Patel S R, Kvols L K, Rubin J, O'Connell M J, Edmonson J H, Ames M M, Kovach J S
Division of Medical Oncology, Mayo Clinic, Rochester, MN 55905.
Invest New Drugs. 1991 Feb;9(1):53-7. doi: 10.1007/BF00194545.
Pibenzimol is a fluorescent molecule known to bind to double stranded DNA. It also induces prolongation of the G2 phase of the cell cycle, inhibition of DNA replication and cessation of the growth of some cells in late S phase after DNA content has been doubled. It has been shown to increase the life span of mice bearing intraperitoneally implanted L1210 and P388 leukemia. These factors coupled with the affinity of pibenzimol for pancreatic tissue led us to conduct a phase I-II trial of pibenzimol hydrochloride in patients with advanced pancreatic cancer. Twenty-six patients were treated with a five day continuous infusion of pibenzimol at a dose ranging from 6-28 mg/m2/d. There were no treatment related deaths. Major toxicity was hyperglycemia which was self-limited. No objective responses were noted.
匹苯齐莫是一种已知能与双链DNA结合的荧光分子。它还能诱导细胞周期G2期延长，抑制DNA复制，并在DNA含量加倍后使一些处于S期后期的细胞停止生长。已证明它能延长腹腔内植入L1210和P388白血病的小鼠的寿命。这些因素加上匹苯齐莫对胰腺组织的亲和力，促使我们对晚期胰腺癌患者进行盐酸匹苯齐莫的I-II期试验。26例患者接受了为期5天的匹苯齐莫持续输注，剂量范围为6-28mg/m²/天。没有与治疗相关的死亡病例。主要毒性是高血糖，且具有自限性。未观察到客观缓解。
