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Cetrorelix

peptide · headlineFDA-approved

Antagonizes GnRH receptors in the pituitary gland

Summary

Cetrorelix is a synthetic GnRH antagonist used to suppress LH and FSH secretion during controlled ovarian stimulation in IVF. It enables precise timing of ovulation and prevents premature hormonal surges that can compromise reproductive outcomes.

How it works

  • Antagonizes GnRH receptors in the pituitary gland
  • Suppresses secretion of LH and FSH from the anterior pituitary
  • Prevents premature LH surge and ovulation during ovarian stimulation
  • Supports controlled follicle development for IVF or ICSI procedures

Dosing

  • unit: mg
    low dose: 0.25
    frequency: Once daily during ovarian stimulation (days 5–10 of cycle)
    high dose: 0.5
    standard dose: 0.25
    administration route: Subcutaneous (SQ)

Cycling

  • Inject 0.25 mg daily during ovarian stimulation (typically days 5–10 of cycle). Used in ART protocols under strict monitoring.

Side effects

common: ["Mild injection site reaction","Headache","Abdominal discomfort"]
warnings: ["May impair fertility if not properly dosed","Should be used under medical supervision during ART cycles"]
long term: ["Long-term hormone suppression risks unknown; short-term ART use well tolerated"]

Chemistry & PK

sequence: Ac-D-Nal-D-Phe-D-His-D-Trp-D-(2-Pal)-D-Tyr-D-Ser-OH
half life: 5–20 hours depending on dose and formulation
degradation: Slow renal and hepatic peptide clearance
molecular weight: 1431.4
molecular formula: C70H92ClN17O14
tissue specificity: Primarily acts on anterior pituitary GnRH receptors

Verified citations

3 · PubMed-checked
  • The LHRH antagonist cetrorelix: a review.reviewPMID 10972520
  • Ovarian stimulation by cetrorelix acetate and HMG for patients with polycystic ovary syndrome.clinicalPMID 15284212
  • Cetrorelix in the treatment of female infertility and endometriosis.reviewPMID 17020439

Used for

No condition evidence rows yet.

Legal / compounding

FDA-approved

Legal status is a hard gate: non-compoundable or delisted agents cannot be filled and are blocked from protocol export. Keep 503A status current.