Valrubicin
Valrubicin
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DOI：
10.2165/00002512-199915010-00006
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发表时间：
1999-07-01
期刊：
影响因子：
2.8
通讯作者：
Lamb, HM
中科院分区：
文献类型：
--
作者：
Onrust, SV;Lamb, HM
Valruicin(AD-32)是一种三氟乙酰，14-戊酸酯类化合物，是蒽环素阿霉素的衍生物。它具有抗肿瘤活性，这可能是由于药物干扰了核酸的代谢。在体外，Valruicin比阿霉素更快地进入个体细胞。膀胱癌患者膀胱内注射呋喃鲁比星后，药物的细胞毒浓度可穿透膀胱浅肌层，对卡介苗无效的原位膀胱癌患者的完全缓解率分别为18%和29%，2次预防性膀胱内注射的完全缓解率为29%。在复发的浅表乳头状肿瘤患者中，完全缓解率为46%，接受Valruicin膀胱内注射的患者不良反应通常是短暂的。88%的患者出现膀胱刺激。膀胱内给药的全身吸收极小。因此，全身不良事件的发生率一般小于或等于5%。与阿霉素相比，Valruicin在体外对鸡胚胎和造血干细胞的毒性较小，对兔的心脏毒性发生率较低。
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 noncomparative 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 less than or equal to 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.