美国FDA批准Ferring Pharmaceuticals公司degarelix粉针剂（Tradename/Firmagon）上市，用于治疗晚期前列腺癌。本品剂量规格：degarelix 80 mg、120 mg/瓶。80 mg瓶含甘露醇 200 mg，120 mg瓶含甘露醇 150 mg。

本品系一促性腺激素释放激素（GnRH）受体抑制剂类药物，可逆性抑制垂体GnRH受体来减少促性腺激素释放继而抑制睾酮的释放。本品通过抑制对前列腺癌持续生长至关重要的睾酮来延缓前列腺癌的生长和恶化。以激素治疗前列腺癌来降低睾酮浓度的初期却造成睾酮浓度激增，此初始刺激该激素受体可暂时性促进肿瘤生长而不是抑制它。而地degarelix则不会。

Ⅲ期临床研究显示，本品降低睾酮浓度的效果至少可与亮丙瑞林储库型控释注射剂（Lupron Depot）相媲美，而且降低睾酮浓度在统计学上显著快。在治疗的第3日，本品组96％达到去生殖腺的睾酮浓度，亮丙瑞林组效果为0％。第14日，本品组99％达到去生殖腺的睾酮浓度，亮丙瑞林组为18％。

在临床研究中，前列腺特异抗原（PSA）浓度可作为监测的第2个疗效判断终点。使用degarelix2周后降低PSA 64％，1月后85％，3月后95％，在治疗的整个1年中始终抑制PSA。

本品在临床研究中报道的最常见的不良反应是注射部位反应（疼痛，红肿和肿胀），热潮红，体重增加，乏力和某些肝酶浓度升高。

FIRMAGON（degarelix注射）皮下注射 醋酸粉。

最初美国批准：2008

辉凌制药公司

适应症
FIRMAGON是GnRH受体拮抗剂，用于治疗晚期前列腺癌患者表示。
 
剂量和用法

FIRMAGON皮下注射，是不是可以静脉给药。

治疗开始剂量注射，每次120毫克240毫克。

其次是维护管理作为一个单一的注射，每28天80毫克剂量的起始剂量。
 
剂型和优势

FIRMAGON（degarelix注射）每瓶120毫克

FIRMAGON（degarelix注射）80毫克每瓶
 
禁忌
degarelix禁忌：

患者以前过敏反应到FIRMAGON。

对孕妇妊娠分类X的胎儿造成伤害，可能会出现。
 
注意事项：
长期雄激素剥夺治疗，延长QT间隔。考虑风险和利益。
 
不良反应
FIRMAGON治疗过程中最常见的不良反应（> 10％）包括注射部位反应（如疼痛，红斑，肿胀，或硬结），潮热，体重增加，增加血清转氨酶和γ-谷氨酶（GGT ）。
 
药物相互作用
临床意义CYP450的药代动力学药物相互作用是不可能的。
 
在特殊人群中使用
有老人或轻度或中度肝或肾功能损害的患者无需调整剂量。严重肝或肾功能不全患者进行了研究和谨慎，因此保证。

更新日期：09/2010

Ferring Pharmaceuticals Announces Availability of FIRMAGON® (degarelix for injection) for the Treatment of Advanced Prostate Cancer
Prostate cancer strikes one in every six men in this country, and is the second leading cause of cancer death among men in the U.S. This year alone, it will claim more than 28,000 lives, but a new treatment offers hope for those with advanced prostate cancer.

FIRMAGON® (degarelix for injection), a new injectable prostate cancer medication for the treatment of advanced prostate cancer, is now available in the U.S. The treatment rapidly inhibits the production of testosterone, a hormone that stimulates cancer growth.  FIRMAGON® was approved by the U.S. Food and Drug Administration (FDA) on December 24, 2008 and was granted marketing authorization by the European Commission on February 19, 2009.  It was launched in the U.S. in March 2009 under the generic name, degarelix. 

FIRMAGON® offers men like Mike D’Ambrosio with advanced prostate cancer a unique therapy that is fast and effective in reducing testosterone and PSA.  If you have advanced prostate cancer, ask your doctor about FIRMAGON®.

In a recent study, after just three days of treatment, participants in the FIRMAGON® group achieved a 90% decrease in median testosterone levels, whereas patients who were treated with 7.5 mg of Lupron Depot®, or leuprolide, a drug commonly used to treat advanced prostate cancer, saw a 65% increase in median testosterone levels. FIRMAGON® was as effective as leuprolide in suppressing testosterone levels from Day 28 to the end of the study (Day 364) with 97.2% of the FIRMAGON® patients maintaining medical castrate levels compared with 96.4% for leuprolide.

FIRMAGON® reduces the production of testosterone by binding immediately and reversibly to the cells in the pituitary gland, quickly reducing the release of a hormone that causes testosterone production. FIRMAGON® also significantly lowered levels of prostate specific antigen or PSA – a marker for prostate cancer. The clinical benefit is not yet known on the value of fast PSA reduction.
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Medication name
Generic name: Degarelix - Injection
Pronunciation: (DEG-a-REL-ix)
Uses
Degarelix is used to treat advanced prostate cancer in men. It is not a cure. Most types of prostate cancer need the male hormone testosterone to grow and spread. Degarelix works by reducing the amount of testosterone that the body makes. This helps slow or stop the growth of cancer cells.
How to use
Read the Patient Information Leaflet provided by your pharmacist before you start using degarelix and each time you get a refill. If you have any questions, consult your doctor or pharmacist.This medication is given as an injection under the skin (subcutaneously) in the abdominal area by a health care professional. It is usually given once a month or as directed by your doctor.The first dose is given as two injections. The following monthly doses are given as one injection. Make sure your injection site is free of any pressure from belts, waistbands, or other types of clothing.Use this medication regularly to get the most benefit from it. To help you remember, mark your calendar to keep track of when to schedule the next dose.
Precautions
Before using degarelix, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: kidney problems, liver problems.This drug may make you dizzy. Do not drive, use machinery, or do any activity that requires alertness until you are sure you can perform such activities safely. Limit alcoholic beverages.Long term use of degarelix may cause a condition that affects the heart rhythm (QT prolongation). QT prolongation can infrequently result in serious (rarely fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that require immediate medical attention. The risk of QT prolongation may be increased if you have certain medical conditions or are taking other drugs that may affect the heart rhythm (see also Drug Interactions section). Before using degarelix, tell your doctor or pharmacist if you have any of the following conditions: certain heart problems (heart failure, slow heartbeat, QT prolongation in the EKG), family history of certain heart problems (QT prolongation in the EKG, sudden cardiac death).Low levels of potassium or magnesium in the blood may also increase your risk of QT prolongation. This risk may increase if you use certain drugs (such as diuretics/"water pills") or if you have conditions such as severe sweating, diarrhea, or vomiting. Talk to your doctor about using degarelix safely.Degarelix may weaken your bones and increase your risk for bone loss (osteoporosis) if used for a long time. Consult your doctor or pharmacist for details.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).This medication is not usually used in women and must not be used during pregnancy. It may harm an unborn baby. If you become pregnant or think you may be pregnant, tell your doctor immediately.It is unknown if degarelix passes into breast milk. Consult your doctor before breast-feeding.
Drug interactions
Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Many drugs besides degarelix may affect the heart rhythm (QT prolongation), including amiodarone, dofetilide, pimozide, procainamide, quinidine, sotalol, macrolide antibiotics (such as erythromycin), among others.This medication may interfere with certain laboratory tests (including pituitary gonadal function), possibly causing false test results. Make sure laboratory personnel and all your doctors know you use this drug.
Side effects
Pain/redness/swelling at the injection site, hot flashes (flushing), increased sweating, night sweats, back/joint pain, chills, increased weight, tiredness, or dizziness may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.Infrequently, shrinking of the testicles, breast tenderness/swelling, and reduced sexual interest/ability may also occur as a result of lowered testosterone levels. Talk to your doctor if these effects occur.Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Get medical help right away if any of these rare but serious side effects occur: fast/irregular heartbeat, severe dizziness, fainting.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
Missed dose
For the best possible benefit, it is important to receive each scheduled dose of this medication as directed. If you miss a dose, contact your doctor immediately to establish a new dosing schedule.
Overdose
If overdose is suspected, contact your local poison control center or emergency room immediately. US residents can call the US National Poison Hotline at 1-800-222-1222. Canada residents can call a provincial poison control center.
Notes
Laboratory and/or medical tests (such as blood testosterone level, PSA blood test) should be performed periodically to monitor your progress. Consult your doctor for more details.
Storage
Not applicable. This medication is given in a clinic and will not be stored at home.
Photos by medication strength
Click the "Photos" link to see sample photographs for a specific medication strength.