Lee C R, Faulds D
Adis International Limited, Auckland, New Zealand.
Drugs. 1995 Jun;49(6):932-53. doi: 10.2165/00003495-199549060-00007.
Altretamine (hexamethylmelamine) is a cytotoxic antineoplastic agent which appears to require metabolic activation. Metabolic intermediates may act as alkylating agents; however, altretamine is not directly cross-resistant with classical alkylating agents. Objective response rates to orally administered altretamine as salvage therapy in patients with advanced ovarian cancer were 0 to 33%, with disease stabilisation in a further 8 to 78% of patients. Response rates appear to be higher in patients who have responded to previous alkylating agent or cisplatin-based therapy. There is some evidence that addition of altretamine to platinum-based combination regimens used for induction therapy of advanced ovarian cancer may improve long term survival, particularly in patients with limited residual disease. Although altretamine displays some activity in small cell lung cancer, it is unlikely to have any clinical role in the management of non-ovarian cancer. Altretamine appears to be relatively well tolerated, with gastrointestinal, neurological and haematological toxicities being the main dose-limiting adverse effects. However, assessment of accurate incidence rates for these effects is complicated by the use of altretamine with cisplatin. On the basis of the emerging body of clinical evidence, altretamine appears to have a limited role in the treatment of persistent or recurrent advanced ovarian cancer, primarily in patients who are potentially platinum sensitive yet intolerant of platinum analogues. Additionally, altretamine may be added to platinum-based regimens for induction therapy of advanced ovarian cancer. At the doses currently recommended, altretamine offers a reasonably well tolerated regimen that can be administered orally and is suitable for use on an outpatient basis.
六甲蜜胺是一种细胞毒性抗肿瘤药物，似乎需要代谢激活。代谢中间体可能作为烷化剂；然而，六甲蜜胺与经典烷化剂没有直接的交叉耐药性。对于晚期卵巢癌患者，口服六甲蜜胺作为挽救治疗的客观缓解率为0%至33%，另有8%至78%的患者病情稳定。对先前烷化剂或顺铂为基础的治疗有反应的患者缓解率似乎更高。有一些证据表明，在用于晚期卵巢癌诱导治疗的铂类联合方案中加入六甲蜜胺可能会提高长期生存率，特别是在残留病灶有限的患者中。虽然六甲蜜胺在小细胞肺癌中显示出一定活性，但在非卵巢癌的治疗中不太可能有任何临床作用。六甲蜜胺似乎耐受性相对较好，胃肠道、神经和血液学毒性是主要的剂量限制性不良反应。然而，由于六甲蜜胺与顺铂联合使用，准确评估这些不良反应的发生率较为复杂。基于新出现的临床证据，六甲蜜胺在持续性或复发性晚期卵巢癌的治疗中作用有限，主要用于可能对铂敏感但不耐受铂类类似物的患者。此外，六甲蜜胺可添加到铂类方案中用于晚期卵巢癌的诱导治疗。按照目前推荐的剂量，六甲蜜胺提供了一种耐受性较好的方案，可口服给药，适合门诊使用。
