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

Brands, Medical Use, Clinical Data

Drug Category

  • Anti-Testosterone Agents
  • Antineoplastic Agents

Dosage Forms

  • Suspension (IM Injection)

Brands / Synonyms

Plenaxis; Plenaxis (Praecis Pharmaceuticals)

Description

Synthetic decapeptide antagonist to gonadotropin releasing hormone (GnRH)

Indications

For palliative treatment of advanced prostate cancer.

Pharmacology

Used in the palliative treatment of advanced prostate cancer. Abarelix is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis.

Mechanism of Action

Abarelix binds to the gonadotropin releasing hormone receptor and acts as a potent inhibitor of gonadotropin secretion.

Absorption

Following IM administration of 100 mg, abarelix is absorbed slowly with a mean peak concentration of 43.4 ng/mL observed approximately 3 days after the injection.

Toxicity

The maximum tolerated dose of abarelix has not been determined. The maximum dose used in clinical studies was 150 mg. There have been no reports of accidental overdose with abarelix.

Biotrnasformation / Drug Metabolism

In vitro hepatocyte (rat, monkey, human) studies and in vivo studies in rats and monkeys showed that the major metabolites of abarelix were formed via hydrolysis of peptide bonds. No significant oxidative or conjugated metabolites of abarelix were found either in vitro or in vivo. There is no evidence of cytochrome P-450 involvement in the metabolism of abarelix.

Contraindications

Not Available

Drug Interactions

Not Available

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