Brands, Medical Use, Clinical Data
Drug Category
- Hormone Antagonists
- Anti-gonadotrophin-releasing hormones
- ATC code: H01CC01
Dosage Forms
Brands / Synonyms
; Ganirelix
Description
Ganirelix is a synthetic decapeptide with high antagonistic activity against naturally occurring gonadotropin-releasing hormone (GnRH). Ganirelix acetate is derived from native GnRH with substitutions of amino acids at positions 1, 2, 3, 6, 8, and 10
Indications
Indicated for the inhibition of premature LH surges in women undergoing controlled ovarian hyperstimulation
Pharmacology
Ganirelix is a GnRH antagonist, which modulates the hypothalamic-pituitary-gonadal axis by competitive binding to the GnRH receptors in the pituitary gland. As a result a rapid, profound, reversible suppression of endogenous gonadotrophins occurs, without initial stimulation as induced by GnRH agonists.
Mechanism of Action
Ganirelix acts by competitively blocking the GnRH receptors on the pituitary gonadotroph and subsequent transduction pathway. It induces a rapid, reversible suppression of gonadotropin secretion. The suppression of pituitary LH secretion by Ganirelix is more pronounced than that of FSH. An initial release of endogenous gonadotropins has not been detected with Ganirelix, which is consistent with an antagonist effect.
Absorption
Rapidly absorbed following subcutaneous injection. The mean absolute bioavailability of Ganirelix following a single 250 µg subcutaneous injection to healthy female volunteers is 91.1%.
Toxicity
Not Available
Biotrnasformation / Drug Metabolism
Metabolized into smaller peptides
Contraindications
Antagon™ (ganirelix acetate) Injection is contraindicated under the following conditions:
- Known hypersensitivity to Antagon™ or to any of its components.
- Known hypersensitivity to GnRH or any other GnRH analog.
- Known or suspected pregnancy.
Drug Interactions
No formal drug-drug interaction studies have been performed.
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