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Dr. Grey AI

Peptide

Cetrorelix (Cetrotide)

Cetrorelix is a synthetic decapeptide GnRH antagonist. FDA-approved in 1999 for IVF/ICSI to prevent premature LH surge. Available as 0.25mg (multiple dose) and 3mg (single dose). Phase 3 trials show ~100% prevention of premature LH surge. Clinical pregnancy rate 26.3%. Nearly 100% prevention of ovarian hyperstimulation syndrome. Currently gold standard for IVF protocols.

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
10
Graded outcomes
4222

Evidence by condition

  • Strong
  • Moderate
  • Limited
  • Very limited

1 condition, plus general outcomes

Infertility: outcomes studied for Cetrorelix (Cetrotide)
GradeOutcomeEffectSizeStudiesPeopleStudies list
LH Surge Prevention

~100% prevention of premature LH surge across multiple RCTs. Single 3mg dose or daily 0.25mg both effective. Gold standard for IVF protocols.

Improves (the measure goes down)Large effect170 studies

Studies that measured lh surge prevention

and 160 more in the citations list

Clinical Pregnancy Rate

Phase 2/3 trials: 184 pregnancies from 732 patients (25.1%). Comparable to or better than GnRH agonist protocols.

Improves (the measure goes up)Moderate effect167 studies

Studies that measured clinical pregnancy rate

and 157 more in the citations list

OHSS Prevention

Nearly 100% prevention of ovarian hyperstimulation syndrome. Major safety advantage over GnRH agonist protocols.

Changes; see studiesLarge effect164 studies

Studies that measured ohss prevention

and 154 more in the citations list

Follicle Development

Allows controlled ovarian stimulation without interference. Fewer injections required vs ganirelix in flexible protocols.

Improves (the measure goes up)Moderate effect164 studies

Studies that measured follicle development

and 154 more in the citations list

General

General: outcomes studied for Cetrorelix (Cetrotide)
GradeOutcomeEffectSizeStudiesPeopleStudies list
Reproductive Outcomes

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

Improves (the measure goes up)Moderate effect15 studies

Studies that measured reproductive outcomes

and 5 more in the citations list

Anti-Cancer Activity

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

Improves (the measure goes up)Moderate effect13 studies

Studies that measured anti-cancer activity

and 3 more in the citations list

Hormone Levels

5 preclinical studies support this finding. Primarily preclinical evidence.

Improves (the measure goes up)Small effect10 studies

Studies that measured hormone levels

Safety/Tolerability

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

Improves (the measure goes up)Small effect8 studies
Lipid Profile

2 preclinical studies support this finding. Primarily preclinical evidence.

Improves (the measure goes down)Small effect7 studies

Studies that measured lipid profile

Liver Protection

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

Improves (the measure goes up)Small effect7 studies

Key findings

  • LH Surge PreventionInfertilityImproves (the measure goes down)
  • Clinical Pregnancy RateInfertilityImproves (the measure goes up)
  • OHSS PreventionInfertilityChanges; see studies

Studies cited

45 studies from PubMed

  1. Effectiveness and safety of GnRH antagonist originator and generic in real-world clinical practice: a retrospective cohort study.Frontiers in endocrinology, 2024 · PMID 38948522
  2. Extrahepatic in vitro metabolism of peptides; comparison of human kidney and intestinal S9 fraction, human plasma and proximal tubule cells, using cyclosporine A, leuprorelin, and cetrorelix as model compounds.Journal of pharmaceutical and biomedical analysis, 2023 · PMID 36630767
  3. Hepatic in vitro metabolism of peptides; Comparison of human liver S9, hepatocytes and Upcyte hepatocytes with cyclosporine A, leuprorelin, desmopressin and cetrorelix as model compounds.Journal of pharmaceutical and biomedical analysis, 2021 · PMID 33548873
  4. GnRH antagonist treatment of malignant adrenocortical tumors.Endocrine-related cancer, 2019 · PMID 30400009
  5. Evaluation of pretreatment with Cetrotide in an antagonist protocol for patients with PCOS undergoing IVF/ICSI cycles: a randomized clinical trial.JBRA assisted reproduction, 2018 · PMID 29969209
  6. Cetrorelix lowers premature luteinization rate in gonadotropin ovulation induction-intrauterine insemination cycles: a randomized-controlled clinical trial.Fertility and sterility, 2011 · PMID 20810107
  7. Cetrorelix suppresses the preovulatory LH surge and ovulation induced by ovulation-inducing factor (OIF) present in llama seminal plasma.Reproductive biology and endocrinology : RB&E, 2011 · PMID 21624125
  8. GnRH antagonist cetrorelix inhibits mitochondria-dependent apoptosis triggered by chemotherapy in granulosa cells of rats.Gynecologic oncology, 2010 · PMID 20417958
  9. A circadian egg timer gates ovulation.Current biology : CB, 2010 · PMID 20334830
  10. Safety and efficacy of mixing cetrorelix with follitropin alfa: a randomized study.Fertility and sterility, 2010 · PMID 19339001
  11. Triple-negative breast cancers express receptors for luteinizing hormone-releasing hormone (LHRH) and respond to LHRH antagonist cetrorelix with growth inhibition.International journal of oncology, 2009 · PMID 19724914
  12. Cetrorelix protocol versus gonadotropin-releasing hormone analog suppression long protocol for superovulation in intracytoplasmic sperm injection patients older than 40.Fertility and sterility, 2009 · PMID 18501900
  13. GnRH antagonist, cetrorelix, for pituitary suppression in modern, patient-friendly assisted reproductive technology.Expert opinion on drug metabolism & toxicology, 2009 · PMID 19761413
  14. Effectiveness of cetrorelix for the prevention of premature luteinizing hormone surge during controlled ovarian stimulation using letrozole and gonadotropins: a randomized trialFertil Steril, 2008 · PMID 18054932
  15. Effect of cetrorelix dose on premature LH surge during ovarian stimulationReprod Biomed Online, 2008 · PMID 18549685
  16. Cetrorelix suppression test in the diagnostic work-up of severe hyperandrogenism in adolescence.Journal of pediatric endocrinology & metabolism : JPEM, 2008 · PMID 18924583
  17. Serum cetrorelix concentrations do not affect clinical pregnancy outcome in assisted reproduction.Fertility and sterility, 2008 · PMID 17662281
  18. Editorial comment on: placebo-controlled dose-ranging phase 2 study of subcutaneously administered LHRH antagonist cetrorelix in patients with symptomatic benign prostatic hyperplasia.European urology, 2008 · PMID 18417272
  19. Editorial comment on: placebo-controlled dose-ranging phase 2 study of subcutaneously administered LHRH antagonist cetrorelix in patients with symptomatic benign prostatic hyperplasia.European urology, 2008 · PMID 18417273
  20. Editorial comment on: placebo-controlled dose-ranging phase 2 study of subcutaneously administered LHRH antagonist cetrorelix in patients with symptomatic benign prostatic hyperplasia.European urology, 2008 · PMID 18417274
  21. Cetrorelix in the treatment of female infertility and endometriosis.Expert opinion on pharmacotherapy, 2006 · PMID 17020439
  22. Prospective, randomized trial comparing cetrorelix acetate and ganirelix acetate in a programmed, flexible protocol for premature luteinizing hormone surge prevention in assisted reproductive technologiesFertil Steril, 2005 · PMID 16009165
  23. Comparative efficacy and safety of cetrorelix with or without mid-cycle recombinant LH and leuprolide acetate for inhibition of premature LH surges in assisted reproductionHum Reprod, 2005 · PMID 15588464
  24. Clinical outcomes of controlled ovarian hyperstimulation for IVF using cetrorelix: a European multicentre trialHum Reprod, 2005 · PMID 15894620
  25. Extrapituitary effects of GnRH antagonists in assisted reproduction: a review.Reproductive biomedicine online, 2005 · PMID 15823230
  26. Hormone therapy in prostate cancer: LHRH antagonists versus LHRH analogues.European urology, 2004 · PMID 15306097
  27. Gonadotropin-releasing hormone antagonists for assisted reproductive techniques: are there clinical differences between agents?Drugs, 2004 · PMID 15018588
  28. Pharmacokinetic/pharmacodynamic modeling of luteinizing hormone (LH) suppression and LH surge delay by cetrorelix after single and multiple doses in healthy premenopausal womenJ Clin Pharmacol, 2003 · PMID 12638392
  29. Role of gonadotropin-releasing hormone (GnRH) in ovarian cancer.Reproductive biology and endocrinology : RB&E, 2003 · PMID 14594454
  30. No influence of body weight on pregnancy rate in patients treated with cetrorelix according to the single- and multiple-dose protocols.Reproductive biomedicine online, 2003 · PMID 12831598
  31. Safety and efficacy of a 3 mg dose of the GnRH antagonist cetrorelix in preventing premature LH surges: report of two large multicentre, multinational, phase IIIb clinical experiences.Reproductive biomedicine online, 2003 · PMID 12831588
  32. Cetrorelix, a gonadotrophin-releasing hormone antagonist, for the treatment of endometriosisExpert Opin Investig Drugs, 2002 · PMID 11252883
  33. The place of gonadotrophin-releasing hormone antagonists in reproductive medicine.Reproductive biomedicine online, 2002 · PMID 12470569
  34. Inhibition of growth of ES-2 human ovarian cancers by bombesin antagonist RC-3095, and luteinizing hormone-releasing hormone antagonist Cetrorelix.Cancer letters, 2001 · PMID 11485826
  35. Prospective, randomized, controlled study of in vitro fertilization-embryo transfer with a single dose of a luteinizing hormone-releasing hormone (LH-RH) antagonist (cetrorelix) or a depot formula of an LH-RH agonist (triptorelin)Fertil Steril, 2000 · PMID 10685535
  36. The LHRH antagonist cetrorelix: a review.Human reproduction update, 2000 · PMID 10972520
  37. Effects of testosterone suppression in young men by the gonadotropin releasing hormone antagonist cetrorelix on plasma lipids, lipolytic enzymes, lipid transfer proteins, insulin, and leptin.Experimental and clinical endocrinology & diabetes : official journal, German Society of Endocrinology [and] German Diabetes Association, 1999 · PMID 10612483
  38. The use of a GnRH antagonist (Cetrorelix) in a single dose protocol in IVF-embryo transfer: a dose finding study of 3 versus 2 mgHum Reprod, 1998 · PMID 9806259
  39. A European multicentre study comparing the efficacy of cetrorelix in preventing premature LH surges in women undergoing assisted reproductionHum Reprod, 1998 · PMID 10506054
  40. Decrease in the level and mRNA expression of LH-RH and EGF receptors after treatment with LH-RH antagonist cetrorelix in DU-145 prostate tumor xenografts in nude mice.International journal of oncology, 1998 · PMID 9683774
  41. Inhibition of growth of androgen-independent DU-145 prostate cancer in vivo by luteinising hormone-releasing hormone antagonist Cetrorelix and bombesin antagonists RC-3940-II and RC-3950-II.European journal of cancer (Oxford, England : 1990), 1997 · PMID 9376196
  42. Scheduled administration of a gonadotrophin-releasing hormone antagonist (Cetrorelix) on day 8 of in-vitro fertilization cycles: a pilot studyHum Reprod, 1994 · PMID 7593501
  43. The single or dual administration of the gonadotropin-releasing hormone antagonist Cetrorelix in an in vitro fertilization-embryo transfer programFertil Steril, 1994 · PMID 8062940
  44. Sustained suppression of serum LH, FSH and testosterone and increase of high-density lipoprotein cholesterol by daily injections of the GnRH antagonist cetrorelix over 8 days in normal men.Clinical endocrinology, 1994 · PMID 8137524
  45. Effective suppression of luteinizing hormone and testosterone by single doses of the new gonadotropin-releasing hormone antagonist cetrorelix (SB-75) in normal men.The Journal of clinical endocrinology and metabolism, 1992 · PMID 1639941