Iturelix

GnRH Antagonist (decapeptide)Rx: ResearchCompound: Investigational

Also known as: Cetrorelix analogue, D-63153, Iturel

Educational Only — Not medical advice. Consult a qualified clinician before using any peptide.

Summary

Iturelix is a synthetic GnRH antagonist peptide investigated primarily for the treatment of hormone-sensitive conditions such as benign prostatic hyperplasia (BPH) and prostate cancer. Unlike GnRH agonists, it produces immediate suppression of gonadotropins without an initial testosterone surge (flare). Development has been limited and it has not reached regulatory approval.

Mechanism of Action

Competitively blocks gonadotropin-releasing hormone (GnRH) receptors in the pituitary gland, rapidly suppressing LH and FSH secretion, leading to decreased testosterone and estradiol production without an initial flare effect.

Routes of Administration

Subcutaneous

Goals & Uses

  • Suppression of LH and FSHEndocrineModerate
  • Testosterone suppressionOncology/EndocrinologyModerate
  • Prostate cancer hormone therapyOncologyLow
  • Treatment of benign prostatic hyperplasia (BPH)UrologyModerate

Contraindications

  • Pre-existing severe hepatic impairmentHepaticModerate
  • PregnancyPopulationHighPotential fetal risk or insufficient safety data
  • Hypersensitivity to GnRH or GnRH analoguesAllergy/immunologyHigh

Adverse Effects

  • Allergic reactionsImmunologicalRare
  • Injection site reactionsLocalCommon
  • Hot flashesEndocrine / VasomotorCommon
  • Bone density reductionMusculoskeletalUncommon
  • Sexual dysfunction / decreased libidoEndocrine/sexualCommon

Drug Interactions

  • Anticoagulants (e.g., warfarin)Low
  • QT-prolonging agentsModerate

Population Constraints

  • Pediatric populationsAgeRelative
  • Patients with pre-existing cardiovascular diseaseCardiovascularRelative
  • Women of childbearing potentialReproductiveAbsolute

Regulatory Status

  • European UnionInvestigationalInvestigated in European clinical settings but not approved by EMA.
  • United StatesInvestigationalNever received FDA approval; evaluated in early-phase clinical trials only.
  • United KingdomUnknownNo known MHRA approval or formal regulatory review record.

Iturelix has not received approval from the FDA, EMA, or other major regulatory agencies. It has been evaluated in clinical trials but did not advance to approved status.

Evidence & Sources

No sources recorded yet.

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