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| Clinical data | |
|---|---|
| Trade names | Zoladex, others |
| Other names | D-Ser(But)6Azgly10-GnRH |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a601002 |
| Routes of administration | Implant |
| Drug class | GnRH analogue;GnRH agonist;Antigonadotropin |
| ATC code | |
| Legal status | |
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| Pharmacokinetic data | |
| Protein binding | 27.3% |
| Eliminationhalf-life | 4–5 hours |
| Identifiers | |
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| IUPHAR/BPS | |
| DrugBank |
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| ChemSpider |
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| UNII | |
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| ChEBI | |
| ChEMBL | |
| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.212.024 |
| Chemical and physical data | |
| Formula | C59H84N18O14 |
| Molar mass | 1269.433 g·mol−1 |
| 3D model (JSmol) | |
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Goserelin, sold under the brand nameZoladex among others, is amedication which is used to suppress production of thesex hormones (testosterone andestrogen), particularly in the treatment ofbreast cancer andprostate cancer.[2][3] It is an injectablegonadotropin releasing hormone agonist (GnRH agonist).
Structurally, it is adecapeptide. It is thenatural GnRH decapeptide with two substitutions to inhibit rapid degradation.
Goserelin stimulates the production of the sex hormones testosterone and estrogen in a non-pulsatile (non-physiological) manner. This causes the disruption of the endogenous hormonal feedback systems, resulting in the down-regulation of testosterone and estrogen production.
It was patented in 1976 and approved for medical use in 1987.[4] Goserelin is a therapeutic alternative on theWorld Health Organization's List of Essential Medicines.[5]
Goserelin is used to treat hormone-sensitive cancers of thebreast (in pre- and peri-menopausal women) andprostate, and some benign gynaecological disorders (endometriosis,uterine fibroids and endometrial thinning). In addition, goserelin is used inassisted reproduction and in the treatment ofprecocious puberty. It may also be used in the treatment of male-to-female transgender people.[6]
Goserelin may causebone pain,hot flashes,headache,stomach upset,depression,difficulty urinating (isolated cases),weight gain,swelling and tenderness of breasts (infrequent),decreased erections andreduced sexual desire. Bone pain can be managed symptomatically, and erectile dysfunction can be treated byvardenafil (Levitra) or other similar oral therapies, although they will not treat the reduced sexual desire. The rates ofgynecomastia with goserelin have been found to range from 1 to 5%.[7]
Short-term memory impairment has also been reported in women and may in some cases be severe, but this effect disappears gradually once treatment is discontinued.[8][9]
Goserelin is a synthetic analogue of a naturally occurringgonadotropin-releasing hormone (GnRH).Bioavailability is almost complete by injection. Goserelin is poorly protein-bound and has a serum elimination half-life of two to four hours in patients with normal renal function. The half-life increases with patients with impaired renal function. There is no significant change in pharmacokinetics in subjects with liver failure. After administration, peak serum concentrations are reached in about two hours. It rapidly binds to the GnRH receptor cells in thepituitary gland thus leading to an initial increase in production ofluteinizing hormone and thus leading to an initial increase in the production of corresponding sex hormones. This initial flare may be treated by co-prescribing/co-administering an androgen receptor antagonist such asbicalutamide (Casodex). Eventually, after a period of about 14–21 days, production of LH is greatly reduced due to receptordownregulation, and sex hormones are generally reduced to castrate levels.[10]
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Goserelin is aGnRH analogue anddecapeptide. It is provided as theacetatesalt.[11]
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Goserelin is thegeneric name[12] of the drug and itsINNTooltip International Nonproprietary Name,USANTooltip United States Adopted Name, andBANTooltip British Approved Name.
