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Cetrorelix Acetate

Last updated on October 8, 2021

Drug Approvals

(BANM, US Adopted Name, rINNM)

Cetrorelix AcetateInternational Nonproprietary Names (INNs) in main languages (French, Latin, and Spanish): Acetato de cetrorelix; Cetrorelix, Acetate de; Cetrorelixi Acetas; D-20761; NS-75A; SB-75 (cetrorelix); SB-075 (cetrorelix). N-Acetyl-3-(2-naphthyl)-D-alanyl-p-chloro-D-phenylalanyl-3-(3-pyridyl)-D-alanyl-L-seryl-L-tyrosyl-N5-carbamoyl-D-ornithyl-L-leucyl-L-arginyl-L-prolyl-D-alaniriamide acetate.

C70H92CIN17O14,xC2H4O2 = 1431.0 (cetrorelix).

CAS 120287-85-6 (cetrorelix); 145672-81-7 (cetrorelix acetate)


Adverse Effects and Precautions

Transient reactions at the injection site, including erythema, pruritus, and swelling, may occur. Nausea and headache have been reported occasionally. Systemic hypersensitivity reactions have been reported rarely.

Cetrorelix should not be used in patients with moderate to severe renal or hepatic impairment.


The bioavailability of cetrorelix after subcutaneous injection is about 85%. The mean terminal half-life after a subcutaneous injection of 3 mg is about 60 hours it is less with lower doses (about 5 and 20 hours respectively after single and multiple doses of 250 micrograms).

Uses and Administration

Cetrorelix is a gonadorelin (gonadotrophin-releasing hormone) antagonist used as a component of ovarian stimulation regimens for assisted reproduction in infertility it is used to prevent luteinising hormone surges and premature ovulation. It has also been tried in benign prostatic hyperplasia, malignant neoplasms of the prostate, endometriosis, and for uterine fibroids. Cetrorelix is given by subcutaneous injection as the acetate an intramuscular depot formulation containing cetrorelix embonate is reported to be under development.

For assisted reproduction, doses of cetrorelix acetate equivalent to cetrorelix 250 micrograms daily may be given either in the morning beginning on day 5 or 6 of ovarian stimulation or in the evening beginning on day 5, and continued until ovulation induction. Alternatively a single dose equivalent to 3 mg of cetrorelix may be given on day 7 if follicle growth does not allow ovulation induction within 4 days, additional doses of cetrorelix 250 micrograms once daily may be given until the day of ovulation induction.


Proprietary Preparations

Argentina: Cetrotide

Australia: Cetrotide

Austria: Cetrotide

Belgium: Cetrotide

Brazil: Cetrotide

Canada: Cetrotide

Chile: Cetrotide

Czech Republic: Cetrotide

Denmark: Cetrotide

Finland: Cetrotide

France: Cetrotide

Germany: Cetrotide

Greece: Cetrotide

Hong Kong: Cetrotide

Hungary: Cetrotide

India: Cetrotide

Indonesia: Cetrotide

Ireland: Cetrotide

Israel: Cetrotide

Italy: Cetrotide

Malaysia: Cetrotide

Mexico: Cetrotide

The Netherlands: Cetrotide

Norway: Cetrotide

New Zealand: Cetrotide

Philippines: Cetrotide

Poland: Cetrotide

Portugal: Cetrotide

Russia: Cetrotide

Singapore: Cetrotide

Spain: Cetrotide

Sweden: Cetrotide

Switzerland: Cetrotide

Thailand: Cetrotide

Turkey: Cetrotide

UK: Cetrotide

USA: Cetrotide

Venezuela: Cetrotide

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