Information about Goserelin
Goserelin is a parenterally administered, gonadotropin releasing hormone (GnRH) agonist which causes an inhibition of estrogen and androgen production and is used predominantly to treat prostate cancer.
Liver safety of Goserelin
Goserelin has been associated with a modest rate of serum enzyme elevations during therapy, but has not been convincingly linked to instances of clinically apparent acute liver injury.
Mechanism of action of Goserelin
Goserelin (goe" se rel' in) is a synthetic decapeptide analogue of gonadotropin releasing hormone that acts as a partial agonist of the gonadotropin receptors in the pituitary that regulate luteinizing hormone (LH) and follicle stimulating hormone (FSH) secretion.
These gonadotropins cause production and secretion of testosterone by the male testes and estrogen by the female ovaries.
The continued receptor occupancy by goserelin, however, ultimately causes a down-regulation of production of LH and FSH and a resultant decrease in testosterone and estrogen levels.
Goserelin, alone or in combination with other antiandrogens, has been found to be palliative in advanced prostate cancer.
FDA approval information for Goserelin
Goserelin was approved for use in the United States in 1989 and is still widely used, being considered important adjuvant therapy in management of advanced prostate cancer.
Advanced breast cancer
Off label use
Brand name for Goserelin
Goserelin is available under the brand name Zoladex in solution for administration subcutaneously as implants every 4 (3.6 mg) or 12 (10.8 mg) weeks.
Goserelin and the other GnRH analogues cause a profound hypogonadism ("chemical castration") .
Side effects of Goserelin
Rare side effects
Rare, but potentially severe adverse events can include immediate hypersensitivity reactions, pituitary apoplexy and, with long term use, weight gain, metabolic changes, diabetes and osteoporosis.
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