University of Western Ontario, Schulich School of Medicine & Dentistry, London Health Sciences Centre-Victoria Hospital, Division of Urology, Department of Surgery, 800 Commissioners Road East, Room C3-120, London, Ontario N6A 5W9, Canada.
Expert Opin Investig Drugs. 2012 Feb;21(2):251-60. doi: 10.1517/13543784.2012.646081. Epub 2011 Dec 21.
Urothelial carcinoma of the bladder is a disease prone to recurrence. A new cytotoxic drug, apaziquone, is an analog of mitomycin C. Given via intravesical instillations it has the ability to specifically target cancer cells.
This article reviews the discovery and pharmacological properties of the agent and the first steps of its application in human disease. The poor performance of the drug as a systemic medication is discussed along with in vivo and in vitro studies that have led to current intravesical applications with encouraging results. In detail the limited number of clinical studies on the drug and compare them with relevant series on currently used agents. In addition, different strategies to enhance the efficacy of other agents are discussed and possible application of this experience to apaziquone is proposed.
Apaziquone is a promising local agent for the treatment and prevention of recurrent urothelial carcinoma of the bladder. The limited number of Phase II studies has demonstrated potency and relatively low toxicity. In light of the dearth of randomized controlled trials, Phase III studies are urgently needed before any conclusive pronouncements on this agent can be made.
膀胱癌是一种易复发的疾病。一种新型细胞毒素药物阿帕齐醌是丝裂霉素 C 的类似物。通过膀胱内灌注给予，它具有特异性靶向癌细胞的能力。
本文综述了该药物的发现和药理学特性及其在人类疾病中的初步应用。讨论了该药物作为全身药物的不良表现，以及导致目前膀胱内应用的体内和体外研究，这些应用取得了令人鼓舞的结果。详细介绍了该药物的少数临床研究，并将其与目前使用的药物的相关系列进行了比较。此外，还讨论了增强其他药物疗效的不同策略，并提出了将这些经验应用于阿帕齐醌的可能性。
阿帕齐醌是一种有前途的局部药物，可用于治疗和预防复发性膀胱癌。有限的 II 期研究表明其具有强大的疗效和相对较低的毒性。鉴于缺乏随机对照试验，在对此药物做出任何明确结论之前，迫切需要进行 III 期研究。
