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美国(FDA)核准degarelix注射剂两种新剂用于治疗末期前列腺癌

2010-10-22 16:43:04 作者：新特药房来源：中国新特药网天津分站浏览次数：296 文字大小：【大】【中】【小】

简介： 2008年12月29日，FDA宣布批准治疗前列腺癌的新药Degarelix在美国上市，它是近年来FDA首个批准用于治疗前列腺癌的新药。这种新型注射剂主要针对晚期前列腺癌患者，它属于“促性腺激素释放激素（GnRH）” ...

2008年12月29日，FDA宣布批准治疗前列腺癌的新药Degarelix在美国上市，它是近年来FDA首个批准用于治疗前列腺癌的新药。这种新型注射剂主要针对晚期前列腺癌患者，它属于“促性腺激素释放激素（GnRH）”受体抑制剂类药物，通过抑制睾丸激素来延缓前列腺癌的病程发展。

前列腺癌是美国最为常见的癌症之一，是美国男性的第二大‘癌症杀手’。据最新数据显示，在2004年，美国大约有190，000名男性被诊断患有前列腺癌，其中29，000人死亡。

先前已有的治疗前列腺癌激素疗法的特点是“先升后降”，即在治疗初期，某些疗法会导致患者的睾丸激素水平激增，然后才会显现疗效，降低睾丸激素水平。这意味着在治疗初期，肿瘤可能非但未受到抑制，反而被刺激生长。而Degarelix从一开始就能产生疗效，不会导致常见的睾丸激素“先升后降”现象。

在该药的III期临床试验中，对比了degarelix（每月用药一次）和标准药物（leuprorelin）治疗前列腺癌的疗效，疗程为期12个月，两组受试者病情情况等同。结果表明，degarelix能更快控制血清睾酮水平和前列腺特异抗原（PSA），并且该药能在12个月的观察期内保持上述疗效。Degarelix在临床研究中最常观察到的副作用除注射部位反应（疼痛，红肿）外，还有潮热，体重增加、乏力以及部分肝酶指标增加。

前列腺癌新药degarelix在III期临床中表现良好

Degarelix可快速降低前列腺癌男性的睾酮水平

根据欧洲泌尿学会协会第21届会议上的一项报告，Degarelix，一种用于前列腺癌激素治疗的新的促性腺激素释放激素（GnRH ）阻断剂，可引起睾酮和前列腺特异性抗原（PSA）水平持续降低，而且没有开始的睾酮波动。

比利时Catholic大学的Hein Van Poppel博士及其同事对187例男性进行了为期1年的研究。他们评估了Degarelix 200mg和240mg作为起始剂量进行皮下注射，以及80，120 和160mg三个维持剂量的治疗作用。

Van Poppel博士说，最重要的结果是，接受240 mg起始剂量的93%的患者在3天内睾酮在去雄水平以下，几乎所有患者在1个月内达到雄激素剥夺，所有患者都未出血睾酮波动。从28天直至1年，每月测量的去雄水平在接受160mg维持剂量的所有患者、在接受120mg维持剂量的96%的患者和接受80mg维持剂量的92%的患者中持续存在。PSA水平在初始治疗后8周降低90%，治疗12周后降低94%，治疗24周后降低96%。

Van Poppel博士说：“这些数据说明我们发现了degarelix的初始和维持剂量。我们目前需要与促黄体生成激素释放激素（LHRH）促效剂进行比较，这是我们所计划的III期研究内容。”

治疗前列腺癌的新型药物degarelix将在美国上市

据悉，FDA已批准美国Ferring制药公司出品的前列腺癌治疗新药degarelix,，该药为注射剂，属促性腺激素释放激素受体拮抗剂，主要用于晚期前列腺癌患者。这种新型药物的商品名目前还处在FDA的审批阶段，一旦它的商品名最后通过批准，Ferring公司将立即在美国市场推出该药。此前，欧洲人用医疗产品委员会也已同意degarelix在欧洲上市。目前，该药也正在等待全球其他主要药品市场的销售批准。Ferring相关负责人称，degarelix的最初研发地点位于圣地亚哥，后由Ferring在美国及欧洲的公司开发。该药在关键的III期临床实验中获得的数据显示，它起效快，并且在长期抑制睾丸激素和前列腺特异抗原方面的效果非常显著。

FDA批准治疗晚期前列腺癌的新药Degarelix上市

2008年12月29日，FDA宣布批准治疗前列腺癌的新药Degarelix在美国上市，它是近年来FDA首个批准用于治疗前列腺癌的新药。前列腺癌是美国最为常见的癌症之一。

据最新数据显示，在2004年，美国大约有190，000名男性被诊断患有前列腺癌，其中29，000人死亡。美国药品评价与研究中心，肿瘤办公室主任，医学博士Richard Pazdur表示“前列腺癌是美国男性的第二大‘癌症杀手’，这些患者需要更多的治疗选择。” 这种新型注射剂主要针对晚期前列腺癌患者，它属于“促性腺激素释放激素（GnRH）”受体抑制剂类药物，通过抑制睾丸激素来延缓前列腺癌的病程发展。先前已有的治疗前列腺癌激素疗法的特点是“先升后降”，即在治疗初期，某些疗法会导致患者的睾丸激素水平激增，然后才会显现疗效，降低睾丸激素水平。这意味着在治疗初期，肿瘤可能非但未受到抑制，反而被刺激生长。而Degarelix从一开始就能产生疗效，不会导致常见的睾丸激素 “先升后降”现象。Degarelix在临床研究中最常观察到的副作用除注射部位反应（疼痛，红肿）外，还有潮热，体重增加、乏力以及部分肝酶指标增加。

美药管局批准一种治疗晚期前列腺癌新药

新华网华盛顿１２月２９日电美国食品和药物管理局２９日宣布，一种治疗晚期前列腺癌的新药Ｄｅｇａｒｅｌｉｘ获准在美国上市，这是美药管局７年来首次批准治疗前列腺癌的新药上市。这种新型注射药剂主要针对晚期前列腺癌患者，它属于“促性腺激素释放激素（ＧｎＲＨ）”受体抑制剂类药物，通过抑制睾丸激素来延缓前列腺癌病程发展。美药管局负责肿瘤学药物产品的官员理查德•帕兹杜尔当天在新闻公报中说，前列腺癌是美国男性的第二大“癌症杀手”，“这些患者需要更多的治疗选择”。据美国媒体报道，此前一些激素疗法的特点是“先升后降”，即在治疗初期，某些疗法会导致患者的睾丸激素水平激增，然后才会显现疗效，降低睾丸激素水平。这意味着在治疗初期，肿瘤可能非但未被抑制，反而会刺激生长。而Ｄｅｇａｒｅｌｉｘ从一开始就能抑制前列腺癌。

前列腺癌是男性中最常见的癌症类型之一。

据美媒体报道，在２００４年，美国有近１９万名男性被诊断患上前列腺癌，另有２．９万名患者死于这种疾病。

目前治疗前列腺癌的疗法除激素疗法外，还有前列腺切除术、放疗和化疗等。

On December 24, 2008, the U. S. Food and Drug Administration (FDA) approved degarelix for injection (Ferring Pharmaceuticals Inc., Parsippany, NJ), a new gonadotropin releasing hormone (GnRH) receptor antagonist, for the treatment of patients with advanced prostate cancer. This indication is based on degarelix’s effectiveness in attaining and maintaining serum testosterone suppression to medical castration levels during 12 months of treatment in an open-label, randomized, multi-center, parallel-group study.
A total of 620 patients were randomized to receive one of two degarelix dosing regimens or leuprolide for one year: degarelix at a starting dose of 240 mg followed by monthly doses of 160 mg subcutaneously, degarelix at a starting dose of 240 mg followed by monthly doses of 80 mg subcutaneously, or monthly doses of leuprolide 7.5 mg intramuscularly. The primary objective was to demonstrate that degarelix is effective in achieving and maintaining testosterone suppression to castration levels ( ≤ 50 ng/dL) during 12 months of treatment. The medical castration rates were 98.3% (95% CI: 94.8%; 99.4%) in the degarelix 240/160 mg arm, 97.2% (95% CI: 93.5%; 98.8%) in degarelix 240/80 mg arm, and 96.4% (95% CI: 92.5%; 98.2%) in the leuprolide 7.5 mg arm. The key secondary analyses showed that no testosterone surges were observed in the degarelix arms and that 96% of patients attained medical castration 3 days after the first degarelix dose compared to no patients receiving leuprolide.
The most commonly observed adverse reactions (frequency of <10%) in either degarelix arm included injection site reactions (e.g., pain, erythema, swelling or induration), hot flashes, weight increase, and increases in transaminases and gamma-glutamyltransferase. The majority of the adverse reactions were grade 1/2 in severity; grade 3/4 adverse reactions were uncommon. The injection site reactions were transient, with frequencies of 35-44% in the degarelix arms compared to a frequency of <1% in the leuprolide arm. Hepatic laboratory abnormalities were generally reversible, with grade 3 abnormalities in less than 1% of patients. There were no important differences in adverse reactions between the two degarelix arms, except for fewer injection site reactions in the 240/80 mg arm.

The recommended dosing regimen is a starting dose of 240 mg given as two subcutaneous injections of 120 mg each followed by monthly maintenance doses of 80 mg given as a single subcutaneous injection.
Full prescribing information, including clinical trial information, safety, dosing, drug-drug interactions and contraindications is available at
FDA Approves Degarelix
The U.S. Food and Drug Administration (FDA) has approved degarelix, an injectable gonadotropin-releasing hormone (GnRH) receptor antagonist, indicated for patients with advanced prostate cancer. Potential trade names are still under review with the FDA.
Phase III studies showed that degarelix is at least as effective as leuprolide (Lupron Depot(R)) in sustaining castrate levels or lower of testosterone, and had a statistically significant faster reduction of testosterone. At Day 3 of treatment, 96% of degarelix patients achieved castrate levels of testosterone, compared with zero percent receiving leuprolide. By Day 14, 99% of degarelix patients achieved castrate levels of testosterone, compared with 18% receiving leuprolide.
In the clinical trial, prostate specific antigen (PSA) levels were also monitored as a secondary endpoint. PSA levels were lowered by 64% two weeks after administration of degarelix, 85% after one month, 95% after three months, and remained suppressed throughout the one year of treatment. These PSA results should be interpreted with caution because of the heterogeneity of the patient population studied. No evidence has shown that the rapidity of PSA decline is related to a clinical benefit.
Prostate cancer is known to grow in the presence of testosterone. Suppression of testosterone has been a treatment goal for advanced prostate cancer for many years. Surgical castration was the standard method of reducing testosterone from the 1940s until the mid-1980s when the earliest forms of medical castration, luteinizing hormone releasing hormone (LHRH) agonists, were introduced.
Degarelix is the only GnRH receptor antagonist approved by the FDA for the treatment of hormonally-sensitive advanced prostate cancer. Degarelix achieves medical castration differently than LHRH agonists, specifically by binding reversibly to GnRH receptors on cells in the pituitary gland, quickly reducing the release of gonadotropins and consequently testosterone.
Overall, the most commonly observed adverse reactions during degarelix therapy included injection site reactions (e.g. pain, erythema, swelling or induration), hot flushes, increased weight, fatigue, and increases in serum levels of transaminases and gamma-glutamyltransferase (GGT). 99% of these observed adverse reactions were Grade 1 or 2 (mild to moderate). Specifically relating to the injection site adverse reactions, most were transient, of mild to moderate intensity, occurred primarily with the starting dose and led to few discontinuations (<1%). Grade 3 (severe) injection site reactions occurred in 2% or less of patients receiving degarelix. Degarelix is contraindicated in patients with known hypersensitivity to degarelix or to any of the product components. Degarelix is not indicated in women or pediatric patients. Long-term androgen deprivation therapy prolongs the QT interval. Physicians should consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients with congenital long QT syndrome, electrolyte abnormalities, or congestive heart failure and in patients taking Class IA (e.g. quinidine, procainamide) or Class III (e.g. amiodarone,sotalol) antiarrhythmic medications.
Degarelix Paitent InformationRead this patient information leaflet before you start taking degarelix and each time you get a refill.
There may be new information. This information does not take the place of talking to your healthcare provider about your medical condition or your treatment.
What is degarelix?
Degarelix is a prescrpition medicine used in the treatment of advanced prostate cancer.
It is not known if degarelix is safe or effective in children.
Who should not use degarelix?
Degarelix should not be given to:
• people who are allergic to any of the other ingredients in degarelix. See the end of this leaflet for a complete list of ingredients in degarelix
• women who are pregnant or may become pregnant
Talk to your healthcare provider before getting degarelix if you have any of these conditions.
What should I tell my healthcare provider before receiving degarelix?
Before receiving degarelix, tell your healthcare provider about all your medical conditions, including if you:
• have any heart problems
• have problems with balance of your body salts or electrolytes, such as sodium, potassium, calcium,and magnesium
• have kidney or liver problems
• are breast-feeding or plan to breast-feed. It is not known if degarelix passes into your breast milk. You and your healthcare provider should decide if you will take degarelix or breast feed. You should not do both without talking with your healthcare provider.
Tell your healthcare provider about all the medicines you take, including prescription and nonprescription medicines, vitamins, and herbal supplements. Especially tell your healthcare provider if you are taking or have taken any medicines for your heart.
Know the medicines you take. Keep a list of them and show it to your healthcare provider and pharmacist when you get a new medicine.
How should I receive degarelix?
• You will receive an injection of degarelix from your healthcare provider.
• The injection site will always be in the abdominal area but will change within that area with the next doses of degarelix.
• The injected medicine gives you a continuous release of degarelix over one month.
• Two injections are given as a first dose and the following monthly doses are one injection.
• Make sure your injection site is free of any pressure from belts, waistbands or other types of clothing.
• Always set up an appointment for your next injection.
• If you miss a dose of degarelix, or if you think you forgot to get your monthly dose of degarelix, talk to your healthcare provider about how to get your next dose.
What are the possible side effects of degarelix?
The common side effects include:
• hot flashes
• injection site pain, redness, and swelling, especially with the first dose
• weight gain
• increase in some liver enzymes
• tiredness
• hypertension
• back and joint pain
• chills
• urinary tract infection
• decreased sex drive and trouble with erectile function (impotence)
These are not all the possible side effects. For more information, ask your healthcare provider or pharmacist.
Tell your healthcare provider if you have any side effect that bothers you or that does not go away.
Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
General information about the safe and effective use of degarelix.
Medicines are sometimes prescribed for conditions that are not mentioned in the patient leaflet. Do not use degarelix for a condition for which it was not prescribed. Do not give degarelix to other people, even if they have the same symptoms that you have. It may harm them.
This patient information leaflet summarizes the most important information about degarelix. If you would like more information, talk with your healthcare provider. You can ask your pharmacist or healthcare provider for information about degarelix that is written for health professionals.
For more information, call 1-888-FERRING (1-888-337-7464)
What are the ingredients in degarelix?
Active ingredient: degarelix (as acetate)
Inactive ingredient: mannitol
FDA核准： Fludarabine Phosphate 与 Degarelix

美国食品药物管理局(FDA)核准degarelix注射剂两种新剂量，用于治疗末期前列腺癌。
　　
【Degarelix核准用于治疗末期前列腺癌】
2008年12月24日，FDA核准degarelix (Ferring药厂) 80-mg和120-mg注射剂，用于治疗末期前列腺癌病患。Degarelix是新的促性腺激素释放荷尔蒙受体拮抗剂，可逆性结合到脑垂体促性腺激素释放荷尔蒙受体，减少睪固酮之释出。
　　
Degarelix之核准是根据一个开放标籤、多中心随机平行小组研究，对象是前列腺癌病患(N = 620)；随机指派接受两种degarelix剂量之一或者leuprolide，为期一年：degarelix开始剂量240 mg、之后每月剂量160 mg、皮下给药，degarelix开始剂量240 mg、之后每月剂量80 mg、皮下给药，或者每月leuprolide 7.5 mg肌肉注射给药。
　　
研究的初级目标是检视degarelix 在12个月治疗期间，达到维持睪固酮抑制到去势程度(≦ 50 ng/dL)的效果。结果显示，平均去势率：degarelix 240/160-mg组为98.3% (95%信心区间94.8% - 99.4%) ，degarelix 240/80-mg组为 97.2% (95%信心区间93.5% - 98.8%) ，leuprolide 7.5-mg组为 96.4% (95%信心区间92.5% - 98.2%)。degarelix组没有测得睪固酮波，96%病患在初次degarelix剂量之后3天达到去势，leuprolide组是0%。
　　
以degarelix治疗的1,325名病患中，最常见的不良反应包括暂时性注射位置反应、热潮红、体重增加、转胺酶与珈玛麩胺酸转胜酵素（gamma-glutamyltransferase）值增加。
　　
Degarelix 的疗效应以週期性监测血清前列腺特定抗原值来监控，此外，长期雄性素去除疗法会延长QT 间隔。对于先天QT间隔长的病患、电解质异常病患、或者先天性心衰竭与服用IA类 (例如quinidine procainamide)或第三类(例如amiodarone) 抗心律不整药物者，医师应考量长期雄性素去除疗法之治疗利益与风险。

　　
Degarelix只可以皮下给药。建议剂量是开始剂量240 mg、分开以120 mg给予，接著是每28天给予一次80mg维持剂量
Degarelix approved for advanced prostate cancer
Date Posted: December 29, 2008
Degarelix (injectable gonadotropin-releasing hormone (GnRH) receptor antagonist, from Ferring Pharmaceuticals) has been approved by the FDA for treatment of hormonally-sensitive advanced prostate cancer. This approval was based on results from a Phase III, 12-month, randomized, open-label, parallel-group clinical trial comparing degarelix with monthly leuprolide in patients with histologically confirmed prostate cancer. The study showed degarelix to be at least as effective as leuprolide in achieving and maintaining castrate levels of testosterone.

前列腺癌新药degarelix在III期临床中表现良好

有专家表示，III期临床试验结果显示，Ferring公司的新型前列腺癌治疗药degarelix取得了突破性效果。
在该药的III期临床试验中，对比了degarelix（每月用药一次）和标准药物（leuprorelin）的疗效，疗程为期12个月，两组受试者病情情况等同。结果表明，degarelix能更快控制血清睾酮水平和前列腺特异抗原（PSA），并且该药能在12个月的观察期内保持上述疗效。
有负责人称，degarelix临床试验终点数据还未出来，但就该药对PSA水平的快速控制可以延长患者的存活时间。试验也证实，这种新药的耐受性至少与目前标准治疗药物相当。值得指出的是，患者用药后，它未引起严重的全身性不良反应。
FDA Approves Ferring Pharmaceuticals' Degarelix (Generic Name) for Treatment of Advanced Prostate Cancer
PARSIPPANY, New Jersey, December 24 /PRNewswire/ --- New Gonadotropin-Releasing Hormone (GnRH) Receptor Antagonist Demonstrates Rapid, Long-term Suppression of Testosterone - a hormone that stimulates prostate cancer growth.
Ferring Pharmaceuticals, USA today received approval from the U.S. Food and Drug Administration (FDA) for degarelix, a new injectable gonadotropin-releasing hormone (GnRH) receptor antagonist, indicated for patients with advanced prostate cancer. Potential trade names are still under review with the FDA. Following issuance of a trade name, Ferring Pharmaceuticals, USA will immediately begin commercialization in the U.S. On December 18, the Committee for Medicinal Products for Human Use (CHMP), part of the European Medicines Agency (EMEA), recommended granting a marketing authorization for degarelix in Europe. Degarelix is awaiting approval in other key global markets. It is a milestone for the company and represents Ferring's first global product launch.
Phase III studies showed that degarelix is at least as effective as leuprolide (Lupron Depot(R)) in sustaining castrate levels or lower of testosterone, and had a statistically significant faster reduction of testosterone. At Day 3 of treatment, 96% of degarelix patients achieved castrate levels of testosterone, compared with zero percent receiving leuprolide. By Day 14, 99% of degarelix patients achieved castrate levels of testosterone, compared with 18% receiving leuprolide.
In the clinical trial, prostate specific antigen (PSA) levels were also monitored as a secondary endpoint. PSA levels were lowered by 64% two weeks after administration of degarelix, 85% after one month, 95% after three months, and remained suppressed throughout the one year of treatment.

These PSA results should be interpreted with caution because of the heterogeneity of the patient population studied. No evidence has shown that the rapidity of PSA decline is related to a clinical benefit.
Prostate cancer is known to grow in the presence of testosterone. Suppression of testosterone has been a treatment goal for advanced prostate cancer for many years. Surgical castration was the standard method of reducing testosterone from the 1940s until the mid-1980s when the earliest forms of medical castration, luteinizing hormone releasing hormone (LHRH) agonists, were introduced.
Degarelix is the only GnRH receptor antagonist approved by the FDA for the treatment of hormonally-sensitive advanced prostate cancer. Degarelix achieves medical castration differently than LHRH agonists, specifically by binding reversibly to GnRH receptors on cells in the pituitary gland, quickly reducing the release of gonadotropins and consequently testosterone.
Degarelix was discovered in San Diego, developed by Ferring Pharmaceuticals in the U.S. and Europe, and in its pivotal Phase III study demonstrated both an immediate onset of action and a profound long-term suppression of testosterone and PSA, commented Dr. Pascal Danglas, Executive Vice President Clinical Product Development, at Ferring. We are delighted to deliver a new treatment option for advanced prostate cancer to the medical community. Ferring has a considerable pipeline of urology products in development, and we expect to introduce additional treatment advances in the urology field in the near future.
Use of a GnRH receptor antagonist is a highly efficient way to stop the production of testosterone, said Neal Shore, MD, FACS, Medical Director for Carolina Urologic Research Center, a clinical trial investigator and advisor to Ferring. The approval of degarelix offers the medical community an effective alternative in the treatment of hormonally-sensitive prostate cancer. Now prostate cancer can be treated with immediate inhibition of the GnRH receptors, inducing rapid reduction of testosterone to castrate levels, and sustaining those levels over time, which are the goals of systemic therapy. When a patient has disease recurrence, it is always encouraging to clinicians and patients to see PSA levels fall so rapidly.
Wayne Anderson, President and CEO Ferring Pharmaceuticals, USA added, We are enthusiastically preparing to enter this therapeutic area of urology. We respect the challenges physicians and patients face in their fight against prostate cancer and hope that we can help them with this new treatment option. This is a big milestone for the U.S. operating unit, and we have been carefully preparing for over two years for this launch.
Phase III Study Results
The 12-month, randomized, open-label, parallel-group Phase III study evaluated the efficacy and safety of degarelix compared with leuprolide administered monthly over one year of prostate cancer treatment. Patients with histologically confirmed prostate cancer were randomized to either degarelix or leuprolide: a degarelix subcutaneous (under the skin) injection of 240 mg for one month with monthly maintenance doses of 80 mg (n=207) or monthly intermuscular (into the muscle) injections of leuprolide depot 7.5 mg (n=201).
The primary endpoint was testosterone suppression to less than or equal to 50 ng/dL during monthly measurements from Day 28 to Day 364. Degarelix was at least as effective as leuprolide in achieving and maintaining castrate levels of testosterone.
N Patients with % (95% CI) treatment response Degarelix 207 202 97.2 240/80 mg Leuprolide 7.5 mg 201 194 96.4
Suppression of testosterone levels to less than or equal to 50 ng/dL occurred significantly faster in patients receiving degarelix than in those receiving leuprolide. At Day 3, 96% of patients demonstrated treatment response. In that same time period, none of the patients who received leuprolide demonstrated treatment response. Conversely, testosterone levels had increased by a median of 65% in 80% of those receiving leuprolide at Day 3.
Overall, the most commonly observed adverse reactions during degarelix therapy included injection site reactions (e.g. pain, erythema, swelling or induration), hot flushes, increased weight, fatigue, and increases in serum levels of transaminases and gamma-glutamyltransferase (GGT). 99% of these observed adverse reactions were Grade 1 or 2 (mild to moderate). Specifically relating to the injection site adverse reactions, most were transient, of mild to moderate intensity, occurred primarily with the starting dose and led to few discontinuations (1%). Grade 3 (severe) injection site reactions occurred in 2% or less of patients receiving degarelix. Degarelix is contraindicated in patients with known hypersensitivity to degarelix or to any of the product components. Degarelix is not indicated in women or pediatric patients. Long-term androgen deprivation therapy prolongs the QT interval. Physicians should consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients with congenital long QT syndrome, electrolyte abnormalities, or congestive heart failure and in patients taking Class IA (e.g. quinidine, procainamide) or Class III (e.g. amiodarone, sotalol) antiarrhythmic medications.
About Prostate CancerProstate cancer is the most common cancer, excluding skin cancers, and the second leading cause of cancer death in American men. About one man in six will be diagnosed with prostate cancer during his lifetime, and one in 35 will die of this disease.(1) Prostate cancer develops from cells in the prostate gland that begin to grow out of control. In most cases, prostate cancer grows slowly and can remain undetected throughout a man's life, although it can grow and spread quickly.(2) The four types of standard treatment are: watchful waiting, surgery, radiation therapy, and hormone therapy, also called androgen deprivation therapy (ADT). Degarelix is a new form of hormone therapy that reversibly binds to the GnRH receptors, inhibiting the production of testosterone. By suppressing the production of testosterone, tumor growth is inhibited.(3)

规格:
Degarelix80MG VIAL
DEGARELIX INJ 240MG 2X120MG 120MG VIAL
Degarelix

Degarelix（注射剂），开发商Ferring；用于治疗前列腺癌；于2008年12月被美国FDA批准用于晚期前列腺癌的治疗。

Degarelix是一种促性腺激素释放激素（GnRH）受体拮抗剂，可与垂体的GnRH受体可逆性结合，减少促性腺激素的释放，从而减少睾酮的形成。该药为粉剂，用注射用水稀释后在腹部进行皮下注射。推荐初始剂量为240 mg，分两次皮下注射，每次120 mg，稀释浓度为40 mg/ mL。推荐维持剂量为80 mg，以20 mg/mL的浓度一次性皮下注射，每28天注射一次。

FDA批准Degarelix上市是基于一项开放标签的多中心随机平行队列研究的结果，共入组620例前列腺癌患者。分为3个治疗组，分别治疗1年：A组，Degarelix起始剂量240 mg（40 mg/mL），维持剂量每个月160 mg（40 mg/mL）皮下注射；B组，Degarelix起始剂量240 mg（40 mg/mL），维持剂量每个月80 mg（20 mg/mL）皮下注射；C组，亮丙瑞林（leuprolide）7.5 mg每个月，肌肉注射。主要观察结局是证明Degarelix治疗12个月能够将睾酮水平控制并维持到去势水平（T < 50 ng/dL）。A组（240/160 mg）有199例患者有治疗反应，98.3%达到去势水平；B组（240/80 mg）有202患者对治疗有反应，97.2%达到去势水平；C组（leuprolide 7.5 mg）有194例有治疗反应，96.4%达到去势水平。

Ferring公司正在进行关于Degarelix的扩展研究，以评价Degarelix 1个月的治疗剂量对需要接受药物去势治疗的前列腺患者的长期安全性和毒性。

该药的主要不良反应包括：潮热、注射部位反应、体重增加、肝酶水平升高、疲倦、高血压、后背及关节疼痛、寒战、尿道感染、性欲降低以及勃起功能障碍等。

药物去势是晚期前列腺癌的首选治疗方法之一。

在Degarelix未问世前，临床上最常应用的去势药物是促性腺激素释放激素类似物（Gonadotrophin Releasing Hormone agonists，GnRH-a），GnRH-a是促性腺激素释放激素（GnRH）受体的激动剂，该类药物首次应用时会引起一过性的血清睾酮升高，从而可导致患者疼痛、排尿困难和脊髓压迫等症状加重，因此临床上常在首次应用GnRH-a前先用抗雄激素药物治疗以避免该副作用发生。

Ferring公司开发的Degarelix是一种GnRH受体的拮抗剂，首次注射后不会引起血清睾酮升高，Ⅲ临床研究结果显示该药物在维持睾酮至去势水平方面可以获得与GnRH-a治疗相同的效果，在降低PSA水平及其对缓解晚期前列腺癌的临床症状方面也与GnRH-a疗效相同。因此该药的问世给晚期前列腺癌患者带来了新的福音，临床应用更为方便。但该药上市时间短，有待于大规模临床研究结果的公布，以进一步确认其疗效及其安全性。