N- [1- [1- [1- [1- [1- [1- [1- [2-
[(carbamoylamino)carbamoyl] pyrrolidin-1-yl] -
-pentan-2-yl] carbamoyl] -3-methyl-
butyl] carbamoyl] -2-tert-butoxy-
ethyl] carbamoyl] -2-(4-hydroxyphenyl)
ethyl] carbamoyl] -2-hydroxy-ethyl]
carbamoyl] -2-(3H-imidazol-4-yl)ethyl] -
CAS_number = 65807-02-5
ATC_prefix = L02
PubChem = 47725
DrugBank = BTD00113
C=59 | H=84| N=18| O=14
molecular_weight = 1269.410 g/mol
synonyms = D-Ser(But)6Azgly10LHRH
excretion = renal
pregnancy_category = D (3.6mg) / X (10.8mg) (USA)
legal_status = Rx-only
routes_of_administration = implant
Excipients = Lactide/glycolide copolymer
Goserelin Acetate is an injectable
gonadotropin releasing hormonesuper-agonist ( GnRH agonist) also known as an LHRH agonist. It stops the production of sex hormones ( testosteroneand oestrogen).
Goserelin Acetate is marketed by
AstraZenecawith the brand name Zoladex. [ [http://www.zoladex.net/ AstraZeneca official Zoladex site] ] 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 [ [http://www.fda.gov/medwatch/safety/1999/nov99.htm#zolade FDA Approval for Zoladex 3.6 mg] ] for treatment of prostate cancer, a 10.8 mg subcutaneous 3-month biodegradable implant and other indications were subsequently approved.
Goserelin is a synthetic analogue of a naturally occurring luteinising-hormone releasing hormone (
LHRH). Bioavailability is almost complete. 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 hepatic failure. After administration, peak serum concentrations are reached in about two hours. It rapidly binds to the LHRH receptor cells in the pituitary glandthus leading to an initial increase in production of luteinizing hormoneand thus leading to an initial increase in the production of corresponding sex hormones. This initial Flare may be treated by co-prescribing/co-administering Casodex(Bicalutamide) or similar medication. 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. [cite journal | last = Kotake | first = Toshihiko | coauthors = Michiyuki Usami, Hideyuki Akaza et al. | title = Goserelin Acetate with or without Antiandrogen or Estrogen in the Treatment of Patients with Advanced Prostate Cancer: a Multicenter, Randomized, Controlled Trial in Japan | journal = Japanese Journal of Clin. Oncol. | volume = 29 | issue = 11 | pages = 562–570 | date = August 1999 | url = http://jjco.oxfordjournals.org/cgi/content/full/29/11/562 | id = ISSN|1465-3621 | accessdate = 2007-02-26 | doi = 10.1093/jjco/29.11.562 | pmid = 10678560 ]
Goserelin Acetate 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 reproductionand in the treatment of precocious puberty. The syringe applicator comes with a protective sleeve, called the SafeSystem, to reduce and prevent needlestick injuries to administering healthcare professionals.
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.
NOTE: The above license is probably from the USA. It should be noted that licensed indications may vary from country to country. For example, in the UK the 1-month depot is licensed for
prostate cancer, endometriosis, uterine fibroids, breast cancer, endometrial thinningand assisted reproduction, and not as above. You are advised to consult a Healthcare Professional or your local regulatory authorities if you need more information on your local license for this product.
Goserelin Acetate may cause a temporary increase in bone pain and symptoms of
prostatic cancerduring the first few weeks of treatment. As the body adjusts to the medication, the symptoms will disappear. Goserelin may cause bone pain, hot flushes, headache, stomach upset, difficulty urinating (isolated cases), weight gain, swelling and tenderness of breasts (infrequent), decreased erections and reduced sexual desire. Bone pain can be managed symptomatically, and decreased libido can be treated by Levitra( Vardenafil) or other similar oral therapies.
No known interaction with other medicinal products.
Effects on ability to drive and operate machinery
There is no evidence that Goserelin Acetate results in impairment of these activities.
* [http://news.bbc.co.uk/1/hi/health/6320397.stm One man's experience of prostate cancer treatment using goserelin] -
Wikimedia Foundation. 2010.
Look at other dictionaries:
goserelin — A drug that belongs to the family of drugs called gonadotropin releasing hormone analogs. Goserelin is used to block hormone production in the ovaries or testicles … English dictionary of cancer terms
goserelin — go·se·rel·in (gō sə rĕlʹĭn) n. A synthetic peptide analogue of gonadotropin releasing hormone used to treat prostate cancer, endometriosis, and advanced breast cancer. [Blend of gonadorelin(from gonadotropin releasing hormone + in), and… … Universalium
goserelin — A synthetic decapeptide agonist analog of the LHRH (GnRH). It inhibits pituitary gonadotropin secretion and is used in the treatment of prostate cancer, breast … Medical dictionary
goserelin — n. a gonadorelin analogue that is used in the treatment of endometriosis, prostate cancer, and fibroids, being administered by subcutaneous depot injection at one or three monthly intervals. It is also used in the treatment of infertility by in… … The new mediacal dictionary
goserelin acetate — the acetate salt of goserelin, used to treat breast and prostate carcinomas and endometriosis, and to thin the endometrium prior to endometrial ablation; administered by subcutaneous implant … Medical dictionary
Гозерелин (Goserelin) — см. Аналог лютеинизирующего гормона. Источник: Медицинский словарь … Медицинские термины
ГОЗЕРЕЛИН — (goserelin) см. Аналог лютеинизирующего гормона … Толковый словарь по медицине
Prostate cancer — is a disease in which cancer develops in the prostate, a gland in the male reproductive system. It occurs when cells of the prostate mutate and begin to multiply out of control. These cells may spread (metastasize) from the prostate to other… … Wikipedia
Management of prostate cancer — Treatment for prostate cancer may involve active surveillance, surgery, radiation therapy including brachytherapy (prostate brachytherapy) and external beam radiation therapy, High intensity focused ultrasound (HIFU), chemotherapy, cryosurgery,… … Wikipedia
Subcutaneous injection — A subcutaneous injection is administered as a bolus into the subcutis, [DorlandsDict|four/000053802|subcutaneous injection] the layer of skin directly below the dermis and epidermis, collectively referred to as the cutis. Subcutaneous injections… … Wikipedia