Abarelix

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Abarelix
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INN
Drug class
Routes of administration	Intramuscular injection
Pregnancy category
Bioavailability
Metabolism
Elimination half-life
Excretion
Legal status
CAS Number	183552-38-7
PubChem	6918285
DrugBank	DB00096
ChemSpider	5293517
KEGG	D02906

Abarelix is a gonadotropin-releasing hormone antagonist (GnRH antagonist) used in the treatment of prostate cancer. It is marketed under the trade name Plenaxis. Abarelix works by directly inhibiting the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the pituitary gland, which in turn reduces the production of testosterone by the testes.

Medical uses

Abarelix is primarily used in the treatment of advanced prostate cancer to reduce the levels of testosterone, which can stimulate the growth of cancer cells. It is administered via intramuscular injection.

Mechanism of action

Abarelix is a synthetic decapeptide that acts as a gonadotropin-releasing hormone antagonist. By binding to the GnRH receptors in the pituitary gland, it prevents the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This suppression leads to a decrease in testosterone production by the testes, which is beneficial in the treatment of hormone-sensitive prostate cancer.

Side effects

Common side effects of Abarelix include hot flashes, fatigue, and nausea. Serious side effects may include allergic reactions and cardiovascular events. Patients receiving Abarelix should be monitored for signs of hypersensitivity and other adverse reactions.

History

Abarelix was developed as an alternative to GnRH agonists, which initially stimulate the release of LH and FSH before suppressing them, potentially causing a temporary surge in testosterone levels. Abarelix was approved for medical use in the early 2000s.

See also

• Prostate cancer
• Gonadotropin-releasing hormone antagonist
• Luteinizing hormone
• Follicle-stimulating hormone
• Testosterone