Cetrorelix is a synthetic peptide gonadotropin-releasing hormone (GnRH) antagonist.
Indication
The injectable generic formulation of cetrorelix is used in assisted reproduction to inhibit premature luteinizing hormone surges. In addition, cetrorelix has indications in hormone-sensitive cancers of the prostate and breast and certain benign gynaecological disorders such as endometriosis, uterine fibroids and endometrial thinning.
Mechanism of Action
Cetrorelix blocks the effects of Gonadotropin Releasing Hormone (GnRH) and regulates the amount of luteinizing hormone (LH) released that triggers ovulation during the menstrual cycle. Some hormone therapies result in premature ovulation which causes eggs to be released before they are capable of being fertilized.
Clearance
1.28 ml/min·kg [adult healthy female with 3 mg single SC administration]
| Cetrorelix sequence: Ac-D-Nal-D-Cpa-D-Pal-Ser-Tyr-D-Cit-Leu-Arg-Pro-D-Ala-NH2 |
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| molecular weight: 1431.04 | molecular formula: C70H92N17O14 |
| CAS No.: [145672-81-7] | US FDA: submitted on 2020/06 (034884) |
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Absorption
The peptide is rapidly absorbed following subcutaneous injection. The mean absolute bioavailability following subcutaneous administration to healthy female subjects is 85%.
Cetrorelix DMF Submission Announcement
SAN JOSE, CA., June 25, 2020 /CPCNewswire/ -- CPC Scientific Inc., a San Jose based CDMO with GMP manufacturing facilities in Hangzhou, is pleased to announce that their drug master file (DMF) for cetrorelix acetate has been submitted to the U.S. Food and Drug Administration and has been issued DMF# 034884. This generic peptide API type II DMF includes characterization and manufacturing controls of the intermediates and final peptide API. Cetrorelix is a synthetic decapeptide [...]