1. GPCR/G Protein
  2. GNRH Receptor

Degarelix 

Cat. No.: HY-16168A Purity: >98.0%
Data Sheet SDS Handling Instructions

Degarelix is a competitive gonadotropin-releasing hormone receptor (GnRHR) antagonist for the treatment of androgen-dependent advanced prostate cancer.

For research use only. We do not sell to patients.
Degarelix Chemical Structure

Degarelix Chemical Structure

CAS No. : 214766-78-6

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Degarelix is a competitive gonadotropin-releasing hormone receptor (GnRHR) antagonist for the treatment of androgen-dependent advanced prostate cancer.

In Vitro

Degarelix acts directly on the pituitary receptors for luteinizing hormone-releasing hormone (LHRH), blocking the action of endogenous LHRH. The use of degarelix eliminates the initial undesirable surge in gonadotropin and testosterone levels, which is produced by agonists of LHRH[1]. Degarelix treatment reduces cell viability in all prostate cell lines (WPE1-NA22, WPMY-1, BPH-1 cells, VCaP cells), with the exception of the PC-3 cells. The GnRH antagonist degarelix exerts a direct effect on prostate cell growth through apoptosis[2].

In Vivo

At single subcutaneous injections of 0.3 to 10 μg/kg in rats, degarelix produces a dose-dependent suppression of the pituitary-gonadal axis as revealed by the decrease in plasma luteinizing hormone (LH) and testosterone levels. Duration of LH suppression increases with the dose: in the rat, significant suppression of LH lasted 1, 2, and 7 days after a single subcutaneous injection of degarelix at 12.5, 50, or 200 μg/kg, respectively[3]. Degarelix is stable when incubated in microsomes and cryopreserved hepatocytes from animal liver tissue. In rat and dog, most of the degarelix dose is eliminated within 48 h via urine and feces in equal amounts (40–50% in each matrix), whereas in monkey the major route of excretion is fecal (50%) and renal (22%)[4].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01344564 Urology of Virginia|Ferring Pharmaceuticals Prostate Cancer April 2011
NCT01696877 Sidney Kimmel Comprehensive Cancer Center Prostate Cancer Adenocarcinoma in Situ September 2012 Phase 1|Phase 2
NCT00801242 Ferring Pharmaceuticals Prostate Cancer December 2008 Phase 3
NCT00117286 Ferring Pharmaceuticals Prostate Cancer March 2005 Phase 2|Phase 3
NCT01071915 Ferring Pharmaceuticals|Ferring Pharmaceuticals Korea, Ltd. Prostate Cancer March 2010 Phase 3
NCT00215683 Ferring Pharmaceuticals Prostate Cancer February 2005 Phase 2|Phase 3
NCT01545882 Ottawa Hospital Research Institute Prostatic Neoplasms May 2011 Phase 2
NCT01242748 Ferring Pharmaceuticals Prostate Cancer October 2010 Phase 3
NCT01220869 Ferring Pharmaceuticals Prostate Cancer December 2010 Phase 3
NCT00116779 Ferring Pharmaceuticals Prostate Cancer February 2004 Phase 2
NCT00946920 Ferring Pharmaceuticals Prostate Cancer June 2009 Phase 3
NCT00738673 Ferring Pharmaceuticals Prostate Cancer July 2008 Phase 2
NCT00819156 Ferring Pharmaceuticals Prostate Cancer February 2004 Phase 2
NCT01852864 University of Cambridge Prostate Cancer July 2011 Early Phase 1
NCT03069937 Medical University of South Carolina|Ferring Pharmaceuticals Metastatic Prostatic Adenocarcinoma March 1, 2017 Phase 2
NCT02526784 Ferring Pharmaceuticals Prostate Cancer December 2015 Phase 3
NCT01512472 Canadian Urology Research Consortium|Ferring Pharmaceuticals Prostate Cancer Recurrent January 2012 Phase 4
NCT00967018 Ferring Pharmaceuticals Prostate Cancer August 2009 Phase 3
NCT00245466 Ferring Pharmaceuticals Prostate Cancer October 2001 Phase 2
NCT01712763 Centre for Endocrinology and Reproductive Medicine, Italy Endometriosis November 2012 Phase 3
NCT00116753 Ferring Pharmaceuticals Prostate Cancer January 2005 Phase 2
NCT00268892 Ferring Pharmaceuticals Prostate Cancer January 2006 Phase 2|Phase 3
NCT02468284 Ferring Pharmaceuticals Prostate Cancer July 2015 Phase 1
NCT00451958 Ferring Pharmaceuticals Prostate Cancer March 2007 Phase 3
NCT00884273 Ferring Pharmaceuticals Prostate Cancer August 2009 Phase 3
NCT00833248 Ferring Pharmaceuticals Prostate Cancer April 2009 Phase 3
NCT00831233 Ferring Pharmaceuticals Prostate Cancer April 2009 Phase 3
NCT02886598 Ferring Pharmaceuticals Prostate Cancer September 2016
NCT02475057 Rabin Medical Center|Ferring Pharmaceuticals Prostatic Neoplasms|Cardiovascular Diseases August 2015 Phase 4
NCT01731912 University of Washington|National Cancer Institute (NCI) Prostate Adenocarcinoma|Stage IIA Prostate Cancer|Stage IIB Prostate Cancer|Stage III Prostate Cancer|Stage IV Prostate Cancer May 2013
NCT00819247 Ferring Pharmaceuticals Prostate Cancer March 2001 Phase 2
NCT00434122 Ferring Pharmaceuticals Infertility, Female March 2007 Phase 2
NCT02229253 Ferring Pharmaceuticals Advanced Hormone Sensitive Prostate Cancer September 2014
NCT03202381 Azienda Ospedaliera Spedali Civili di Brescia|Ferring Pharmaceuticals Prostate Cancer June 26, 2017 Phase 4
NCT00928434 Ferring Pharmaceuticals Prostate Cancer May 2009 Phase 3
NCT01215513 Ferring Pharmaceuticals|Ferring Pharmaceuticals Korea, Ltd. Prostate Cancer September 2010 Phase 3
NCT01446991 British Columbia Cancer Agency Prostate Cancer April 2012 Phase 2
NCT01491971 Ferring Pharmaceuticals Prostate Cancer January 2012 Phase 2
NCT01710098 United Clinic Management GmbH Prostate Cancer June 2012
NCT00947882 Ferring Pharmaceuticals Lower Urinary Tract Symptoms (LUTS) August 2009 Phase 2
NCT02726009 Ferring Pharmaceuticals Prostate Cancer May 2016 Phase 4
NCT02005887 International Breast Cancer Study Group Breast Cancer Invasive Nos February 2014 Phase 2
NCT01751451 Memorial Sloan Kettering Cancer Center|Janssen Scientific Affairs, LLC|OHSU Knight Cancer Institute|Rutgers Cancer Institute of New Jersey|NorthShore University HealthSystem|Duke University|Feinberg School of Medicine, Northwestern University|Sidney Kimmel Comprehensive Cancer Center|University of North Carolina|Wayne State University|Perlmutter New York University Cancer Center|Weill Medical College of Cornell University|Ferring Pharmaceuticals|GU Research Network, LLC|University of California, Los Angeles Prostate Cancer December 2012 Phase 2
NCT01674270 University Health Network, Toronto Prostate Cancer August 2012 Phase 2
NCT01744366 Ferring Pharmaceuticals Prostate Cancer January 2013 Phase 3
NCT02015871 Ferring Pharmaceuticals Prostate Cancer January 2014 Phase 3
NCT02020070 Memorial Sloan Kettering Cancer Center|Ferring Pharmaceuticals Metastatic Castration Sensitive Prostate Cancer December 2013 Phase 2
NCT01630967 British Columbia Cancer Agency|Ferring Pharmaceuticals Prostate Neoplasm August 2012 Phase 2
NCT00527488 Ferring Pharmaceuticals BPH October 2007 Phase 2
NCT00117312 Ferring Pharmaceuticals Prostate Cancer October 2002 Phase 2
NCT00728533 Ferring Pharmaceuticals Prostate Cancer Phase 3
NCT02663908 Ferring Pharmaceuticals|Memorial Sloan Kettering Cancer Center|Duke Clinical Research Institute Prostate Cancer April 2016 Phase 3
NCT00117949 Ferring Pharmaceuticals Prostate Cancer April 2002 Phase 2
NCT00295750 Ferring Pharmaceuticals Prostate Cancer February 2006 Phase 3
NCT00468286 Ferring Pharmaceuticals Prostate Cancer May 2007 Phase 2
NCT02324998 Cambridge University Hospitals NHS Foundation Trust|AstraZeneca Prostate Cancer December 2016 Phase 1
NCT02084940 Bioroma Polycystic Ovarian Syndrome|Ovarian Hyperstimulation Syndrome|Invitro Fertilization March 2014
NCT01709942 Centre for Endocrinology and Reproductive Medicine, Italy PCOS|OHSS|INFERTILITY November 2012 Phase 3
NCT02234089 Ferring Pharmaceuticals Advanced Prostate Cancer September 2014
NCT02849990 University of Washington|Janssen Scientific Affairs, LLC|National Cancer Institute (NCI) Stage III Prostate Adenocarcinoma|Stage III Prostate Cancer|Stage IV Prostate Adenocarcinoma|Stage IV Prostate Cancer March 9, 2017 Phase 2
NCT00818623 Ferring Pharmaceuticals Prostate Cancer November 2002 Phase 2
NCT03080116 Universitaire Ziekenhuizen Leuven Prostate Cancer|Neoadjuvant Therapy|Androgen Antagonists|Prostatectomy April 30, 2017 Phase 2
NCT01861236 Ferring Pharmaceuticals Advanced Hormone Dependent Prostate Cancer March 2013
NCT02159690 Kenneth Pienta, MD|Prostate Cancer Foundation Norway|Johns Hopkins University Prostate Cancer|Localized Prostate Cancer September 2014 Phase 2
NCT00215657 Ferring Pharmaceuticals Prostate Cancer March 2003 Phase 2
NCT01994239 UNICANCER|Ferring Pharmaceuticals Adenocarcinoma of Prostate December 2012 Phase 2
NCT02135445 Millennium Pharmaceuticals, Inc.|Takeda Prostate Cancer June 2014 Phase 2
NCT01542021 Memorial Sloan Kettering Cancer Center|Ferring Pharmaceuticals Prostate Cancer|Prostatic Adenocarcinoma February 2012
NCT03056638 Memorial Sloan Kettering Cancer Center|Ferring Pharmaceuticals|University of Texas Southwestern Medical Center|University of Michigan Prostate Cancer March 28, 2017 Phase 3
NCT03009981 Alliance Foundation Trials, LLC.|Janssen Research & Development, LLC Prostate Cancer March 6, 2017 Phase 3
NCT02478775 University of Colorado, Denver Obesity|Fertility July 2015
NCT01729676 Ferring Pharmaceuticals Prostate Cancer May 2013
NCT01377389 M.D. Anderson Cancer Center|Bristol-Myers Squibb Prostate Cancer June 17, 2011 Phase 2
NCT02560051 The University of Texas Health Science Center, Houston Prostatic Neoplasms November 2015 Phase 2
NCT02489357 Sidney Kimmel Comprehensive Cancer Center|National Cancer Institute (NCI) Stage IV Prostate Cancer November 2015
NCT01990196 Jonsson Comprehensive Cancer Center Prostate Cancer September 23, 2014 Phase 2
NCT01862835 Mayo Clinic Normal Healthy Volunteers May 2013 Phase 1
NCT02494713 The University of Texas Health Science Center, Houston Prostate Cancer October 2015 Phase 2
NCT02799706 European Organisation for Research and Treatment of Cancer - EORTC Prostate Cancer April 2017 Phase 3
NCT02346253 Stanford University|National Cancer Institute (NCI) Prostate Adenocarcinoma|Stage I Prostate Cancer|Stage IIA Prostate Cancer|Stage IIB Prostate Cancer|Stage III Prostate Cancer January 2015 Phase 1|Phase 2
NCT02278185 University of Colorado, Denver Adenocarcinoma of the Prostate|Recurrent Prostate Cancer|Stage III Prostate Cancer|Stage IV Prostate Cancer November 11, 2015 Phase 2
NCT01786265 M.D. Anderson Cancer Center|Janssen Services, LLC Prostate Cancer February 2013 Phase 2
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References
Cell Assay
[2]

Cells are allowed to attach for 24–48 hours (h). After that, they are treated with different concentrations of degarelix, a GnRH antagonist (0.1 to 10 μM). 10 μL of MTT labeling reagent is added to each well and the plates are incubated at 37°C for 4h. Then, 100 μL of solubilization solution is added, and the plates are incubated at 37°C, overnight, in a humidified atmosphere. The final reaction is measured at 550–600 nm. The obtained absorbance directly correlates to the number of live and metabolically active cells, providing an indication of cell viability[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[4]

Rat: To study the absorption, distribution, metabolism, and excretion, male and female rats are dosed with 30 μg [3H]degarelix free base peptide/kg (∼300 μCi/kg). Feces, heparin plasma, and urine samples from groups A and B are collected up to 240 h after dosing. Bile sampling from cannulated rats (group C) as well as urine and feces are collected for up to 48 h. All samples in this study are analyzed by LC-RAD at the contract research[4].

Monkey: Four male cynomolgus monkeys (4.2–7.5 kg) are dosed for a disposition of radioactivity study. The animals are administered a single subcutaneous dose of 8.2 μg/kg (200 μCi/kg) [3H]degarelix. Urine and feces samples are collected quantitatively from each animal after dosing until the time of sacrifice. Blood samples are collected at the time of the sacrifice of the individual animal (6, 24, 48, and 240 h) into tubes containing EDTA as an anticoagulant[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

1632.26

Formula

C₈₂H₁₀₃ClN₁₈O₁₆

CAS No.

214766-78-6

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

H2O: ≥ 500 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Degarelix
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