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Cetrorelix

peptide · headlineFDA-approved

Antagonizes GnRH receptors in the pituitary gland

Overview

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

Daily protocol: 0.25 mg SQ once daily starting day 5–6 of ovarian stimulation for 5–10 days. Single-dose protocol: 3 mg SQ once on stimulation day 7 (lasts ~4 days, no daily injections needed). Both protocols used in ART under strict monitoring.

Subcutaneous (SQ)0.25 mg standardrange 0.250.5 mg· Once daily during ovarian stimulation (days 5–10 of cycle)

Caution: Clinical studies often use 0.25–3 mg/day subcutaneously. Use is limited to regulated fertility and endocrine protocols.

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

Stacking & combinations

With

Seractide/ACTH (1-39)

Benefit

Can be integrated with ACTH (1-39) for full hormonal evaluation or support

Lifestyle support

Diet

Adequate hydration supports ovarian function. Avoid alcohol and limit caffeine during stimulation cycles.

Sleep

Adequate rest during stimulation cycles.

Timing

Used exclusively in IVF/fertility protocols under reproductive endocrinologist supervision.

Exercise

Reduce strenuous exercise during ovarian stimulation to minimize ovarian torsion risk.

Research studies

Studies summarized for educational purposes only. Inclusion does not imply human use; referenced research was conducted in vitro, in animal models, or in regulated clinical trials.

Research study

Ovarian stimulation with HMG: results of a prospective randomized phase III European study comparing the luteinizing hormone-releasing hormone (LHRH)-antagonist cetrorelix and the LHRH-agonist buserelin

Albano C, Felberbaum RE, Smitz J, Riethmüller-Winzen H, Engel J, Diedrich K, Devroey P Human Reproduction. 2000;15(3):526-531 View source ↗

Scientific findings

This prospective randomized phase III European multicentre trial allocated 188 patients to the GnRH antagonist cetrorelix and 85 to the GnRH agonist buserelin during HMG-stimulated IVF/ICSI cycles. Premature LH surges occurred in only 1.6% of cetrorelix-treated patients, and the antagonist arm required significantly fewer HMG ampoules and a shorter duration of stimulation. On the day of hCG, the buserelin group showed more small follicles and higher serum estradiol, while fertilization, cleavage, and clinical pregnancy rates were comparable between arms. The authors concluded the short-duration antagonist approach is advantageous with equivalent efficacy.

Plain English

In this large European study, women preparing for IVF received either cetrorelix (a newer 'antagonist' drug) or buserelin (an older 'agonist' drug) to stop their bodies from releasing eggs too early. Cetrorelix worked just as well at preventing early ovulation but needed far fewer days of injections and less fertility medication. Pregnancy rates were similar with both approaches, and the shorter, simpler cetrorelix schedule was seen as a practical advantage for patients.

Research study

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)

Olivennes F, Belaisch-Allart J, Emperaire JC, Dechaud H, Alvarez S, Moreau L, Nicollet B, Zorn JR, Bouchard P, Frydman R Fertility and Sterility. 2000;73(2):314-320 View source ↗

Scientific findings

This multicentre randomized controlled trial compared a single 3 mg dose of cetrorelix administered in the late follicular phase (115 patients) with depot triptorelin, a long-protocol GnRH agonist (39 patients), for prevention of premature LH surges in IVF-ET. No LH surge occurred in any patient after cetrorelix administration. Although the cetrorelix group yielded fewer oocytes and embryos, the proportion of mature oocytes, fertilization rates, and clinical pregnancy rates did not differ significantly, while the antagonist protocol required shorter stimulation, fewer hMG ampoules, and had reduced hyperstimulation risk with excellent tolerability.

Plain English

This study tested whether a single injection of cetrorelix late in the stimulation cycle could reliably prevent eggs from being released prematurely during IVF. It completely prevented early surges in every patient who received it. Compared with the older long-protocol drug, cetrorelix meant fewer injection days and less medication, and although slightly fewer eggs were collected, egg quality, fertilization, and pregnancy rates were comparable, making the single-dose approach an attractive, patient-friendly option.

Research study

A randomised study of GnRH antagonist (cetrorelix) versus agonist (busereline) for controlled ovarian stimulation: effect on safety and efficacy

Xavier P, Gamboa C, Calejo L, Silva J, Stevenson D, Nunes A, Martinez-de-Oliveira J European Journal of Obstetrics & Gynecology and Reproductive Biology. 2005;120(2):185-189 View source ↗

Scientific findings

In this phase III randomized trial, 131 patients undergoing IVF (with or without ICSI) were allocated to a cetrorelix GnRH-antagonist protocol (n=66) or a buserelin GnRH-agonist protocol (n=65). The antagonist protocol produced a significantly shorter stimulation duration (9.5 vs 10.6 days) and a markedly shorter pituitary suppression period (4.6 vs 27.3 days). No significant differences were found in gonadotropin requirements, follicular development, number of oocytes retrieved, fertilization rates, or clinical pregnancy rates, leading the authors to conclude that GnRH antagonists are an effective, safe, and well-tolerated alternative to agonists for controlled ovarian stimulation.

Plain English

This trial directly compared the antagonist drug cetrorelix with the older agonist drug buserelin in women having IVF. Cetrorelix achieved its effect much faster, cutting the pituitary 'shut-down' phase from about four weeks to less than a week and shortening overall treatment. Importantly, the number of eggs collected, fertilization rates, and pregnancy rates were the same, showing the shorter cetrorelix approach is just as effective and safe while being easier on patients.

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

Reconstitution calculator

Subcutaneous (SQ)
Draw to5 units

= 0.05 mL on a U-100 insulin syringe

Concentration5 mg/mL
Doses / vial40

Assumes a U-100 insulin syringe (100 units = 1 mL). This is a preparation aid, not a protocol — dose and route are the prescriber's decision. Use immediately after reconstitution. Do not store.

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

Bioavailability

Oral
Ineffective orally due to enzymatic degradation
Subq
High absorption with peak plasma concentration within 1–2 hours

Storage & handling

Lyophilized

Store at 2–8°C (refrigerate). Protect from light. Stable until expiration date.

Reconstituted

Use immediately after reconstitution. Do not store.

Used for

No condition evidence rows yet.

Legal / compounding

FDA-approved
EU
Approved
FDA
Approved
Canada
Approved
Australia
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.