. doi: 10.3109/07357909409038234.
Fotemustine is a new chloroethylnitrosourea characterized by the grafting of a phosphonoalanine group onto a nitrosourea radical. Clinical studies using fotemustine have been conducted in malignant glioma, brain metastasis of non-small cell lung cancer, and disseminated malignant melanoma. In recurrent malignant glioma, fotemustine has been used as a single agent: assessed by computed tomography scan, after 8 weeks, the objective response rate was 26.3% among 38 evaluable patients. Median duration of response was 33 weeks. The main toxicity was hematological (thrombocytopenia and leucopenia). A trial with high-dose fotemustine and autologous bone marrow rescue in newly diagnosed glioma was conducted in 26 patients, and 6 showed a partial response. The median overall survival was approximately 11 months. Myelosuppression was noted in all patients except 1, and other toxicity reported was central nervous system toxicity and epigastric pain. Combined with radiotherapy in 55 patients, a 29% response rate was observed, and this combination was well tolerated and easily manageable on an outpatient basis. Finally, fotemustine has been used intraarterially, with 10 objective responses observed among 26 evaluable patients. In brain metastases of non-small cell lung cancer, fotemustine proved to be active with a response rate of 16.7%. Combined with cisplatinum, fotemustine is still under study, but preliminary results are promising. In cerebral metastases of disseminated malignant melanoma, fotemustine has been evaluated in a total of 140 patients in the various studies: median response rate is 24.3%, ranging from 8.3% to 60.0%. Fotemustine appears to be a good candidate in the treatment of primary brain tumors and metastases.
福莫司汀是一种新型氯乙基亚硝脲，其特点是在亚硝脲基团上接枝了一个膦酰丙氨酸基团。使用福莫司汀的临床研究已在恶性胶质瘤、非小细胞肺癌脑转移和播散性恶性黑色素瘤中开展。在复发性恶性胶质瘤中，福莫司汀已作为单一药物使用：通过计算机断层扫描评估，8周后，38例可评估患者中的客观缓解率为26.3%。中位缓解持续时间为33周。主要毒性为血液学毒性（血小板减少和白细胞减少）。一项针对新诊断的胶质瘤患者使用高剂量福莫司汀和自体骨髓挽救的试验纳入了26例患者，其中6例出现部分缓解。中位总生存期约为11个月。除1例患者外，所有患者均出现骨髓抑制，报告的其他毒性为中枢神经系统毒性和上腹部疼痛。55例患者联合放疗，观察到缓解率为29%，这种联合耐受性良好，在门诊即可轻松管理。最后，福莫司汀已通过动脉内给药，26例可评估患者中有10例出现客观缓解。在非小细胞肺癌脑转移中，福莫司汀被证明具有活性，缓解率为16.7%。与顺铂联合使用时，福莫司汀仍在研究中，但初步结果很有前景。在播散性恶性黑色素瘤的脑转移中，福莫司汀在各项研究中总共评估了140例患者：中位缓解率为24.3%，范围为8.3%至60.0%。福莫司汀似乎是治疗原发性脑肿瘤和转移瘤的良好选择。
