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Goserelin



Goserelin
Systematic (IUPAC) name
N-[1-[[1-[[1-[[1-[[1-[[1-[[1-[2-
[(carbamoylamino)carbamoyl]pyrrolidin-1-yl]-
5-(diaminomethylideneamino)-1-oxo
-pentan-2-yl]carbamoyl]-3-methyl-
butyl]carbamoyl]-2-tert-butoxy-
ethyl]carbamoyl]-2-(4-hydroxyphenyl)
ethyl]carbamoyl]-2-hydroxy-ethyl]
carbamoyl]-2-(1H-indol-3-yl)ethyl]
carbamoyl]-2-(3H-imidazol-4-yl)ethyl]-
5-oxo-pyrrolidine-2-carboxamide
Identifiers
CAS number 65807-02-5
ATC code L02AE03
PubChem 47725
DrugBank BTD00113
Chemical data
Formula C59H84N18O14 
Mol. mass 1269.410 g/mol
Synonyms D-Ser(But)6Azgly10LHRH
Pharmacokinetic data
Bioavailability  ?
Protein binding 27.3%
Metabolism  ?
Half life 4-5 hours
Excretion renal
Therapeutic considerations
Pregnancy cat.

D (3.6mg) / X (10.8mg) (USA)

Legal status

Prescription only

Routes implant

Goserelin is an injectable gonadotropin releasing hormone super-agonist (GnRH agonist). It stops the production of sex hormones (testosterone and oestrogen).

Goserelin is marketed by AstraZeneca with the brand name Zoladex.[1] It was first launched in 1987 and is currently the second-largest selling GnRH analogue in the world. It is currently available in more than one hundred markets.

Zoladex 3.6 mg subcutaneous monthly biodegradable implant was first approved by the FDA on November 3, 1989[2] for treatment of prostate cancer, a 10.8 mg subcutaneous 3-month biodegradable implant and other indications were subsequently approved.

Additional recommended knowledge

Contents

Pharmacokinetics

Goserelin is an GnRH analogue. It is chemically similar to the body's natural GnRH though it has a greatly extended half-life. After administration, peak serum concentrations are reached in about two hours. It rapidly binds to the GnRH receptor cells in the pituitary gland thus leading to an initial increase in production of luteinizing hormone and thus leading to an initial increase in the production of corresponding sex hormones. Eventually, after a period of about 14-21 days, production of LH is greatly reduced due to receptor downregulation, and sex hormones are generally reduced to castrate levels.[3]

Indications

  Goserelin is used to treat hormone-sensitive cancers of the prostate and breast (in pre-/perimenopausal women) and some benign gynaecological disorders (endometriosis, uterine fibroids and endometrial thinning). In addition, goserelin is used in assisted reproduction and in the treatment of precocious puberty.

It is available as a 1-month depot and a long-acting 3-month depot. Both depots are used for the treatment of prostate cancer, endometriosis and uterine fibroids but only the 1-month depot is approved for breast cancer, endometrial thinning and assisted reproduction.

Side effects

Goserelin causes an increase in bone pain and symptoms of prostatic cancer during the first few weeks of treatment. As the body adjusts to the medication, the symptoms will disappear. Goserelin may cause hot flushes, headache, stomach upset, difficulty urinating, weight gain, swelling and tenderness of breasts, decreased erections, reduced sexual desire.

References

  1. ^ AstraZeneca official Zoladex site
  2. ^ FDA Approval for Zoladex 3.6 mg
  3. ^ Kotake, Toshihiko; Michiyuki Usami, Hideyuki Akaza et al. (August 1999). "Goserelin Acetate with or without Antiandrogen or Estrogen in the Treatment of Patients with Advanced Prostate Cancer: a Multicenter, Randomized, Controlled Trial in Japan". Japanese Journal of Clin. Oncol. 29 (11): 562-570. ISSN 1465-3621. Retrieved on 2007-02-26.
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Goserelin". A list of authors is available in Wikipedia.
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