Basic Profile / Key Facts
Drug Category
- Infertility Agents
- Hormone Antagonists
Dosage Forms
Indications
For the inhibition of premature LH surges in women undergoing controlled ovarian stimulation.
Pharmacology
Cetrorelix is a synthetic decapeptide with gonadotropin-releasing hormone (GnRH) antagonistic activity. GnRH induces the production and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH) from the gonadotrophic cells of the anterior pituitary. Due to a positive estradiol (E2) feedback at midcycle, GnRH liberation is enhanced resulting in an LH-surge. This LH-surge induces the ovulation of the dominant follicle, resumption of oocyte meiosis and subsequently luteinization as indicated by rising progesterone levels. Cetrorelix competes with natural GnRH for binding to membrane receptors on pituitary cells and thus controls the release of LH and FSH in a dose-dependent manner.
Mechanism of Action
Cetrorelix binds to the gonadotropin releasing hormone receptor and acts as a potent inhibitor of gonadotropin secretion. It competes with natural GnRH for binding to membrane receptors on pituitary cells and thus controls the release of LH and FSH in a dose-dependent manner.
Absorption
Rapidly absorbed following subcutaneous injection. The mean absolute bioavailability following subcutaneous administration to healthy female subjects is 85%.
Toxicity
Not Available
Biotrnasformation / Drug Metabolism
In in vitro studies, cetrorelix was stable against phase I- and phase II-metabolism. Cetrorelix was transformed by peptidases, and the (1-4) peptide was the predominant metabolite.
Contraindications
Cetrotide® (cetrorelix acetate for injection) is contraindicated under the following
conditions:
1. Hypersensitivity to cetrorelix acetate, extrinsic peptide hormones or mannitol.
2. Known hypersensitivity to GnRH or any other GnRH analogs.
3. Known or suspected pregnancy, and lactation.
4. Severe renal impairment
Drug Interactions
No formal drug interaction studies have been performed with Cetrotide®.
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