Buserelin

Buserelin

Buserelin
Clinical data
Trade names Etilamide
AHFS/Drugs.com
Pregnancy cat.
  • X
Legal status
  • ℞-only
Routes implant, intranasal
Pharmacokinetic data
Half-life 72 to 80 minutes
Excretion Renal
Identifiers
CAS number  YesY
ATC code L02 QH01
PubChem
DrugBank
ChemSpider  YesY
UNII  YesY
ChEMBL  N
Synonyms D-Ser(Tbu)6EA10LHRH
Chemical data
Formula C62H90N16O15 
Mol. mass 1299.48 g/mol
 N   

Buserelin is a Gonadotropin-releasing hormone agonist (GnRH agonist). The drug's effects are dependent on the frequency and time course of administration. GnRH is released in a pulsatile fashion in the postpubertal adult. Initial interaction of any GnRH agonist, such as buserelin, with the GnRH receptor induces release of FSH and LH by gonadotrophes. Long-term exposure to constant levels of buserelin, rather than endogenous pulses, leads to downregulation of the GnRH receptors and subsequent suppression of the pituitary release of LH and FSH.

Like other GnRH agonists, buserelin may be used in the treatment of hormone-responsive cancers such as prostate cancer or breast cancer, estrogen-dependent conditions (such as endometriosis or uterine fibroids), and in assisted reproduction.

It is normally delivered via a nasal spray, but is also available as an injection.

Buserelin acetate is marketed by Sanofi-Aventis under the brand name Suprefact and a generic form of Buserelin is now produced by CinnaGen under the brand name CinnaFact.

Buserelin is also marketed under the brand name Metrelef. Metrelef is approved to treat patients with endometriosis by suppression of ovarian hormone production. In ovulation induction Metrelef is used as a pituitary blockade as an adjunct to gonadotrophin administration.