Cetrorelix

Summary

Cetrorelix is a synthetic decapeptide GnRH antagonist used in assisted reproductive technology (ART) to prevent premature luteinizing hormone (LH) surges in women undergoing controlled ovarian stimulation. It acts rapidly without the initial gonadotropin flare seen with GnRH agonists.

Mechanism of Action

Competitive antagonist of gonadotropin-releasing hormone (GnRH) receptors in the pituitary gland, suppressing LH and FSH secretion, thereby inhibiting premature LH surges during controlled ovarian stimulation

Routes of Administration

Goals & Uses

• Prevention of premature LH surge during IVFReproductive EndocrinologyHigh
• Prostate cancerOncologyLow
• Controlled ovarian hyperstimulation supportReproductive EndocrinologyHigh
• Uterine fibroidsGynecologyLow
• Endometriosis treatmentGynecologyLow

Contraindications

• Moderate to severe hepatic impairmentHepaticModerate
• Severe renal impairmentOrganHighKidney function concerns
• PregnancyPopulationHighPotential fetal risk or insufficient safety data
• BreastfeedingPopulationHighPotential transfer into breast milk or insufficient safety data
• Hypersensitivity to cetrorelix or extrinsic peptide hormonesAllergyHigh

Adverse Effects

• Injection site reactionsLocalCommon
• HeadacheNeurologicUncommonPain in the head or upper neck
• Hot flashesEndocrine / VasomotorUncommon
• NauseaGastrointestinalUncommonFeeling of sickness or urge to vomit
• Allergic/anaphylactic reactionsImmunologicalRare
• Ovarian hyperstimulation syndrome (OHSS)ReproductiveUncommon

Drug Interactions

• hCG (human chorionic gonadotropin)Moderate
• Gonadotropins (FSH, hMG)Low
• GnRH agonistsHigh

Population Constraints

• Pediatric patientsAgeAbsolute
• Women with known latex allergyAllergyRelative
• Patients with renal impairmentOrgan ImpairmentRelative
• Postmenopausal womenReproductive StatusAbsolute

Regulatory Status

• European UnionApprovedApproved: Prevention of premature LH surges in women undergoing controlled ovarian stimulation for assisted reproductionApproved by EMA; Cetrotide is the primary brand name
• United StatesApprovedApproved: Prevention of premature LH surges in women undergoing controlled ovarian stimulationApproved by FDA in August 1999 under brand name Cetrotide; available as 0.25 mg and 3 mg powder for injection
• United KingdomApprovedApproved: Prevention of premature LH surges in women undergoing controlled ovarian stimulationRetained EU approval post-Brexit; available on NHS for ART

FDA-approved since 1999 (Cetrotide) for prevention of premature LH surges in women undergoing controlled ovarian hyperstimulation. Also approved in EU. Available in 0.25 mg and 3 mg formulations.

Evidence & Sources

No sources recorded yet.