Cetrorelix

Class: Antigonadotropins
- Gonadotropin-releasing Hormone Antagonists
- GnRH Antagonists
ATC Class: H01CC02
VA Class: HS701
Chemical Name: N-Acetyl-3-(2-naphthalenyl)-d-alanyl-4-chloro-d-phenylalanyl-3-(3-pyridinyl)-d-alanyl-l-seryl-l-tyrosyl-N5-(aminocarbonyl-d-ornithyl-l-leucyl-l-arginyl-l-prolyl acetate (salt)
Molecular Formula: C₇₀H₉₂ClN₁₇O₁₄•C₂H₄O₂
CAS Number: 145672-81-7
Brands: Cetrotide

Medically reviewed by Drugs.com on Oct 6, 2021. Written by ASHP.

Introduction

Gonadotropin-releasing hormone (GnRH) antagonist; a synthetic decapeptide analog of naturally occurring GnRH.

Uses for Cetrorelix

Female Infertility

Used as a component of controlled ovarian stimulation regimens (e.g., recombinant FSH or human menopausal gonadotropin [hMG], and human chorionic gonadotropin [hCG]) to delay premature LH surges and consequently ovulation during assisted reproductive technologies (ART) programs.

Cetrorelix Dosage and Administration

General

• Should be prescribed by clinicians experienced in infertility treatment.

• Prior to use of cetrorelix, initiate controlled ovarian stimulation (COS) therapy with gonadotropins (FSH or hMG) usually on day 2 or 3 of the menstrual cycle. Individualize dosage of gonadotropins based on the patient’s ovarian response to allow sufficient follicular development.

• Initiate therapy with cetrorelix on days 5–7 of COS therapy and continue COS therapy until sufficient follicular growth is verified (e.g., ultrasound).

• When ultrasound assessement shows sufficient follicular maturation, discontinue COS therapy and cetrorelix and administer hCG to complete final follicular maturation and induce ovulation. Perform oocyte retrieval, followed by in vitro fertilization or intracytoplasmic sperm injection, with subsequent attempts at implantation and pregnancy.

• Do not administer hCG if the ovaries show an excessive response to treatment with gonadotropins because of an increased risk of ovarian hyperstimulation syndrome.

Administration

Sub-Q Administration

Administer by sub-Q injection either once as a single dose or once daily in multiple smaller doses in early- to mid-follicular phase of the menstrual cycle.

For the single-dose regimen, administer by sub-Q injection once on the day of COS when the serum estradiol concentration is indicative of an appropriate stimulation response (400 pg/mL), usually on stimulation day 7 (range: day 5–9).

For the multiple-dose regimen, administer by sub-Q injection on day 5 (morning or evening) or on the morning of day 6 of COS and continue daily until an adequate follicular response is achieved.

Administer using 27-gauge needle (provided by manufacturer) into lower abdominal area, preferably around, but ≥2.54 cm (1 inch) from the umbilicus. With multiple doses, rotate injection sites to minimize local irritation.

Reconstitution

Reconstitute vial containing 0.25 or 3 mg of cetrorelix acetate.