ApprovedReproductive & hormoneSubcutaneousEvidence 4/5

Cetrorelix

Also known as: Cetrotide

Cetrorelix competitively blocks pituitary GnRH receptors, immediately and reversibly suppressing LH and FSH release to prevent a premature LH surge without the initial flare seen with GnRH agonists.

Cetrorelix
Drug class
GnRH antagonist (synthetic decapeptide)
Primary targets
GnRH receptor, Pituitary gonadotrophs, Luteinizing hormone (LH), Follicle-stimulating hormone (FSH)
Dose reference
Reference label regimens (not recommendations): 0.25 mg subcutaneously every 24 hours during the late follicular phase, or a single 3 mg subcutaneous dose providing at least 4 days of action.
Half-life
Median ~5 hours after a single 0.25 mg dose and ~62.8 hours after a single 3 mg dose (Cetrotide label)
Developer / origin
Originated with ASTA Medica (Germany); US product marketed by EMD Serono
Reference year
2000
Evidence score
4/5 - Strong

Approved uses

  • Inhibition of premature LH surges in women undergoing controlled ovarian stimulation
Evidence 4/5

Strong

Cetrorelix is FDA-approved (2000) with a clear labeled indication, well-characterized pharmacology, and supporting IVF literature; evidence is strong but narrow to controlled ovarian stimulation.

Investigational compound with human randomized or phase 2/3 evidence.

Evidence basis

  • FDA-approved Cetrotide prescribing information defines indication, dosing, pharmacokinetics and safety
  • Peer-reviewed reviews and pharmacodynamic studies characterize GnRH antagonist mechanism and LH/FSH suppression
  • Multiple IVF clinical studies evaluate antagonist protocols using cetrorelix

How to read this entry

Dose references and half-life values are pulled from trial protocols, labels, reviews, or published summaries where available. They are context for research and comparison, not a personal dosing recommendation.

Status matters: approved drugs have regulated indications; investigational compounds are still being studied; research-only peptides do not have established human dosing, safety, or efficacy for consumer use.

Cetrorelix guides

Read the matching guide or adjacent research pages for more context.

Peptide calculators

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Compare with related peptides

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5/5
Reproductive & hormoneApproved

Triptorelin is a potent GnRH-receptor agonist that first transiently stimulates LH and FSH release, then, with continuous exposure, downregulates and desensitizes pituitary GnRH receptors to suppress gonadotropins and sex steroids.

Goserelin

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5/5
Reproductive & hormoneApproved

Goserelin is a synthetic decapeptide GnRH agonist that first stimulates and then, with continuous depot exposure, downregulates pituitary GnRH receptors to suppress LH, FSH and downstream sex steroids toward castrate or postmenopausal levels.

Buserelin

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4/5
Reproductive & hormoneApproved

Buserelin is a GnRH receptor superagonist that initially stimulates and then, with continuous non-pulsatile exposure, desensitizes pituitary gonadotrophs to suppress LH, FSH and downstream testosterone or estradiol production.

Nafarelin

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4/5
Reproductive & hormoneApproved

Nafarelin is a potent GnRH receptor agonist that initially stimulates pituitary LH and FSH release but with continued dosing downregulates the receptor, suppressing gonadotropins and sex steroid production.

Research & educational purposes only

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