曲昔匹特作为第二代喹啉-3-甲酰胺类口服抗血管生成药物用于前列腺癌治疗的漫长曲折之路。

The long and winding road for the development of tasquinimod as an oral second-generation quinoline-3-carboxamide antiangiogenic drug for the treatment of prostate cancer.

机构信息

The Johns Hopkins University, Baltimore, MD 21287, Maryland, USA.

出版信息

Expert Opin Investig Drugs. 2010 Oct;19(10):1235-43. doi: 10.1517/13543784.2010.514262.

Abstract

IMPORTANCE OF THE FIELD

Prostate cancer is the mostly commonly diagnosed non-skin cancer in males. The culmination of the last 70 years of clinical drug development has documented that androgen ablation plus taxane-based systemic chemotherapy enhances survival, but is not curative, in metastatic prostate cancer. To effect curative therapy, additional drugs must be developed that enhance the response when combined with androgen ablation/taxane therapy.

AREAS COVERED IN THIS REVIEW

The history of the discovery and development of tasquinimod as a second-generation oral quinoline-3-carboxamide analogue for prostate cancer will be presented.

WHAT THE READER WILL GAIN

The mechanism for such anticancer efficacy is via tasquinimod's ability to inhibit the 'angiogenic switch' within cancer sites required for their continuous lethal growth.

TAKE HOME MESSAGE

Tasquinimod is a novel inhibitor of tumor angiogenesis that enhances the therapeutic anticancer response when combined with other standard-of-care modalities (radiation, androgen ablation, and/or taxane-based chemotherapies) in experimental animal models, but does not inhibit normal wound healing. It has successfully completed clinical Phase II testing in humans and will shortly enter registration Phase III evaluation for the treatment of metastatic prostate cancer.

摘要

重要性领域

前列腺癌是男性最常见的非皮肤癌。过去 70 年临床药物开发的成果表明,雄激素剥夺加紫杉烷类药物系统化疗可提高转移性前列腺癌的生存率,但不能治愈。为了实现治愈性治疗,必须开发出额外的药物,以增强与雄激素剥夺/紫杉烷治疗联合使用时的反应。

本综述涵盖的领域

本文将介绍 tasquinimod 作为第二代口服喹啉-3-甲酰胺类似物在前列腺癌中的发现和开发历程。

读者将获得的收益

这种抗癌疗效的机制是通过 tasquinimod 抑制癌症部位持续致命生长所需的“血管生成开关”。

结论

tasquinimod 是一种新型的肿瘤血管生成抑制剂,在实验动物模型中与其他标准治疗方法(放疗、雄激素剥夺和/或紫杉烷类化疗)联合使用时,可增强治疗抗癌反应,但不抑制正常伤口愈合。它已在人体中成功完成了临床 II 期试验,很快将进入转移性前列腺癌治疗的注册 III 期评估。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索