三种阿霉素治疗方法的比较：游离阿霉素、脂质体阿霉素和β-葡萄糖醛酸酶激活前药（HMR 1826）。
Comparison of three approaches to doxorubicin therapy: free doxorubicin, liposomal doxorubicin, and beta-glucuronidase-activated prodrug (HMR 1826).
作者信息
Woessner R, An Z, Li X, Hoffman R M, Dix R, Bitonti A
机构信息
Aventis Pharmaceuticals, Bridgewater, NJ 08807, USA.
出版信息
Anticancer Res. 2000 Jul-Aug;20(4):2289-96.
BACKGROUND
Three approaches to doxorubicin therapy are directly compared: free doxorubicin, liposomal doxorubicin and beta-glucuronidase-activated prodrug (HMR 1826).
MATERIALS AND METHODS
The optimal dose of HMR 1826 was determined to be 200 mg/kg once a week and subsequent studies were carried out comparing HMR 1826 at 200 mg/kg 1x/wk, liposomal doxorubicin (Doxil) at 9 mg/kg 1x/wk and free doxorubicin at 7 mg/kg 1x/wk in seven different human tumor xenograft models.
RESULTS
All three forms of doxorubicin inhibited tumor growth with similar efficacy in each of the tumor models with the exception of MDA-MB-231 tumor xenografts, which were resistant to free doxorubicin but sensitive to Doxil and HMR 1826. Overall less weight loss was observed with HMR 1826 treatment.
CONCLUSIONS
The efficacy of HMR 1826 is equal to or better than that of doxorubicin and Doxil at a safe dose and schedule, indicating that the beta-glucuronidase activated prodrug approach is safe and effective.
背景
直接比较了阿霉素治疗的三种方法：游离阿霉素、脂质体阿霉素和β-葡萄糖醛酸酶激活前药（HMR 1826）。
材料与方法
确定HMR 1826的最佳剂量为每周一次200mg/kg，随后在七种不同的人肿瘤异种移植模型中进行研究，比较每周一次200mg/kg的HMR 1826、每周一次9mg/kg的脂质体阿霉素（多美素）和每周一次7mg/kg的游离阿霉素。
结果
除MDA-MB-231肿瘤异种移植对外源性游离阿霉素耐药但对多美素和HMR 1826敏感外，三种形式的阿霉素在每种肿瘤模型中均以相似的疗效抑制肿瘤生长。总体而言，HMR 1826治疗观察到的体重减轻较少。
结论
在安全剂量和给药方案下，HMR 1826的疗效等于或优于阿霉素和多美素，表明β-葡萄糖醛酸酶激活前药方法是安全有效的。
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