Abarelix and other gonadotrophin-releasing hormone antagonists in prostate cancer.

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Kirby RS, Fitzpatrick JM, Clarke N

Abarelix and other gonadotrophin-releasing hormone antagonists in prostate cancer.

BJU Int. 2009 Dec;104(11):1580-4. doi: 10.1111/j.1464-410X.2009.08924.x.

PubMed ID

20053189 [ View in PubMed

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Abstract

Hormonal therapy is the main recommended treatment for locally advanced and metastatic prostate cancer. Luteinizing hormone-releasing hormone (LHRH) agonists, such as buserelin, goserelin, leuprorelin and triptorelin, stimulate the pituitary's gonadotrophin-releasing hormone (GnRH) receptor, ultimately leading to its de-sensitization and subsequent reduction of LH and testosterone levels. However, this reduction is accompanied by a well described increase or 'surge' in LH and testosterone levels, necessitating the concomitant administration of an antiandrogen to combat the potential effects of transient acceleration in cancer activity. Two pure GnRH antagonists have been developed, abarelix and degarelix, that are devoid of any agonist effect on the GnRH receptor and consequently do not result in testosterone flare. Abarelix was the first GnRH antagonist to be developed and was approved by the USA Food and Drug Administration in 2004 for the initiation of hormonal castration in advanced or metastasizing hormone-dependent prostate carcinoma, when rapid androgen suppression is necessary. Clinical data on both abarelix and degarelix show that they can produce rapid and sustained decreases in testosterone to castrate levels without the need for co-administration of an antiandrogen, and with a very low complication rate in the short term.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Buserelin	Gonadotropin-releasing hormone receptor	Protein	Humans	Yes	Not Available	Details
Buserelin	Lutropin-choriogonadotropic hormone receptor	Protein	Humans	Yes	Not Available	Details
Degarelix	Gonadotropin-releasing hormone receptor	Protein	Humans	Yes	Antagonist	Details
Goserelin	Gonadotropin-releasing hormone receptor	Protein	Humans	Yes	Agonist	Details
Goserelin	Lutropin-choriogonadotropic hormone receptor	Protein	Humans	Yes	Agonist	Details

Pharmaco-metabolomics

Drug	Drug Groups	Metabolite	Change	Description
Leuprolide	Approved Investigational	Testosterone	decreased	Leuprolide decreases the level of Testosterone in the blood
Triptorelin	Approved Vet Approved	Testosterone	decreased	Triptorelin decreases the level of Testosterone in the blood
Buserelin	Approved Investigational	Testosterone	decreased	Buserelin decreases the level of Testosterone in the blood
Buserelin	Approved Investigational	Testosterone	increased	Buserelin increases the level of Testosterone in the blood
Goserelin	Approved	Testosterone	decreased	Goserelin decreases the level of Testosterone in the blood