Cetrorelix Brand Name– Cetrotide
What is Cetrorelix
Cetrorelix is a synthetic decapeptide with gonadotropin-releasing hormone (GnRH) antagonist activity similar to ganirelix.
The drug is used to inhibit premature leuteinizing hormone (LH) surges in women undergoing controlled ovarian hyperstimulation followed by insemination or assisted reproductive technology (ART) procedures; cetrorelix has also been used off-label for the treatment of endometriosis and benign prostatic hyperplasia (BPH).
Some data indicate that cetrorelix may also be effective in the treatment of uterine leiomyomata, ovarian cancer, and prostate cancer.
When used in infertility, the main advantage of GnRH antagonists versus GnRH agonists (e.g., leuprolide) is a reduction in the required fertility therapy cycle from several weeks (i.e., 3 weeks) to several days.
Secondarily, the onset of GnRH antagonists occurs rapidly after drug initiation, and the effects reverse rapidly, allowing pituitary function to return to baseline within 1—4 days after drug discontinuation.
Thus, pituitary and hormonal release is essentially normalized at the time of embryo transfer or implantation.
It was theorized that these properties would improve embryo viability and pregnancy success rates; however, results from meta-analyses comparing GnRH antagonists to GnRH agonists do not support this theory.
FDA approval for cetrorelix was granted in August 2000.
Indications
- benign prostatic hyperplasia (BPH)
- endometriosis
- infertility
For inhibiting premature leuteinizing hormone (LH) surges in women undergoing controlled ovarian hyperstimulation and subsequent in vitro fertilization (IVF) or other assisted reproductive technology (ART) for the treatment of infertility
Side Effects
- abdominal pain
- anaphylactoid reactions
- antibody formation
- ecchymosis
- elevated hepatic enzymes
- erythema
- fetal death
- headache
- hot flashes
- hypotension
- injection site reaction
- menstrual irregularity
- nausea
- ovarian enlargement
- ovarian hyperstimulation syndrome (OHSS)
- pelvic pain
- pruritus
- rash
- teratogenesis
- vomiting
Monitoring Parameters
- pelvic exam
- pelvic ultrasound
- serum estradiol concentrations
- serum gonadotropin concentrations
- weight
Contraindications
- atopy
- breast-feeding
- children
- geriatric
- hepatic disease
- mannitol hypersensitivity
- obesity
- ovarian cyst
- ovarian failure
- polycystic ovary syndrome
- pregnancy
- renal failure
- renal impairment
- tobacco smoking
Interactions
- Aripiprazole
- Asenapine
- atypical antipsychotic
- Brexpiprazole
- Cariprazine
- Cimetidine
- Clozapine
- Fluoxetine; Olanzapine
- Haloperidol
- Iloperidone
- Loxapine
- Lumateperone
- Lurasidone
- Molindone
- Olanzapine
- Paliperidone
- Phenothiazines
- Pimozide
- Prasterone, Dehydroepiandrosterone, DHEA (Dietary Supplements)
- Prasterone, Dehydroepiandrosterone, DHEA (FDA-approved)
- Quetiapine
- Risperidone
- Tetrabenazine
- Thiothixene
- Ziprasidone
Mechanism of Action
- During assisted reproductive technology (ART), roughly 30% of women undergoing controlled ovarian hyperstimulation experience a marked rise in estrogen levels in response to follicle stimulating hormone (FSH), which can trigger an early surge of luteinizing hormone (LH) and premature ovulation during the menotropin or follitropin treatments.
- The eggs that are released prematurely typically do not lead to successful conception or implantation.
- By taking control of the pituitary release of LH with either gonadotropin-releasing hormone (GnRH) agonists (e.g., leuprolide) or GnRH antagonists (e.g., cetrorelix), fertility specialists can prevent the premature LH surge and improve the success rate of the fertility procedure.46911
- In the typical protocol, cetrorelix is initiated on roughly day 5 to 9 of FSH or menotropins therapy. Cetrorelix suppresses LH production by competitively blocking the GnRH receptors directly at the pituitary level.
- Rapid and reversible suppression of gonadotropin secretion occurs within a few days; cetrorelix induced suppression of endogenous LH is more pronounced than the suppression of endogenous FSH.
- The production of the LH surge, which is required for ovulation and the initiation of the luteal phase of the cycle, is thus placed in the control of the fertility specialist.
- The LH surge is artificially induced by the proper timing of human chorionic gonadotropin (HCG) administration once the follicles have obtained appropriate size (e.g. 17 mm or more) as indicated by ultrasound.
- Following HCG administration, cetrorelix and FSH are discontinued and final maturation of the oocytes occurs.
- Thereafter, either ovulation can ensue for timed insemination, or oocyte retrieval can take place for ART procedures such as in vitro fertilization (IVF).
