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Peptide

Degarelix (Firmagon)

Degarelix is a third-generation GnRH antagonist peptide. FDA-approved for advanced prostate cancer. Phase III trial (CS21) showed 97.2% achieved testosterone ≤0.5 ng/mL. Achieves castration in 96% of patients by day 3 (vs 0% with leuprolide). No testosterone flare or need for antiandrogen flare protection. Median PSA significantly lower at days 14 and 28 vs leuprolide (p<0.001).

Research notice. This page is for education and research. Peptides may not be FDA-approved for human use and may only be legally available for research. Talk to a qualified clinician before considering any peptide.

Best evidence
Grade A
Conditions studied
1
Outcomes
11
Graded outcomes
5303

Evidence by condition

  • Strong
  • Moderate
  • Limited
  • Very limited

1 condition, plus general outcomes

Prostate Cancer: outcomes studied for Degarelix (Firmagon)
GradeOutcomeEffectSizeStudiesPeopleStudies list
Disease Control

Pooled analysis of 5 RCTs confirms non-inferior disease control. Better S-ALP control suggests improved bone metastases management.

Improves (the measure goes up)Large effect17 studies

Studies that measured disease control

and 7 more in the citations list

Testosterone Suppression

Phase III: 97.2% achieve T ≤0.5 ng/mL. 96% castrate by day 3 (vs 0% leuprolide). Fastest testosterone suppression among ADT options.

Improves (the measure goes down)Large effect14 studies

Studies that measured testosterone suppression

and 4 more in the citations list

PSA Suppression

Median PSA significantly lower at days 14 and 28 vs leuprolide (p<0.001). Faster PSA decline than GnRH agonists.

Improves (the measure goes down)Large effect14 studies

Studies that measured psa suppression

and 4 more in the citations list

PSA Progression-Free Survival

Extension trial showed statistically significant PSA PFS benefit for degarelix over leuprolide with 27.5-month median follow-up.

Improves (the measure goes up)Moderate effect14 studies

Studies that measured psa progression-free survival

and 4 more in the citations list

Flare Prevention

No testosterone flare by design (antagonist mechanism). Eliminates need for antiandrogen flare protection therapy.

Improves (the measure goes up)Large effect14 studies

Studies that measured flare prevention

and 4 more in the citations list

General

General: outcomes studied for Degarelix (Firmagon)
GradeOutcomeEffectSizeStudiesPeopleStudies list
Anti-Cancer Activity

62 human trials and systematic reviews support this finding. Evidence includes systematic reviews/meta-analyses. Human clinical trial data available.

Improves (the measure goes up)Moderate effect20 studies

Studies that measured anti-cancer activity

and 10 more in the citations list

Hormone Levels

10 human trials support this finding. Human clinical trial data available.

Improves (the measure goes up)Moderate effect16 studies

Studies that measured hormone levels

and 6 more in the citations list

Safety/Tolerability

13 human trials and systematic reviews support this finding. Evidence includes systematic reviews/meta-analyses. Human clinical trial data available.

Improves (the measure goes up)Moderate effect13 studies

Studies that measured safety/tolerability

and 3 more in the citations list

Blood Glucose Control

2 human trials and systematic reviews support this finding. Evidence includes systematic reviews/meta-analyses. Human clinical trial data available.

Improves (the measure goes down)Small effect5 studies
Cardiac Protection

2 preclinical studies support this finding. Primarily preclinical evidence.

Improves (the measure goes up)Small effect4 studies
Immune Function

2 preclinical studies support this finding. Primarily preclinical evidence.

Improves (the measure goes up)Small effect4 studies

Key findings

  • Disease ControlProstate CancerImproves (the measure goes up)
  • Testosterone SuppressionProstate CancerImproves (the measure goes down)
  • PSA SuppressionProstate CancerImproves (the measure goes down)

Studies cited

57 studies from PubMed

  1. Testosterone recovery after androgen deprivation therapy.Urologic oncology, 2025 · PMID 39242300
  2. Exploration of cardiac adverse events associated with relugolix and degarelix: a multi-center pharmacovigilance study based on the FAERS database.Expert opinion on drug safety, 2025 · PMID 40177731
  3. Comparative Cardiovascular Safety of Gonadotropin-releasing Hormone Antagonists and Agonists Among Patients Diagnosed with Prostate Cancer: A Systematic Review and Meta-analysis of Real-world Evidence Studies.European urology oncology, 2025 · PMID 39343637
  4. Risk of cardiovascular disease following degarelix versus gonadotropin-releasing hormone agonists in patients with prostate cancer: a systematic review and meta-analysis.Urologic oncology, 2025 · PMID 39818461
  5. Comparing the risk of cardiovascular disease between degarelix and gonadotropin-releasing hormone agonists:a systematic review and meta-analysis.Frontiers in oncology, 2025 · PMID 41103953
  6. Effectiveness and safety of degarelix compared to GnRH agonists for prostate cancer: a systematic review and meta-analysis.The aging male : the official journal of the International Society for the Study of the Aging Male, 2025 · PMID 41216753
  7. A systematic review and meta-analysis of cardiovascular disease risk with degarelix and GnRH agonists in prostate cancerProstate Cancer Prostatic Dis, 2024 · PMID 39500846
  8. Testosterone bounce predicts favorable prognoses for prostate cancer patients treated with degarelix.The Prostate, 2024 · PMID 38413843
  9. Duration of androgen deprivation therapy with postoperative radiotherapy for prostate cancer: a comparison of long-course versus short-course androgen deprivation therapy in the RADICALS-HD randomised trial.Lancet (London, England), 2024 · PMID 38763153
  10. Risk of cardiovascular events following intermittent and continuous androgen deprivation therapy in patients with nonmetastatic prostate cancer.Urologic oncology, 2024 · PMID 39003108
  11. Androgen Deprivation Therapy Drives a Distinct Immune Phenotype in Localized Prostate Cancer.Clinical cancer research : an official journal of the American Association for Cancer Research, 2024 · PMID 39269310
  12. The landscape of androgen deprivation therapies for the treatment of advanced prostate cancer.Future oncology (London, England), 2024 · PMID 39555581
  13. Sodium-Glucose Cotransporter-2 Inhibitors and Major Adverse Cardiovascular Outcomes: A SMART-C Collaborative Meta-Analysis.Circulation, 2024 · PMID 38583093
  14. Efficacy and Safety of Radiotherapy Plus Relugolix in Men With Localized or Advanced Prostate Cancer.JAMA oncology, 2024 · PMID 38451492
  15. Effects of Catheter-Based Renal Denervation in Hypertension: A Systematic Review and Meta-Analysis.Circulation, 2024 · PMID 39355923
  16. Reversal of Lactate and PD-1-mediated Macrophage Immunosuppression Controls Growth of PTEN/p53-deficient Prostate Cancer.Clinical cancer research : an official journal of the American Association for Cancer Research, 2023 · PMID 36862086
  17. Short-Term DAPT and DAPT De-Escalation Strategies for Patients With Acute Coronary Syndromes: A Systematic Review and Network Meta-Analysis.Circulation. Cardiovascular interventions, 2023 · PMID 37609850
  18. Advances with androgen deprivation therapy for prostate cancer.Expert opinion on pharmacotherapy, 2022 · PMID 35108137
  19. The Efficacy and Safety of Relugolix Compared with Degarelix in Advanced Prostate Cancer Patients: A Network Meta-analysis of Randomized Trials.European urology oncology, 2022 · PMID 34301529
  20. A review of clinical evidence to assess differences in efficacy and safety of luteinizing hormone-releasing hormone (LHRH) agonist (goserelin) and LHRH antagonist (degarelix).Indian journal of cancer, 2022 · PMID 35343199
  21. Real-World Evidence Prediction of a Phase IV Oncology Trial: Comparative Degarelix vs Leuprolide Safety.JNCI cancer spectrum, 2022 · PMID 35947646
  22. Cardiovascular Safety of Degarelix Versus Leuprolide in Patients With Prostate Cancer: The Primary Results of the PRONOUNCE Randomized TrialCirculation, 2021 · PMID 34459214
  23. Degarelix as a neoadjuvant hormonal therapy for acute urinary tract toxicity associated with external beam radiotherapy for intermediate- and high-risk prostate cancer: a propensity score matched analysis.Japanese journal of clinical oncology, 2021 · PMID 32875317
  24. Does Exist a Differential Impact of Degarelix Versus LHRH Agonists on Cardiovascular Safety? Evidences From Randomized and Real-World Studies.Frontiers in endocrinology, 2021 · PMID 34194398
  25. Randomized Phase 2 Trial of Abiraterone Acetate Plus Prednisone, Degarelix, or the Combination in Men with Biochemically Recurrent Prostate Cancer After Radical Prostatectomy.European urology open science, 2021 · PMID 34934969
  26. Efficacy and safety of degarelix in patients with prostate cancer: Results from a phase III study in China.Asian journal of urology, 2020 · PMID 32742930
  27. Cardiovascular Safety of Degarelix Versus Leuprolide for Advanced Prostate Cancer: The PRONOUNCE Trial Study Design.JACC. CardioOncology, 2020 · PMID 34396210
  28. GnRH Antagonists Have Direct Inhibitory Effects On Castration-Resistant Prostate Cancer Via Intracrine Androgen and AR-V7 Expression.Molecular cancer therapeutics, 2019 · PMID 31341032
  29. Effect of Degarelix, a Gonadotropin-Releasing Hormone Receptor Antagonist for the Treatment of Prostate Cancer, on Cardiac Repolarisation in a Randomised, Placebo and Active Comparator Controlled Thorough QT/QTc Trial in Healthy Men.Clinical drug investigation, 2017 · PMID 28660498
  30. Degarelix treatment is compatible with diabetes and antithrombotic therapy in patients with prostate cancer.Research and reports in urology, 2017 · PMID 29264358
  31. Degarelix for Treating Advanced Hormone-Dependent Prostate Cancer: An Evidence Review Group Perspective of a NICE Single Technology Appraisal.PharmacoEconomics, 2017 · PMID 27943135
  32. Degarelix monotherapy compared with luteinizing hormone-releasing hormone (LHRH) agonists plus anti-androgen flare protection in advanced prostate cancer: an analysis of two randomized controlled trials.Therapeutic advances in urology, 2016 · PMID 27034720
  33. Degarelix for the treatment of advanced prostate cancer compared with GnRh-Agonists: a systematic review and meta-analysis.Medical journal of the Islamic Republic of Iran, 2016 · PMID 27390687
  34. A meta-analysis and systematic review of randomized controlled trials with degarelix versus gonadotropin-releasing hormone agonists for advanced prostate cancer.Medicine, 2016 · PMID 27399062
  35. Degarelix versus goserelin plus bicalutamide therapy for lower urinary tract symptom relief, prostate volume reduction and quality of life improvement in men with prostate cancer: a systematic review and meta-analysis.Urologia internationalis, 2014 · PMID 24603064
  36. Degarelix: a review of its use in patients with prostate cancer.Drugs, 2014 · PMID 24756432
  37. Degarelix versus goserelin (+ antiandrogen flare protection) in the relief of lower urinary tract symptoms secondary to prostate cancer: results from a phase IIIb study (NCT00831233).Urologia internationalis, 2013 · PMID 23258223
  38. The effect of baseline testosterone on the efficacy of degarelix and leuprolide: further insights from a 12-month, comparative, phase III study in prostate cancer patientsBJU Int, 2012 · PMID 22748873
  39. Experience with degarelix in the treatment of prostate cancerClin Prostate Cancer, 2012 · PMID 23372607
  40. Cost-effectiveness analysis of degarelix for advanced hormone-dependent prostate cancer.BJU international, 2012 · PMID 21883830
  41. Rapid elimination kinetics of free PSA or human kallikrein-related peptidase 2 after initiation of gonadotropin-releasing hormone-antagonist treatment of prostate cancer: potential for rapid monitoring of treatment responses.Clinical chemistry and laboratory medicine, 2012 · PMID 22718641
  42. Evaluation of degarelix in the management of prostate cancerCancer Manag Res, 2011 · PMID 21188095
  43. A phase III extension trial with a 1-arm crossover from leuprolide to degarelix: comparison of gonadotropin-releasing hormone agonist and antagonist effect on prostate cancerJ Urol, 2011 · PMID 21788033
  44. Changes in alkaline phosphatase levels in patients with prostate cancer receiving degarelix or leuprolide: results from a 12-month, comparative, phase III studyBJU Int, 2010 · PMID 19912212
  45. Degarelix: a gonadotropin-releasing hormone antagonist for the management of prostate cancerFuture Oncol, 2010 · PMID 20110043
  46. Cardiovascular safety of degarelix: results from a 12-month, comparative, randomized, open label, parallel group phase III trial in patients with prostate cancerJ Urol, 2010 · PMID 20952020
  47. Additional analysis of the secondary end point of biochemical recurrence rate in a phase 3 trial (CS21) comparing degarelix 80 mg versus leuprolide in prostate cancer patients segmented by baseline characteristicsEur Urol, 2010 · PMID 19962227
  48. Degarelix and its therapeutic potential in the treatment of prostate cancerDrugs Today (Barc), 2009 · PMID 19503784
  49. Degarelix: a novel gonadotropin-releasing hormone blocker for the treatment of prostate cancer.Future oncology (London, England), 2009 · PMID 19450172
  50. Degarelix for prostate cancer.Expert opinion on investigational drugs, 2009 · PMID 19453267
  51. Degarelix: a new approach for the treatment of prostate cancer.Neuroendocrinology, 2009 · PMID 19602868
  52. Degarelix (firmagon) for prostate cancer.The Medical letter on drugs and therapeutics, 2009 · PMID 19838145
  53. Degarelix 240/80 mg: a new treatment option for patients with advanced prostate cancer.Expert review of anticancer therapy, 2009 · PMID 19954284
  54. Degarelix acetate for the treatment of prostate cancer.Drugs of today (Barcelona, Spain : 1998), 2009 · PMID 20069136
  55. The efficacy and safety of degarelix: a 12-month, comparative, randomized, open-label, parallel-group phase III study in patients with prostate cancerBJU Int, 2008 · PMID 19035858
  56. Degarelix: a novel gonadotropin-releasing hormone (GnRH) receptor blocker--results from a 1-yr, multicentre, randomised, phase 2 dosage-finding study in the treatment of prostate cancer.European urology, 2008 · PMID 18538469
  57. Drug evaluation: Degarelix--a potential new therapy for prostate cancer.IDrugs : the investigational drugs journal, 2006 · PMID 16871466