Version July 2025
Controlled ovarian stimulation: SUBQ: 0.25 mg once daily the morning or evening of ovarian stimulation day 5, or morning of ovarian stimulation day 6; continue 0.25 mg once daily until the day hCG is administered.
Mild to moderate impairment: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
Severe impairment: Use is contraindicated.
There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Reported adverse reactions are for adults.
1% to 10%:
Gastrointestinal: Nausea (1%)
Genitourinary: Ovarian hyperstimulation syndrome (4%)
Hepatic: Increased liver enzymes (1% to 2%; including increased gamma-glutamyl transferase, increased serum alanine aminotransferase, increased serum alkaline phosphatase, increased serum aspartate aminotransferase)
Nervous system: Headache (1%)
Postmarketing:
Hypersensitivity: Anaphylaxis, hypersensitivity reaction, nonimmune anaphylaxis
Local: Injection-site reaction (including bruising at injection site, erythema at injection site, injection-site pruritus, swelling at injection site)
Hypersensitivity to cetrorelix, extrinsic peptide hormones, gonadotropin releasing hormone (GnRH) or other GnRH analogs, mannitol, or any component of the formulation; severe renal impairment; pregnancy; breastfeeding.
Canadian labeling: Additional contraindications (not in the US labeling): Moderate to severe hepatic function impairment; moderate renal function impairment.
Concerns related to adverse effects:
• Hypersensitivity: Hypersensitivity reactions, including severe anaphylactoid reactions, have been reported after initial dose and months after starting therapy; use with caution in patients with signs and symptoms of active allergic conditions or known history of allergic predisposition. Treatment is not recommended in patients with severe allergic conditions.
Other warnings/precautions:
• Experienced specialists: Should only be prescribed by fertility specialists.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Kit, Subcutaneous:
Cetrotide: 0.25 mg [contains mannitol]
Generic: 0.25 mg
Kit, Subcutaneous [preservative free]:
Generic: 0.25 mg
Yes
Kit (Cetrorelix Acetate Subcutaneous)
0.25 mg (per each): $240.86 - $326.87
Kit (Cetrotide Subcutaneous)
0.25 mg (per each): $379.34
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Kit, Subcutaneous:
Cetrotide: 0.25 mg [contains mannitol]
SUBQ: Administer by SUBQ injection following proper aseptic technique procedures. Injections should be to the lower abdomen, preferably around the navel (but staying at least 1 inch from the navel). The injection site should be rotated daily.
Hazardous agent (NIOSH 2024 [table 2]).
Use appropriate precautions for receiving, handling, storage, preparation, dispensing, transporting, administration, and disposal. Follow NIOSH and USP 800 recommendations and institution-specific policies/procedures for appropriate containment strategy (NIOSH 2023; NIOSH 2024; USP-NF 2020).
Note: Facilities may perform risk assessment of some hazardous drugs to determine if appropriate for alternative handling and containment strategies (USP-NF 2020). Refer to institution-specific handling policies/procedures.
Controlled ovarian stimulation: Inhibition of premature luteinizing hormone surges in patients undergoing controlled ovarian stimulation.
The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drugs (contraindicated in pregnancy) which have a heightened risk of causing significant patient harm when used in error (High-Alert Medications in Community/Ambulatory Care Settings).
None known.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.
Flotufolastat F18: Coadministration of Androgen Deprivation Therapy Agents and Flotufolastat F18 may alter diagnostic results. Management: Androgen deprivation therapy (ADT) may result in changes in the uptake of flotufolastat F18 in prostate cancer. The impact of ADT on the performance of flotufolastat F18 is unknown, but use of alternative agents should be considered. Risk D: Consider Therapy Modification
Gallium Ga 68 PSMA-11: Androgen Deprivation Therapy Agents may decrease therapeutic effects of Gallium Ga 68 PSMA-11. Management: Androgen deprivation therapy (ADT) may result in changes in the uptake of gallium Ga 68 PSMA-11 (gozetotide) in prostate cancer. The impact of ADT on the performance of gallium Ga 68 PSMA-11 is unknown, but use of alternative agents should be considered. Risk D: Consider Therapy Modification
Indium 111 Capromab Pendetide: Coadministration of Antigonadotropic Agents and Indium 111 Capromab Pendetide may alter diagnostic results. Risk X: Avoid
Piflufolastat F18: Coadministration of Androgen Deprivation Therapy Agents and Piflufolastat F18 may alter diagnostic results. Management: Androgen deprivation therapy (ADT) may result in changes in the uptake of piflufolastat F18 in prostate cancer. The impact of ADT on the performance of piflufolastat F18 is unknown, but use of alternative agents should be considered. Risk D: Consider Therapy Modification
Evaluate pregnancy status before beginning treatment. Ovarian stimulation may be initiated with gonadotropins (FSH, hMG) on day 2 or 3 of a regular menstrual cycle followed by cetrorelix administered either on a specific day of the cycle, or when follicles reach an appropriate size (Al-Inany 2016).
Based on data from animal reproduction studies, resorption resulting in fetal loss would be expected. Major congenital abnormalities have been reported following in utero exposure to cetrorelix; however, a causal link has not been determined.
Use is contraindicated in pregnant patients.
It is not known if cetrorelix is present in breast milk.
Use while breastfeeding is contraindicated.
Ultrasound to assess follicle size
Competes with naturally-occurring GnRH for binding on receptors of the pituitary. This delays luteinizing hormone surge, preventing ovulation until the follicles are of adequate size.
Onset of action: Luteinizing hormone suppression 0.25 mg dose: ~2 hours.
Duration: Luteinizing hormone suppression 0.25 mg dose: 24 hours.
Absorption: Rapid.
Distribution: Vd: ~1 L/kg.
Protein binding: 86%.
Metabolism: Transformed by peptidases; cetrorelix and peptides (1-9), (1-7), (1-6), and (1-4) are found in the bile; peptide (1-4) is the predominant metabolite.
Bioavailability: SUBQ: 85%.
Half-life elimination: 0.25 mg dose: 5 hours; 0.25 mg multiple doses: 20.6 hours.
Time to peak: 1 to 2 hours.
Excretion: Feces (5% to 10% as unchanged drug and metabolites); urine (2% to 4% as unchanged drug).
