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Degarelix

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Information about Degarelix

Degarelix is a parenterally administered, gonadotropin releasing hormone (GnRH) antagonist that effectively blocks androgen production and is used to treat advanced prostate cancer.   

Liver safety of Degarelix

Degarelix therapy is associated with serum enzyme elevations during therapy, but has yet to be linked to instances of clinically apparent acute liver injury

Mechanism of action of Degarelix

Degarelix (deg" a rel' ix) is synthetic decapeptide antagonist of gonadotropin releasing hormone (GnRH) that blocks GnRH stimulation of luteinizing hormone (LH) and follicular stimulating hormone (FSH) production by the pituitary gland, thereby decreasing the synthesis of testosterone by the testes in men and estrogen by the ovaries in women.  Degarelix has been found to be palliative in advanced prostate cancer with equivalent efficacy to the GnRH agonists, such as leuprolide and goserelin.  Because degarelix is an antagonist of GnRH, it does not cause the initial increase in testosterone synthesis that occurs with use of GnRH agonists. 

FDA approval information for Degarelix

Degarelix was approved for use in the United States in 2008, and current indications are limited to therapy of advanced prostate cancer. 

Brand name for Degarelix

Degarelix is available under the brand name Firmagon as a powder for reconstitution in 80 and 120 mg vials.  The typical dose is 240 mg initially, with maintenance doses of 80 mg every 28 days. 

Side effects of Degarelix

Common side effects include injection site reactions and symptoms typical of hypogonadism such as hot flashes, decreased libido, erectile dysfunction, nausea, diarrhea, weight gain and fluid retention.  Potential severe adverse reactions include acute hypersensitivity reactions.

 


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