Belgrad R, Wampler G L
Int J Radiat Oncol Biol Phys. 1982 Jul;8(7):1219-23. doi: 10.1016/0360-3016(82)90071-2.
Ethyl bis (2,2 dimethyl-1-aziridinyl) phosphinate (AB-163), a TEPA analogue, was used with radiation therapy in treating 18 patients with advanced malignancies. There were 12 patients with esophageal carcinoma; 3 with adenocarcinomas of the gastrointestinal tract; one, squamous carcinoma of the cervix; and one, adenocarcinoma of the ovary. One hundred mg/M2 AB-163 was given by rapid i.v. drip one half-hour before conventional radiation therapy. The majority of patients received 10 combined treatments. Three of those with squamous cell carcinomas (two in the esophagus and one in the cervix) remained disease-free for more than 2 years. One with liver metastasis and unresectable carcinoma of the stomach survived for 9 months. The drug causes side effects mainly involving the central nervous system and gastrointestinal tract. Drug-related myelosuppression has not been observed. The mode of action is speculated to be a result of active intermediate hydrolysis products which appear capable of phosphorylating X ray induced DNA strand damage. However, much additional investigation is required, both in vitro and clinically, before its efficacy and safety can be demonstrated.
双（2,2-二甲基-1-氮丙啶基）次膦酸乙酯（AB - 163），一种三乙烯磷酰胺类似物，与放射治疗联合用于治疗18例晚期恶性肿瘤患者。其中有12例食管癌患者；3例胃肠道腺癌患者；1例子宫颈鳞状细胞癌患者；1例卵巢腺癌患者。在常规放射治疗前半小时，通过快速静脉滴注给予100mg/M²的AB - 163。大多数患者接受了10次联合治疗。3例鳞状细胞癌患者（2例在食管，1例在子宫颈）无病生存超过2年。1例有肝转移且不可切除的胃癌患者存活了9个月。该药物的副作用主要累及中枢神经系统和胃肠道。尚未观察到与药物相关的骨髓抑制。其作用模式推测是活性中间水解产物的结果，这些产物似乎能够使X射线诱导的DNA链损伤磷酸化。然而，在证明其疗效和安全性之前，还需要进行大量的体外和临床研究。
