Goserelin

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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	L02 AE03
PubChem	47725
DrugBank	BTD00113
Chemical data
Formula	C₅₉H₈₄N₁₈O₁₄
Mol. weight	1269.410 g/mol
Synonyms	D-Ser(But)⁶Azgly¹⁰LHRH
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	2-4 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. It was first launched in 1987 and is currently the second-largest selling LHRHa in the world. It is currently available in more than one hundred markets.

Zoladex 3.6 mg subcutaneous monthly biodegradeble implant was first approved by the FDA on December 29, 1989 for treatment of prostate cancer, a 10.8 mg subcutaneous 3-month biodegradeble implant and other indications were subsequently approved.

[edit] 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.

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.

[edit] Side effects

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

Sex hormones and related medications (primarily G03, also L02, H01C) edit

Progestogens: (receptor)	Desogestrel, Drospirenone, Dydrogesterone, Ethisterone, Etonogestrel, Ethynodiol diacetate, Gestodene, Gestonorone, Levonorgestrel, Lynestrenol, Medroxyprogesterone, Megestrol, Norelgestromin, Norethisterone, Norethynodrel, Norgestimate, Norgestrel, Norgestrienone, Tibolone Antiprogestogen: Mifepristone
Androgens: (receptor)	Androstanolone, Fluoxymesterone, Mesterolone, Methyltestosterone, Testosterone, (see also anabolic steroids) Antiandrogens: Bicalutamide, Cyproterone, Flutamide, Nilutamide, Spironolactone
Estrogens: (receptor)	Chlorotrianisene, Dienestrol, Diethylstilbestrol, Estradiol, Estriol, Estrone, Ethinylestradiol, Fosfestrol, Mestranol, Polyestradiol phosphate Selective estrogen receptor modulator: Bazedoxifene, Clomifene, Fulvestrant, Raloxifene, Tamoxifen, Toremifene Aromatase inhibitor: Aminogluthetimide, Anastrozole, Exemestane, Formestane, Letrozole, Vorozole
Gonadotropins: (FSHR/LHCGR)	ovulation stim.: Clomifene, Urofollitropin Antigonadotropins: Danazol, Gestrinone
GnRH: (receptor)	Gonadotropin-releasing hormone agonist: Buserelin, Goserelin, Leuprorelin, Nafarelin, Triptorelin Gonadotropin-releasing hormone antagonist: Histrelin, Abarelix