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Active ingredient: Ganirelix - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Hormone Antagonists
  • Anti-gonadotrophin-releasing hormones
  • ATC code: H01CC01

Dosage Forms

  • Liquid
  • Solution

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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