(BANM, US Adopted Name, rINNM)
International 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)
AIC — H01CC02
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.
Czech Republic: Cetrotide
Hong Kong: Cetrotide
The Netherlands: Cetrotide
New Zealand: Cetrotide