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Degarelix

Alias: Degarelix Free Base; HSDB 7817; HSDB7817; HSDB-7817
Cat No.:V4133 Purity: ≥98%
Degarelix is a competitive, reversible gonadotropin-releasing hormone receptor (GnRHR/LHRHR) antagonist.
Degarelix
Degarelix Chemical Structure CAS No.: 214766-78-6
Product category: GnRH Receptor
This product is for research use only, not for human use. We do not sell to patients.
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10mg
25mg
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Other Forms of Degarelix:

  • Degarelix-d7
  • Degarelix acetate hydrate
  • Degarelix acetate
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
Degarelix is a competitive, reversible gonadotropin-releasing hormone receptor (GnRHR/LHRHR) antagonist. Degarelix may be used in prostate cancer research.
Biological Activity I Assay Protocols (From Reference)
Targets
GnRHR
ln Vitro
Degarelix, among the LHRH antagonists Cetrorelix (HY-P0009), Abarelix (HY-13534), and Ganirelix (HY-P1628), exhibits the least amount of histamine release and the weakest histamine-releasing properties[1]. Except for PC-3 cells, degarelix (1 nM-10 μM, 0-72 h) decreases cell viability in all prostate cell lines (WPE1-NA22, WPMY-1, BPH-1, and VCaP cells)[2].
Degarelix (10 μM, 0-72 h) uses apoptosis to directly affect the growth of prostate cells[2].
ln Vivo
Degarelix (0-10 μg/kg; s.c.; once) reduces plasma levels of testosterone and LH in castrated rats in a dose-dependent manner[3].
Degarelix is stable when incubated in microsomes and cryopreserved hepatocytes from animal liver tissue. In rats and dogs, the majority of the degarelix dosage is excreted in the urine and feces in equal proportions (40–50% in each matrix) within 48 hours, while in monkeys, the main excretion routes are the feces (50%) and the kidneys (22%)[4].
Animal Protocol
Male Sprague-Dawley rats, castrated
0.3, 1, 3 and 10 μg/kg or 12.5, 50, and 200 μg/kg
Subcutaneous injection, once
ADME/Pharmacokinetics
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.
Toxicity/Toxicokinetics
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.
References

[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.

Additional Infomation
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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C₈₂H₁₀₃CLN₁₈O₁₆
Molecular Weight
1632.26
Exact Mass
1630.748
Elemental Analysis
C, 60.34; H, 6.36; Cl, 2.17; N, 15.45; O, 15.68
CAS #
214766-78-6
Related CAS #
Degarelix-d7; Degarelix acetate hydrate; 934246-14-7;214766-78-6;Degarelix-d7;934016-19-0
PubChem CID
16136245
Appearance
White to off-white solid powder
Density
1.3±0.1 g/cm3
Index of Refraction
1.620
LogP
4.45
Hydrogen Bond Donor Count
17
Hydrogen Bond Acceptor Count
18
Rotatable Bond Count
41
Heavy Atom Count
117
Complexity
3390
Defined Atom Stereocenter Count
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
Chemical Name
(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
Synonyms
Degarelix Free Base; HSDB 7817; HSDB7817; HSDB-7817
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~10 mg/mL (~6.1 mM)
H2O: ~5 mg/mL (~3.1 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 1 mg/mL (0.61 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 1 mg/mL (0.61 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 1 mg/mL (0.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Clinical Trial Information
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
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Neoadjuvant Degarelix With or Without Apalutamide (ARN-509) Followed by Radical Prostatectomy
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Phase: Phase 2    Status: Active, not recruiting
Date: 2024-07-03
Cardiometabolic Consequences of the Loss of Ovarian Function
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Phase: Phase 4    Status: Recruiting
Date: 2024-06-20
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CTID: NCT02478775
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Phase: Phase 2    Status: Active, not recruiting
Date: 2024-05-06
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CTID: NCT03358563
PhaseEarly Phase 1    Status: Completed
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Real World Evidence Study on Metastatic Prostate Cancer in the Pirkanmaa Hospital District in Finland
CTID: NCT05701007
Phase:    Status: Completed
Date: 2024-04-24
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Phase: Phase 3    Status: Completed
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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

Biological Data
  • 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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