Onrust S V, Lamb H M
Adis International Limited, Auckland, New Zealand.
Drugs Aging. 1999 Jul;15(1):69-75; discussion 76. doi: 10.2165/00002512-199915010-00006.
Valrubicin (AD-32) is an N-trifluoroacetyl, 14-valerate derivative of the anthracycline doxorubicin. It has antineoplastic activity which probably results from interference with nucleic acid metabolism by the drug. Valrubicin entered individual cells more rapidly than doxorubicin in vitro. When valrubicin was administered intravesically to patients with bladder cancer, cytotoxic concentrations of the drug penetrated the superficial muscle layer of the bladder. Complete response rates were 18 and 29% in patients with carcinoma in situ of the bladder which was refractory to intravesical BCG in 2 non-comparative trials of prophylactic intravesical valrubicin. In patients with recurrent superficial papillary tumours, the complete response rate was 46%. Adverse events were generally transient in patients who received intravesical valrubicin. Bladder irritation occurred in 88% of patients. Systemic absorption of intravesically administered valrubicin was minimal. Accordingly, systemic adverse events generally occurred in < or =5% of patients. Valrubicin was less toxic to chick embryos and haematopoietic stem cells in vitro and produced a lower incidence of cardiotoxicity in rabbits, compared with doxorubicin.
瓦鲁比星（AD - 32）是蒽环类药物阿霉素的N - 三氟乙酰基、14 - 戊酸酯衍生物。它具有抗肿瘤活性，这可能是由于该药物干扰核酸代谢所致。在体外，瓦鲁比星比阿霉素更迅速地进入单个细胞。当对膀胱癌患者进行膀胱内给药时，该药物的细胞毒性浓度可穿透膀胱浅肌层。在两项预防性膀胱内使用瓦鲁比星的非对照试验中，对膀胱内卡介苗治疗无效的原位膀胱癌患者的完全缓解率分别为18%和29%。在复发性浅表乳头状肿瘤患者中，完全缓解率为46%。接受膀胱内瓦鲁比星治疗的患者不良事件通常是短暂的。88%的患者出现膀胱刺激症状。膀胱内给药的瓦鲁比星全身吸收极少。因此，全身不良事件一般发生在≤5%的患者中。与阿霉素相比，瓦鲁比星在体外对鸡胚和造血干细胞的毒性较小，在兔中产生心脏毒性的发生率较低。
