Histrelin

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Histrelin chemical structure
Histrelin
Systematic (IUPAC) name
 ?
Identifiers
CAS number 76712-82-8
ATC code H01CA03
PubChem  ?
Chemical data
Formula C66H86N18O12 
Mol. weight 1323.5 g/mol
Pharmacokinetic data
Bioavailability 92%
Protein binding 70%
Metabolism Hepatic
Half life 4 hours
Excretion Undetermined
Therapeutic considerations
Pregnancy cat.

X(US)

Legal status

-only(US)

Routes Subcutaneous implant

Histrelin acetate is an injectable gonadotropin releasing hormone antagonist (GnRH antagonist). It stops the production of sex hormones (testosterone and oestrogen).

Histrelin is marketed by Valera Pharmaceuticals with the brand name Supprelin.

[edit] Indications

Histrelin is used to treat hormone-sensitive cancers of the prostate in men and uterine fibroids in women. In addition, histrelin is used to treat systemic precocious puberty.

It is available as a daily intramuscular injection. A 12-month depot injection (Supprelin-LA) is currently undergoing the approval process with the U.S. Food and Drug Administration.


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