Degarelix

别名: Degarelix Free Base; HSDB 7817; HSDB7817; HSDB-7817 醋酸地加瑞克;地加瑞克;加瑞克标准品
目录号: V4133 纯度: ≥98%
地加瑞克是一种竞争性、可逆性促性腺激素释放激素受体 (GnRHR/LHRHR) 拮抗剂。
Degarelix CAS号: 214766-78-6
产品类别: GnRH Receptor
产品仅用于科学研究,不针对患者销售
规格 价格 库存 数量
5mg
10mg
25mg
50mg
100mg
Other Sizes

Other Forms of Degarelix:

  • Degarelix-d7
  • Degarelix acetate hydrate
  • 醋酸地加瑞克
点击了解更多
InvivoChem产品被CNS等顶刊论文引用
产品描述
地加瑞克是一种竞争性、可逆性促性腺激素释放激素受体 (GnRHR/LHRHR) 拮抗剂。地加瑞克可用于前列腺癌研究。
生物活性&实验参考方法
靶点
GnRHR
体外研究 (In Vitro)
地加瑞克仅表现出非常弱的组胺释放特性,并且在 LHRH 拮抗剂(包括 Cetrorelix 、 Abarelix 和 Ganirelix )中组胺释放能力最低 [1]。 Degarelix(1 nM-10 μM,0-72 小时)可降低所有前列腺细胞系(WPE1-NA22、WPMY-1、BPH-1、VCaP 细胞)的细胞活力,PC-3 细胞除外[2] 。 Degarelix(10 μM,0-72 小时)通过细胞凋亡对前列腺细胞生长产生直接影响[2]。细胞活力测定[2] 细胞系:WPMY-1、WPE1-NA22、BPH-1、LNCaP 和 VCaP 浓度:1 nM-10 μM 孵育时间:WPMY-1 细胞 48 小时和 72 小时,WPE1-NA22 细胞 72 小时、BPH-1 细胞(48 小时和 72 小时)、LNCaP 细胞(48 小时和 72 小时) 结果:除 PC-3 细胞外,所有前列腺细胞系的细胞活力均降低。细胞凋亡分析[2] 细胞系:WPE1-NA22、BPH-1、LNCaP 和 VCaP 浓度:10 μM 孵育时间:24、48 和 72 小时 结果:诱导 caspase 3/7 激活显着增加。
体内研究 (In Vivo)
地加瑞克(0-10 μg/kg;皮下注射;一次)以剂量依赖性方式降低去势大鼠血浆 LH 水平和血浆睾酮水平[3]。当在微粒体和来自动物肝组织的冷冻保存的肝细胞中孵育时,地加瑞克是稳定的。在大鼠和狗中,大部分地加瑞克剂量在 48 小时内通过尿液和粪便以等量(每种基质中 40-50%)消除,而在猴子中,主要排泄途径是粪便(50%)和肾脏(22 %)[4]。动物模型:雄性 Sprague-Dawley 大鼠,去势[3] 剂量:0.3、1、3 和 10 μg/kg 或 12.5、50 和 200 μg/kg 给药方法:皮下注射,一次 结果:产生剂量依赖性且可逆的最小有效剂量为 3 μg/kg 即可降低血浆 LH 水平。对于50μg/kg和200μg/kg剂量,吸收t1/2值为4分钟和30分钟,Tmax值为1小时和5小时,表观血浆消失t1/2值为12小时和67小时,分别。最小有效剂量为 1 μg/kg,血浆睾酮水平呈剂量依赖性下降。
动物实验
Male Sprague-Dawley rats, castrated
0.3, 1, 3 and 10 μg/kg or 12.5, 50, and 200 μg/kg
Subcutaneous injection, once
药代性质 (ADME/PK)
Absorption, Distribution and Excretion
Degarelix forms a depot at the site of injection after subcutaneous administration from which the drug slowly released into circulation. After a single bolus dose of 2mg/kg, peak plasma concentrations of degarelix occured within 6 hours at a concentration of 330 ng/mL. Ki = 0.082 ng/mL and 93% of receptors were fully suppressed; MRT = 4.5 days.
Fecal (70% to 80%) and renal (20%-30% of unchanged drug)
Central compartment: 8.88 - 11.4 L; Peripheral compartment: 40.9 L
Following subcutaneous administration of degarelix to prostate cancer patients the clearance is approximately 9 L/hr.
The protein binding in plasma of mouse, rat, dog, monkey, and humans was measured using the (3)H-degarelix and the ultracentrifugation technique. The plasma binding was approximately 90% in animals and humans. Distribution of radioactivity following administration of (3)H-degarelix was studied in rats, dogs and monkeys, doses were respectively 0.03 mg/kg, 0.003 mg/kg and 0.0082 mg/kg. Radioactivity of tissues was measured after sacrifice and necropsy of the animals. High concentrations were mainly seen at the s.c. injection site and in organs of excretion. Lower concentrations, but still higher than those in plasma were generally seen in some organs of the endocrine and reproductive systems most of which contain specific receptors for LHRH, and organs rich in reticuloendothelial cells during the elimination phase. There was no indication of tissue retention.
Balance of the radioactivity following SC administration of (3)H-degarelix was studied in rats, dogs and monkeys. Degarelix was mainly excreted unchanged via the urine and was subject to sequential peptidic degradation during its elimination via the hepato-biliary pathway in both animals and man.
After subcutaneous administration, degarelix forms a local depot at the injection site, leading to retarded and extended release of the active drug. The release from the depot is dependent on the concentration in the dose formulation and the dose volume. Furthermore, in repeat dose studies, increasing concentrations in the dose formulation resulted in sub-proportional increases in maximum plasma concentration (Cmax) and area under plasma concentration vs time in the dosing interval (AUC), an increase in trough plasma concentration (Ctrough), an increase in terminal half-life (t1/2), thus increasing the time to reach steady state, and a tendency of increase in time to maximum plasma concentration (Tmax).
Degarelix forms a depot at the injection site following subcutaneous administration from which the drug is very slowly released into circulation. Peak plasma concentrations of degarelix generally occur within 2 days following subcutaneous administration of a single 240 mg dose at a concentration of 40 mg/mL.. The pharmacokinetic behavior of degarelix is strongly influenced by its concentration in the injection solution. Approximately 90% of the drug is bound to plasma proteins. No quantitatively substantial metabolites have been detected in plasma following subcutaneous adminstration. Degarelix does not appear to be a substrate, inducer, or inhibitor of the cytochrome P-450 (CYP) enzyme or P-glycoprotein transport systems based on in vitro studies. Degarelix is eliminated in a biphasic manner, with a median terminal half-life of about 53 days following subcutaneous administration of a 240 mg dose at a concentration of 40 mg/mL in prostate cancer patients. Degarelix is subject to peptide hydrolysis during its passage through the hepatobiliary system and is mainly excreted as peptide fragments in feces. Approximately 20-30% of a given dose of degarelix is renally eliminated, suggesting that approximately 70-80% is excreted via the hepatobiliary system.
For more Absorption, Distribution and Excretion (Complete) data for Degarelix (6 total), please visit the HSDB record page.
Metabolism / Metabolites
70% - 80% of degarelix is subject to peptide hydrolysis during its passage through the hepatobiliary system and then fecally eliminated. No active or inactive metabolites or involvement of CYP450 isozymes.
The stability of degarelix was studied in liver microsomes from males in rat, guinea pig, rabbit, dog, monkey, and human, for up to 60 min. No degradation of degarelix was detected in liver microsomes from rabbit, dog, monkey, and human. Tendency to minor degradation of degarelix was seen in liver microsomes from guinea pig and rat. The in vitro metabolism of degarelix was further investigated in human liver microsomes for up to 60 min. The metabolism pattern of degarelix was reported to be similar in humans and animals. Degarelix was virtually no substrate for oxidative metabolism, but was degraded by peptidases with generation of various truncated peptides. Only low concentration of one metabolite was seen in human plasma, and this metabolite was also seen in rats, dogs and monkeys.
Biological Half-Life
Terminal half-life: 41.5 - 70.2 days; Absorption half-life: 32.9 hours; Half-life from injection site: 1.17 days.
Degarelix is eliminated in a biphasic manner, with a median terminal half-life of about 53 days following subcutaneous administration of a 240 mg dose at a concentration of 40 mg/mL in prostate cancer patients.
毒性/毒理 (Toxicokinetics/TK)
Hepatotoxicity
Degarelix therapy has been associated with serum enzyme elevations in up to one-third of patients. The elevations, however, are generally mild and self-limited, resolving even without dose adjustment. ALT values above 3 times the ULN occur in less than 1% of patients. Occasional patients require drug discontinuation because of serum enzyme elevations, but no instances of liver injury with jaundice or clinically apparent acute liver injury were reported in the initial clinical trials of degarelix. Since its approval and more widescale use, there have been no published reports of clinically apparent liver injury attributed to degarelix, although its general use has been limited.
Likelihood score: E (unlikely cause of clinically apparent liver injury).
Protein Binding
90% of the drug is bound to plasma proteins.
Interactions
Since androgen deprivation treatment may prolong the QTc interval, the concomitant use of degarelix with medicinal products known to prolong the QTc interval or medicinal products able to induce torsades de pointes such as class IA (e.g. quinidine, disopyramide) or class III (e.g. amiodarone, sotalol, dofetilide, ibutilide) antiarrhythmic medicinal products, methadone, cisapride, moxifloxacine, antipsychotics, etc. should be carefully evaluated.
参考文献

[1]. An update on the use of degarelix in the treatment of advanced hormone-dependent prostate cancer. Onco Targets Ther. 2013 Apr 16;6:391-402.

[2]. In search of the molecular mechanisms mediating the inhibitory effect of the GnRH antagonistdegarelix on human prostate cell growth. PLoS One. 2015 Mar 26;10(3):e0120670.

[3]. Pharmacological profile of a new, potent, and long-acting gonadotropin-releasing hormoneantagonist: degarelix. J Pharmacol Exp Ther. 2002 Apr;301(1):95-102.

[4]. Metabolite profiles of degarelix, a new gonadotropin-releasing hormone receptor antagonist, in rat, dog, and monkey. Drug Metab Dispos. 2011 Oct;39(10):1895-903.

其他信息
Therapeutic Uses
Degarelix is used for the treatment of advanced prostate cancer. /Use included in US product label/
Drug Warnings
Degarelix is contraindicated in women who are or may become pregnant. Degarelix can cause fetal harm when administered to a pregnant woman.
FDA Pregnancy Risk Category: X /CONTRAINDICATED IN PREGNANCY. Studies in animals or humans, or investigational or post-marketing reports, have demonstrated positive evidence of fetal abnormalities or risk which clearly outweights any possible benefit to the patient./
The most frequently reported adverse reactions at the injection sites were pain (28%), erythema (17%), swelling (6%), induration (4%) and nodule (3%). These adverse reactions were mostly transient, of mild to moderate intensity, occurred primarily with the starting dose and led to few discontinuations (<1%). Grade 3 injection site reactions occurred in 2% or less of patients receiving degarelix.
A total of 1325 patients with prostate cancer received Firmagon either as a monthly treatment (60-160 mg) or as a single dose (up to 320 mg). A total of 1032 patients (78%) were treated for at least 6 months and 853 patients (64%) were treated for one year or more. The most commonly observed adverse reactions during Firmagon therapy included injection site reactions (e.g. pain, erythema, swelling or induration), hot flashes, increased weight, fatigue, and increases in serum levels of transaminases and gammaglutamyltransferase (GGT). The majority of the adverse reactions were Grade 1 or 2, with Grade 3/4 adverse reaction incidences of 1% or less.
For more Drug Warnings (Complete) data for Degarelix (15 total), please visit the HSDB record page.
Pharmacodynamics
Degarelix is a synthetic derivative of GnRH decapeptide, the ligand of the GnRH receptor. Gonadotropin and androgen production result from the binding of endogenous GnRH to the GnRH receptor. Degarelix antagonizes the GnRH receptor which in turn blocks the release of LH and FSH from the pituitary. LF and FSH decreases in a concentration-dependent manner. The reduction in LH leads to a decrease in testosterone release from the testes.
*注: 文献方法仅供参考, InvivoChem并未独立验证这些方法的准确性
化学信息 & 存储运输条件
分子式
C₈₂H₁₀₃CLN₁₈O₁₆
分子量
1632.26
精确质量
1630.748
元素分析
C, 60.34; H, 6.36; Cl, 2.17; N, 15.45; O, 15.68
CAS号
214766-78-6
相关CAS号
Degarelix-d7; Degarelix acetate hydrate; 934246-14-7;214766-78-6;Degarelix-d7;934016-19-0
PubChem CID
16136245
外观&性状
White to off-white solid powder
密度
1.3±0.1 g/cm3
折射率
1.620
LogP
4.45
tPSA
512.87
氢键供体(HBD)数目
17
氢键受体(HBA)数目
18
可旋转键数目(RBC)
41
重原子数目
117
分子复杂度/Complexity
3390
定义原子立体中心数目
11
SMILES
C[C@H](C(N)=O)NC([C@H]1N(C([C@H](CCCCNC(C)C)NC([C@H](CC(C)C)NC([C@@H](CC2=CC=C(NC(N)=O)C=C2)NC([C@H](CC3=CC=C(NC([C@H](CC(N4)=O)NC4=O)=O)C=C3)NC([C@H](CO)NC([C@@H](CC5=CC=CN=C5)NC([C@@H](CC6=CC=C(Cl)C=C6)NC([C@@H](CC7=CC=C8C=CC=CC8=C7)NC(C)=O)=O)=O)=O)=O)=O)=O)=O)=O)CCC1)=O
InChi Key
MEUCPCLKGZSHTA-XYAYPHGZSA-N
InChi Code
InChI=1S/C82H103ClN18O16/c1-45(2)35-60(72(107)92-59(16-9-10-33-87-46(3)4)80(115)101-34-12-17-68(101)79(114)88-47(5)70(84)105)93-74(109)63(38-51-23-30-58(31-24-51)91-81(85)116)95-76(111)64(39-50-21-28-57(29-22-50)90-71(106)66-42-69(104)100-82(117)99-66)97-78(113)67(44-102)98-77(112)65(41-53-13-11-32-86-43-53)96-75(110)62(37-49-19-26-56(83)27-20-49)94-73(108)61(89-48(6)103)40-52-18-25-54-14-7-8-15-55(54)36-52/h7-8,11,13-15,18-32,36,43,45-47,59-68,87,102H,9-10,12,16-17,33-35,37-42,44H2,1-6H3,(H2,84,105)(H,88,114)(H,89,103)(H,90,106)(H,92,107)(H,93,109)(H,94,108)(H,95,111)(H,96,110)(H,97,113)(H,98,112)(H3,85,91,116)(H2,99,100,104,117)/t47-,59+,60+,61-,62-,63-,64+,65-,66+,67+,68+/m1/s1
化学名
(4S)-N-[4-[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-acetamido-3-naphthalen-2-ylpropanoyl]amino]-3-(4-chlorophenyl)propanoyl]amino]-3-pyridin-3-ylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-[[(2R)-1-[[(2S)-1-[[(2S)-1-[(2S)-2-[[(2R)-1-amino-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxo-6-(propan-2-ylamino)hexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-[4-(carbamoylamino)phenyl]-1-oxopropan-2-yl]amino]-3-oxopropyl]phenyl]-2,6-dioxo-1,3-diazinane-4-carboxamide
别名
Degarelix Free Base; HSDB 7817; HSDB7817; HSDB-7817
HS Tariff Code
2934.99.9001
存储方式

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意: 请将本产品存放在密封且受保护的环境中,避免吸湿/受潮。
运输条件
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
溶解度数据
溶解度 (体外实验)
DMSO: ~10 mg/mL (~6.1 mM)
H2O: ~5 mg/mL (~3.1 mM)
溶解度 (体内实验)
配方 1 中的溶解度: ≥ 1 mg/mL (0.61 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。
例如,若需制备1 mL的工作液,可将100 μL 10.0 mg/mL澄清DMSO储备液加入400 μL PEG300中,混匀;然后向上述溶液中加入50 μL Tween-80,混匀;加入450 μL生理盐水定容至1 mL。
*生理盐水的制备:将 0.9 g 氯化钠溶解在 100 mL ddH₂O中,得到澄清溶液。

配方 2 中的溶解度: ≥ 1 mg/mL (0.61 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。
例如,若需制备1 mL的工作液,可将 100 μL 10.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中,混匀。
*20% SBE-β-CD 生理盐水溶液的制备(4°C,1 周):将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中,得到澄清溶液。

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配方 3 中的溶解度: ≥ 1 mg/mL (0.61 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。
例如,若需制备1 mL的工作液,可将 100 μL 10.0 mg/mL 澄清 DMSO 储备液加入900 μL 玉米油中,混合均匀。


请根据您的实验动物和给药方式选择适当的溶解配方/方案:
1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL;

3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果,工作液请现配现用!
6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。
制备储备液 1 mg 5 mg 10 mg
1 mM 0.6126 mL 3.0632 mL 6.1265 mL
5 mM 0.1225 mL 0.6126 mL 1.2253 mL
10 mM 0.0613 mL 0.3063 mL 0.6126 mL

1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;

2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;

3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);

4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。

计算器

摩尔浓度计算器可计算特定溶液所需的质量、体积/浓度,具体如下:

  • 计算制备已知体积和浓度的溶液所需的化合物的质量
  • 计算将已知质量的化合物溶解到所需浓度所需的溶液体积
  • 计算特定体积中已知质量的化合物产生的溶液的浓度
使用摩尔浓度计算器计算摩尔浓度的示例如下所示:
假如化合物的分子量为350.26 g/mol,在5mL DMSO中制备10mM储备液所需的化合物的质量是多少?
  • 在分子量(MW)框中输入350.26
  • 在“浓度”框中输入10,然后选择正确的单位(mM)
  • 在“体积”框中输入5,然后选择正确的单位(mL)
  • 单击“计算”按钮
  • 答案17.513 mg出现在“质量”框中。以类似的方式,您可以计算体积和浓度。

稀释计算器可计算如何稀释已知浓度的储备液。例如,可以输入C1、C2和V2来计算V1,具体如下:

制备25毫升25μM溶液需要多少体积的10 mM储备溶液?
使用方程式C1V1=C2V2,其中C1=10mM,C2=25μM,V2=25 ml,V1未知:
  • 在C1框中输入10,然后选择正确的单位(mM)
  • 在C2框中输入25,然后选择正确的单位(μM)
  • 在V2框中输入25,然后选择正确的单位(mL)
  • 单击“计算”按钮
  • 答案62.5μL(0.1 ml)出现在V1框中
g/mol

分子量计算器可计算化合物的分子量 (摩尔质量)和元素组成,具体如下:

注:化学分子式大小写敏感:C12H18N3O4  c12h18n3o4
计算化合物摩尔质量(分子量)的说明:
  • 要计算化合物的分子量 (摩尔质量),请输入化学/分子式,然后单击“计算”按钮。
分子质量、分子量、摩尔质量和摩尔量的定义:
  • 分子质量(或分子量)是一种物质的一个分子的质量,用统一的原子质量单位(u)表示。(1u等于碳-12中一个原子质量的1/12)
  • 摩尔质量(摩尔重量)是一摩尔物质的质量,以g/mol表示。
/

配液计算器可计算将特定质量的产品配成特定浓度所需的溶剂体积 (配液体积)

  • 输入试剂的质量、所需的配液浓度以及正确的单位
  • 单击“计算”按钮
  • 答案显示在体积框中
动物体内实验配方计算器(澄清溶液)
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
第二步:请输入动物体内配方组成(配方适用于不溶/难溶于水的化合物),不同的产品和批次配方组成不同,如对配方有疑问,可先联系我们提供正确的体内实验配方。此外,请注意这只是一个配方计算器,而不是特定产品的确切配方。
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+
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计算结果:

工作液浓度 mg/mL;

DMSO母液配制方法 mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。

体内配方配制方法μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。

(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
            (2) 一定要按顺序加入溶剂 (助溶剂) 。

临床试验信息
Radium Ra 223 Dichloride, Hormone Therapy and Stereotactic Body Radiation Therapy in Treating Patients With Metastatic Prostate Cancer
CTID: NCT03361735
Phase: Phase 2    Status: Active, not recruiting
Date: 2024-12-02
Finite Androgen Ablation With or Without Abiraterone Acetate and Prednisone in Treating Patients With Recurrent Prostate Cancer
CTID: NCT01786265
Phase: Phase 2    Status: Active, not recruiting
Date: 2024-11-29
Antiandrogen Therapy and Radiation Therapy With or Without Docetaxel in Treating Patients With Prostate Cancer That Has Been Removed by Surgery
CTID: NCT03070886
Phase: Phase 2/Phase 3    Status: Active, not recruiting
Date: 2024-11-29
Two Studies for Patients With High Risk Prostate Cancer Testing Less Intense Treatment for Patients With a Low Gene Risk Score and Testing a More Intense Treatment for Patients With a High Gene Risk Score, The PREDICT-RT Trial
CTID: NCT04513717
Phase: Phase 3    Status: Recruiting
Date: 2024-11-27
Two Studies for Patients With Unfavorable Intermediate Risk Prostate Cancer Testing Less Intense Treatment for Patients With a Low Gene Risk Score and Testing a More Intense Treatment for Patients With a Higher Gene Risk Score
CTID: NCT05050084
Phase: Phase 3    Status: Recruiting
Date: 2024-11-27
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Stereotactic Body Radiation Therapy Plus Androgen Receptor Pathway Inhibitor and Androgen Deprivation Therapy for Treatment of Metastatic, Recurrent Hormone-Sensitive Prostate Cancer, DIVINE Trial
CTID: NCT06378866
Phase: Phase 2    Status: Recruiting
Date: 2024-11-26


Targeting Androgen Signaling in Urothelial Cell Carcinoma - Neoadjuvant
CTID: NCT05839119
Phase: Phase 1    Status: Recruiting
Date: 2024-11-25
Treating Prostate Cancer That Has Come Back After Surgery With Apalutamide and Targeted Radiation Based on PET Imaging
CTID: NCT04423211
Phase: Phase 3    Status: Recruiting
Date: 2024-11-05
Trial Comparing Irradiation Plus Long Term Adjuvant Androgen Deprivation With GnRH Antagonist Versus GnRH Agonist Plus Flare Protection in Patients With Very High Risk Localized or Locally Advanced Prostate Cancer
CTID: NCT02799706
Phase: Phase 3    Status: Active, not recruiting
Date: 2024-11-05
Study to Find Maintenance Dose for Periodic Administration of ASP3550
CTID: NCT01261572
Phase: Phase 2    Status: Completed
Date: 2024-10-31
A Study of Copanlisib in Combination with Degarelix in People with Prostate Cancer
CTID: NCT06218667
Phase: Phase 1/Phase 2    Status: Withdrawn
Date: 2024-10-31
A Study to Compare the Effect of ASP3550 With Goserelin in Patients With Prostate Cancer
CTID: NCT01964170
Phase: Phase 3    Status: Completed
Date: 2024-10-31
Androgen Deprivation Therapy Prior to Prostatectomy for Patients with Intermediate and High Risk Prostate Cancer
CTID: NCT01542021
Phase: N/A    Status: Completed
Date: 2024-10-03
ETHAN - ET for Male BC
CTID: NCT05501704
Phase: Phase 2    Status: Recruiting
Date: 2024-10-03
Neoadjuvant Phase 2 Study Comparing the Effects of AR Inhibition With/Without SRC or MEK Inhibition in Prostate Cancer
CTID: NCT01990196
Phase: Phase 2    Status: Active, not recruiting
Date: 2024-10-01
Phase II Study of Docetaxel Before Degarelix in Patients With Newly Diagnosed Metastatic Prostate Cancer.
CTID: NCT03069937
Phase: Phase 2    Status: Active, not recruiting
Date: 2024-09-19
Androgen Deprivation, With or Without pTVG-AR, and With or Without T-Cell Checkpoint Blockade, in Patients With Newly Diagnosed, High-Risk Prostate Cancer
CTID: NCT04989946
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-08-29
Trial of ADT and SBRT Versus SBRT for Intermediate Prostate Cancer
CTID: NCT03056638
Phase: Phase 3    Status: Terminated
Date: 2024-08-28
Presurgical Phase II Study of Talazoparib in Combination With Enzalutamide in Prostate Cancer
CTID: NCT05873192
Phase: Phase 2    Status: Not yet recruiting
Date: 2024-08-27
Neo-DAB: Darolutamide and Abemaciclib in Prostate Cancer
CTID: NCT05617885
Phase: Phase 1/Phase 2    Status: Active, not recruiting
Date: 2024-08-20
Combining Ipilimumab, Degarelix, and Radical Prostatectomy in Men With Newly Diagnosed Metastatic Castration Sensitive Prostate Cancer or Ipilimumab and Degarelix in Men With Biochemically Recurrent Castration Sensitive Prostate Cancer After Radical Prostatectomy
CTID: NCT02020070
Phase: Phase 2    Status: Active, not recruiting
Date: 2024-08-16
Standard Systemic Therapy With or Without Definitive Treatment in Treating Participants With Metastatic Prostate Cancer
CTID: NCT03678025
Phase: Phase 3    Status: Recruiting
Date: 2024-08-16
Non-fucosylated Anti-CTLA-4 (BMS-986218) + Degarelix Acetate vs. Degarelix Acetate Alone in Men With High-risk Localized Prostate Cancer
CTID: NCT04301414
PhaseEarly Phase 1    Status: Active, not recruiting
Date: 2024-07-09
Neoadjuvant Degarelix With or Without Apalutamide (ARN-509) Followed by Radical Prostatectomy
CTID: NCT03080116
Phase: Phase 2    Status: Active, not recruiting
Date: 2024-07-03
Cardiometabolic Consequences of the Loss of Ovarian Function
CTID: NCT06264882
Phase: Phase 4    Status: Recruiting
Date: 2024-06-20
Dysregulation of FSH in Obesity: Functional and Statistical Analysis
CTID: NCT02478775
Phase: N/A    Status: Completed
Date: 2024-06-05
Enzalutamide Versus Standard Androgen Deprivation Therapy for the Treatment Hormone Sensitive Prostate Cancer
CTID: NCT02278185
Phase: Phase 2    Status: Active, not recruiting
Date: 2024-05-06
Pilot Trial of Chemohormonal Therapy Followed by Prostatectomy in High Risk Prostate Cancer
CTID: NCT03358563
PhaseEarly Phase 1    Status: Completed
Date: 2024-05-03
Neoadjuvant ADT With TULSA in the Treatment of Intermediate Risk Prostate Cancer
CTID: NCT05917860
Phase: Phase 1    Status: Recruiting
Date: 2024-04-25
Real World Evidence Study on Metastatic Prostate Cancer in the Pirkanmaa Hospital District in Finland
CTID: NCT05701007
Phase:    Status: Completed
Date: 2024-04-24
Degarelix in the Treatment of Endometriosis Recurrence
CTID: NCT01712763
Phase: Phase 3    Status: Completed
Date: 2024-03-06
Treatment of High-Risk Prostate Cancer Guided by Novel Diagnostic Radio- and Molecular Tracers
CTID: NCT06282588
Phase: Phase 2/Phase 3    Status: Recruiting
Date: 2024-02-28
Study of Radiation Therapy in Combination With Darolutamide + Degarelix in Intermediate Risk Prostate Cancer
CTID: NCT04176081
Phase: Phase 2    Status: Not yet recruiting
Date: 2024-01-24
Palifermin With Leuprolide Acetate for the Promotion of Immune Recovery Following Total Body Irradiation Based T-Cell Depleted Allogeneic Hematopoietic Stem Cell Transplantation
CTID: NCT01746849
Phase: Phase 2    Status: Active, not recruiting
Date: 2024-01-05
Talazoparib With Androgen Deprivation Therapy and Abiraterone for the Treatment of Castration Sensitive Prostate Cancer
CTID: NCT04734730
Phase: Phase 2    Status: Recruiting
Date: 2024-01-03
Nivolumab and BMS-986253 for Hormone-Sensitive Prostate Cancer (MAGIC-8)
CTID: NCT03689699
Phase: Phase 1/Phase 2    Status: Active, not recruiting
Date: 2023-12-22
Comparison of HT Concomitant With RT vs RT Alone in Patients With a Detectable PSA After Prostatectomy
CTID: NCT01994239
Phase: Phase 2    Status: Active, not recruiting
Date: 2023-12-08
A Clinical Study Evaluating The Benefit of Adding Rucaparib to Enzalutamide for Men With Metastatic Prostate Cancer That Has Become Resistant To Testosterone-Deprivation Therapy
CTID: NCT04455750
Phase: Phase 3    Status: Active, not recruiting
Date: 2023-12-04
Dose Finding Trial With a New Treatment (Degarelix) for Prostate Cancer
CTID: NCT00819156
Phase: Phase 2    Status: Completed
Date: 2023-11-30
Investigation of a New Trial Drug (FE200486) in Prostate Cancer Patients
CTID: NCT00818623
Phase: Phase 2    Status: Completed
Date: 2023-11-30
High-Dose Brachytherapy in Treating Patients With Prostate Cancer
CTID: NCT02346253
Phase: N/A    Status: Active, not recruiting
Date: 2023-11-22
The Efficacy and Safety of FE 200486 in Treatmen
A phase 2 Randomized Open-Label Study of Oral darolutamide (ODM-201) vs. androgen deprivation therapy (ADT) with LHRH agonists or antagonist in Men with Hormone Naive Prostate Cancer
CTID: null
Phase: Phase 2    Status: Ongoing, Trial now transitioned, Completed
Date: 2017-09-21
Neoadjuvant degarelix +/- apalutamide (ARN-509) followed by radical prostatectomy for intermediate and high-risk prostate cancer: a randomized, placebo-controlled trial.
CTID: null
Phase: Phase 2    Status: Completed
Date: 2017-08-03
A PILOT PHASE IV STUDY TO EVALUATE VARIATION IN BONE MINERAL DENSITY, LEAN AND FAT BODY MASS MEASURED BY DUAL-ENERGY X-RAY ABSORPTIOMETRY IN PATIENTS WITH PROSTATE CANCER WITHOUT BONE METASTASIS TREATED WITH DEGARELIX
CTID: null
Phase: Phase 4    Status: Completed
Date: 2017-03-29
An experimental pilot study on immune and inflammatory biomarkers in patients with advanced prostatecancer treated with degarelix vs. GnRH agonist and with cardiovascular disease
CTID: null
Phase: Phase 2    Status: Completed
Date: 2017-03-13
A Multi-Centre, Open-Label, Randomised Trial Evaluating Two Subcutaneous Injection Techniques and Intramuscular Administration of Degarelix in Patients with Prostate Cancer
CTID: null
Phase: Phase 3    Status: Completed
Date: 2015-11-19
Molecular-biological tumor profiling for drug treatment selection in patients with advanced and refractory carcinoma
CTID: null
Phase: Phase 2    Status: Completed
Date: 2015-05-04
Investigation of the efficacy of degarelix as an acute treatment for patients with pedophilic disorder to reduce the risk for sexual child molestation: a prospective, randomized, double blind, and placebo controlled study.
CTID: null
Phase: Phase 2    Status: Completed
Date: 2014-10-22
A randomized phase II trial evaluating the endocrine activity and efficacy of neoadjuvant degarelix versus triptorelin in premenopausal patients receiving letrozole for locally advanced endocrine responsive breast cancer
CTID: null
Phase: Phase 2    Status: Completed
Date: 2013-11-11
Etude de phase II randomisée multicentrique comparant l'efficacité d'une hormonothérapie courte concomitante à une radiothérapie versus une radiothérapie exclusive dans le traitement de rattrapage de patients présentant un PSA détectable après prostatectomie totale
CTID: null
Phase: Phase 2    Status: Ongoing
Date: 2012-09-11
An Open-label, Multi-Centre, Extension Trial, Evaluating the Long-Term Progression-Free Survival of Degarelix or Goserelin Three-Month Dosing Regimens in Patients with Prostate Cancer Requiring Androgen Deprivation Therapy
CTID: null
Phase: Phase 3    Status: Completed, Prematurely Ended
Date: 2010-11-11
A dose-finding, multi-centre, double-blind, randomised, parallel, placebo-controlled trial to investigate efficacy and safety of degarelix in men with lower urinary tract symptoms (LUTS) associated with benign prostatic hyperplasia (BPH)
CTID: null
Phase: Phase 2    Status: Completed
Date: 2009-10-21
An Open-Label, Multi-Centre, Randomised, Parallel-Arm One-Year Trial, Comparing the Efficacy and Safety of Degarelix Three-Month Dosing Regimen with Goserelin Acetate in Patients with Prostate Cancer Requiring Androgen Deprivation Therapy
CTID: null
Phase: Phase 3    Status: Completed
Date: 2009-07-17
Ensayo clínico fase IIIb, no aleatorizado, abierto, multicéntrico, de seguimiento de la seguridad de dosis mensuales de degarelix en pacientes con cáncer de próstata.
CTID: null
Phase: Phase 3    Status: Completed
Date: 2009-04-27
A randomised, parallel arm, open-label trial comparing degarelix with goserelin plus anti-androgen flare protection (bicalutamide), in terms of prostate size reduction in prostate cancer patients of intermediate-to-high risk, who require neoadjuvant hormone therapy prior to radiotherapy (curative intent)
CTID: null
Phase: Phase 3    Status: Completed
Date: 2009-04-15
A randomised, parallel-arm, open-label trial comparing degarelix with goserelin plus anti-androgen flare protection (bicalutamide), in terms of volume reduction of the prostate in patients with prostate cancer being candidates for medical castration
CTID: null
Phase: Phase 3    Status: Completed
Date: 2009-04-09
An Open-Label, Multi-Centre, Uncontrolled, Trial Investigating Degarelix One-Month Dosing Regimen Administered as Intermittent Androgen Deprivation (IAD) for One or More Cycles in Patients with Prostate Cancer Requiring Androgen Deprivation Therapy
CTID: null
Phase: Phase 3    Status: Completed
Date: 2008-12-22
A randomised, parallel-arm, open-label trial comparing degarelix with goserelin plus anti-androgen flare protection (bicalutamide), in terms of reduction in International Prostate Symptom Score (IPSS), in patients with lower urinary tract symptoms (LUTS) secondary to locally advanced prostate cancer
CTID: null
Phase: Phase 3    Status: Prematurely Ended, Completed
Date: 2008-11-18
A single-centre, open-label, randomised explorative pharmacokinetic/pharmacodynamic study of the gonadotropin-releasing hormone receptor antagonist degarelix (FE 200486) in patients with benign prostatic hyperplasia
CTID: null
Phase: Phase 2    Status: Completed
Date: 2008-06-30
An Open-Label, Multi-Centre, Uncontrolled, Exploratory Study, Investigating Degarelix One-Month Dosing Regimen as Second-Line Hormonal Treatment after PSA-Failure in GnRH Agonist Treated Patients with Prostate Cancer
CTID: null
Phase: Phase 2    Status: Completed
Date: 2008-06-20
An Open-Label, Multi-Centre, Randomised Parallel-Group Study, Investigating Efficacy and Safety of Different Degarelix Three-Month Dosing Regimens in Patients with Prostate Cancer Requiring Androgen Ablation Therapy
CTID: null
Phase: Phase 3    Status: Prematurely Ended, Completed
Date: 2008-01-30
An Open-Label, Multi-Centre, Randomised Parallel-Group Dose-Finding Study, Investigating Efficacy and Safety of Two Degarelix Three-Month Dosing Regimens in Patients with Prostate Cancer Requiring Androgen Ablation Therapy
CTID: null
Phase: Phase 2    Status: Completed
Date: 2007-05-14
An Open-Label, Multi-Centre, Extension Study, Evaluating the Long-Term Safety and Tolerability of Degarelix One-Month Dosing Regimen in Patients with Prostate Cancer Requiring Androgen Ablation Therapy
CTID: null
Phase: Phase 3    Status: Completed
Date: 2007-03-23
A randomised, assessor-blind, parallel groups, multi-centre, exploratory study assessing the impact of subcutaneous administration of degarelix 2.5 mg on synchronisation of follicle cohort compared to placebo and evaluating the effects of degarelix 2.5 mg started in the mid-luteal or early follicular phase on endometrial receptivity compared to a fixed gonadotrophin releasing hormone antagonist protocol in oocyte donors undergoing controlled ovarian hyperstimulation for assisted reproductive technologies
CTID: null
Phase: Phase 2    Status: Completed
Date: 2007-01-08
An Open-Label, Multi-Centre, Extension Study, evaluating the Long-Term Safety and Tolerability of Different Three-Month Degarelix Dosing Regimens, 240 mg (40 mg/mL), 240 mg (60 mg/mL), in Patients with Prostate Cancer.
CTID: null
Phase: Phase 2    Status: Completed
Date: 2006-07-17
An open-label, multi-centre, extension study evaluation the long-term safety and tolerability of Degarelix one-month depots in patients with prostate cancer
CTID: null
Phase: Phase 2    Status: Completed
Date: 2005-02-01
An Open-Label, Multi-Centre, Randomised Parallel Group Comparison of Efficacy and Safety of Degarelix Three-Month Depot in Three Different Dosing Regimens of 240 mg (40 mg/mL) and 240 mg (60 mg/mL) in Patients with Prostate Cancer Requiring Androgen Ablation Therapy
CTID: null
Phase: Phase 2, Phase 3    Status: Completed
Date: 2005-01-27
Systemic Therapy in Advancing or Metastatic Prostate Cancer: Evaluation of Drug Efficacy
CTID: null
Phase: Phase 2, Phase 3    Status: GB - no longer in EU/EEA
Date: 2004-10-04
An Open-label, Multi-Centre, Randomized, Parallel-group Study, Investigating the Efficacy and Safety of Degarelix One Month Dosing Regimens; 160 mg (40 mg/ml) and 80 mg (20mg/ml), in Comparison to LUPRON DEPOT® 7.5 mg in Patients with Prostate Cancer Requiring Androgen Ablation Therapy
CTID: null
Phase: Phase 3    Status: Completed
Date:
The evaluation of the efficacy of a switch from GnRH agonist to GnRH antagonist in prostate cancer patients who relapsed during combined androgen blockade.
CTID: UMIN000013514
PhaseNot applicable    Status: Complete: follow-up complete
Date: 2014-03-27
An analytical study of laboratory tests and clinical effectiveness for combination therapies using GnRH antagonist/antiandrogen and GnRH aonist/antiandrogen in prostate cancer patients.
CTID: UMIN000013151
Phase:    Status: Recruiting
Date: 2014-02-13
Endocrinological profiles in patients with prostate cancer treated with LHRH antagonist
CTID: UMIN000011990
Phase:    Status: Complete: follow-up complete
Date: 2013-10-08
Endocrinological profiles in patients with prostate cancer treated with LHRH antagonist
CTID: UMIN000011990
Phase:    Status: Complete: follow-up complete
Date: 2013-10-08
A randomized phase II study of degarelix combined with anti-androgen for prostate cancer
CTID: UMIN000011506
Phase:    Status: Complete: follow-up complete
Date: 2013-08-17
Deferred combined androgen blockade therapy using antiandrogen in hormone-refractory metastatic prostate cancer patients treated with Degarelix, GnRH antagonist
CTID: UMIN000011437
Phase:    Status: Recruiting
Date: 2013-08-09

生物数据图片
  • MTT assay showing the viability of prostate cell lines following treatment with the GnRH antagonist, degarelix. PLoS One . 2015 Mar 26;10(3):e0120670.
  • PLoS One . 2015 Mar 26;10(3):e0120670.
  • Gene ontology classification (based on biological processes) of degarelix-deregulated genes on BPH-1 cells. PLoS One . 2015 Mar 26;10(3):e0120670.
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