【中文品名】曲洛司坦
【药效类别】脂皮质素合成抑制药
【通用药名】TRILOSTANE
【别　　名】Desopan, Modrastane, Modrenal, Triwinol, Win-14540
【化学名称】 Androst-2-ene-2-carbonitrile, 4,5-epoxy-3,17-dihydroxy-, (4α,5α,17β)-
【CA登记号】[13647-35-3]
【结 构 式】

【分 子 式】C20H27NO3
【分 子 量】329.433
【收录药典】
【开发单位】Sterling Drug
【首次上市】1980年，英国
【性　　状】
【用　　途】为一种3/6-羟类固醇脱氢酶/δ5-4异构酶的可逆性抑制剂，用于醛甾醇过多症和肾上腺皮质功能亢进。
【药理作用】
主要抑制皮质激素合成过程中的3β-脱氢酶，使皮质醇、醛固酮合成减少。本品也有明显的降低血睾酮水平作用，可能与抑制其合成有关。
【药 动 学】
本品口服吸收容易，血药浓度高峰约4h，代谢产物主要经尿排出。
【特    点】本身没有激素活性，故其副反应较少，安全性和耐受性也特别好。
【适 应 证】主要用于治疗库欣综合征(皮质醇增多症)和原发性醛固酮增多症，但治疗库欣综合征(皮质醇增多症)的疗效不如美替拉酮。晚期乳腺癌的治疗。
【禁 忌 证】肝、肾功能不良及孕妇不宜使用。       
【注意事项】用药期间应监测血皮质醇水平、电解质和血压。出现应激时应停药，必要时补充皮质激素。如同时使用保钾利尿药要注意发生高钾血症。          
【不良反应】不良反应较轻，部分病人可有脸红、恶心、呕吐、腹泻和胃肠不适。       
【用法用量】口服，每次60mg，2次/d。3～7天后，可根据病人对疗效反应调整剂量。一般的剂量范围是120～360mg/d，最大不超过480mg。

We currently market Modrenal(trilostane) in the U.K. for the treatment of post-menopausal advanced breast cancer following relapse to initial hormone therapy. We have a team of six sales specialists and two marketing executives selling and marketing Modrenal(and Evoltra) in the U.K.
Modrenal's approved indication enables us to promote Modrenal for use immediately after relapse to initial hormone therapy such as tamoxifen or one of a class of drugs known as aromatase inhibitors (including Faslodex and Arimidex). However, we are initially positioning Modrenal as a third or fourth line treatment option in post-menopausal advanced breast cancer.
In the five largest E.U. countries (France, Germany, Italy, Spain and the U.K.), we believe approximately 520,000 women are currently living with post-menopausal advanced breast cancer of which over a third require third or fourth line agents following prior treatment failure.
Modrenal has been extensively studied in clinical trials in the U.S., Europe and Australia, and an analysis, known as a meta-analysis, of a series of these clinical studies, that together included 714 patients with post-menopausal advanced breast cancer who received Modrenal has been conducted. Overall, a clinical benefit rate of 35% was achieved in patients with both hormone-sensitive and hormone-insensitive breast cancers. Generally, a clinical benefit is achieved when a patient's disease disappears, is decreased by greater than fifty percent or is stabilized for at least six months. In a sub-set analysis of these clinical trial data, a clinical benefit rate of 46% was achieved for 351 patients with hormone-sensitive breast cancer who had responded to one or more prior hormonal therapies and were given Modrenal upon relapse of the cancer. In one of the studies which was conducted in Australia , a clinical benefit rate of 55% was achieved for 64 patients who received Modrenal having previously responded to tamoxifen and subsequently relapsed. We believe these data compare favorably to currently marketed aromatase inhibitors and other agents given as second line or subsequent therapies. Furthermore, Modrenal® has an acceptable side-effect profile. On the basis of these data, Modrenal® was granted a product license in the U.K. for the treatment of post-menopausal advanced breast cancer following relapse to initial hormone therapy.
We began marketing Modrenal in May 2004 in the U.K. for the treatment of post-menopausal advanced breast cancer following relapse to initial hormone therapy. Our strategy may include seeking regulatory approval for Modrenal in the U.S. as a therapy for hormone-sensitive breast cancers and hormone independent prostate cancers, but this strategy is dependent upon the results of the ongoing clinical trials and the resource capability of the Company. Our ongoing clinical trials in breast cancer target patients that have hormone-sensitive cancers and have become refractory to prior hormone treatments, such as tamoxifen or any of the aromatase inhibitors. We will continue to develop our commercial and regulatory strategies for Modrenal® as we continue to analyze the results of these clinical data.
In mid-2005 we began enrollment in a U.K. , Phase IV study in post-menopausal advanced breast cancer, a Phase II study in pre-menopausal breast cancer and a Phase II study in neo-adjuvent, pre-operative breast cancer.
We plan to use the data from these clinical trials to support a filing process for mutual recognition for approval of Modrenal® on a country-by-country basis in Europe . Each such approval, if granted, would be based upon Modrenal's® approval in the U.K. for post-menopausal advanced breast cancer following relapse to initial hormone therapy.
The grant of any such approval is entirely within the control of the individual regulatory authorities.
We have the exclusive right to market and distribute Modrenal® throughout the world for all human applications, except for South Africa and Japan where the drug is marketed for the treatment of low-renin hypertension. Our exclusive license expires upon the last to expire of the patents used or useful in connection with the marketing of Modrenal. Given that we have new patent applications filed, which are subject to issuance, we expect the last of our underlying patents to expire in 2020.

曲洛司坦（Trilostane）由生技公司Bioenvision开发的一种新型作用机制的抗雌激素新药，以Modrenal的商品名上市，于2002年8月在英国首次正式获得了用于绝经后妇女进行性乳腺癌，曲洛司坦本身没有激素活性，其治疗相关副反应较少，安全性和耐受性颇好。
目前，对绝经后激素受体阳性或不明类型乳腺癌患者，临床一致推荐首选抗雌激素药物予以治疗，而此疗法在延缓患者疾病进展、提高存活时间方面的作用也早已得到大量研究的肯定与确认。乳腺癌属激素依赖性肿瘤，而雌激素则是此癌细胞生长的主要驱动因子。乳腺癌的现代主要疗法之一就是靶向雌激素，通过抑制雌激素生产或在其作用位点即雌激素受体环节阻断雌激素的作用。曲洛司坦除能降低雌激素的生产外，还可调节雌激素对不同亚型雌激素受体的结合，同时显现α-雌激素受体抑制剂和β-雌激素受体激动剂的双重效应，最终阻滞和改变雌激素对癌细胞的负性影响。曲洛司坦独特的作用模式不仅使它区别于现有的其他抗雌激素药物，而且也是它对经其他抗雌激素疗法治疗失败或耐药乳腺癌仍然高度有效的药理学基础。作为一种新型作用机制的抗雌激素新药，用于治疗乳腺癌，曲洛司坦可能是晚期乳腺癌病人的一个新选择。
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原产地英文药品名:
TRILOSTANE
中文参考商品译名:
MODRENAL 120毫克/胶囊 100胶囊/盒
中文参考药品译名:
曲洛司坦
生产厂家中文参考译名:
健赞
生产厂家英文名:
Genzyme
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原产地英文药品名:
TRILOSTANE
中文参考商品译名:
MODRENAL 60毫克/胶囊 100胶囊/盒
中文参考药品译名:
曲洛司坦
生产厂家中文参考译名:
健赞
生产厂家英文名: