Buserelin

Buserelin

Clinical data
Trade names	Etilamide
AHFS/Drugs.com	Micromedex Detailed Consumer Information
Pregnancy category	X
Routes of administration	implant, intranasal
ATC code	L02AE01 (WHO) QH01CA90 (WHO)
Legal status
Legal status	In general: ℞ (Prescription only)
Pharmacokinetic data
Biological half-life	72 to 80 minutes
Excretion	Renal
Identifiers
Synonyms	D-Ser(Tbu)6EA10LHRH
CAS Number	57982-77-1 Y
PubChem CID	50225
IUPHAR/BPS	3860
DrugBank	DB06719 N
ChemSpider	45545 Y
UNII	PXW8U3YXDV
ChEMBL	CHEMBL1909304 N
ECHA InfoCard	100.055.493
Chemical and physical data
Formula	C60H86N16O13
Molar mass	1239.42 g/mol
3D model (Jmol)	Interactive image
SMILES CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](COC(C)(C)C)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CO)NC(=O)[C@H](Cc3c[nH]c4c3cccc4)NC(=O)[C@H](Cc5cnc[nH]5)NC(=O)[C@@H]6CCC(=O)N6
InChI InChI=1S/C60H86N16O13/c1-7-64-57(87)48-15-11-23-76(48)58(88)41(14-10-22-65-59(61)62)69-51(81)42(24-33(2)3)70-56(86)47(31-89-60(4,5)6)75-52(82)43(25-34-16-18-37(78)19-17-34)71-55(85)46(30-77)74-53(83)44(26-35-28-66-39-13-9-8-12-38(35)39)72-54(84)45(27-36-29-63-32-67-36)73-50(80)40-20-21-49(79)68-40/h8-9,12-13,16-19,28-29,32-33,40-48,66,77-78H,7,10-11,14-15,20-27,30-31H2,1-6H3,(H,63,67)(H,64,87)(H,68,79)(H,69,81)(H,70,86)(H,71,85)(H,72,84)(H,73,80)(H,74,83)(H,75,82)(H4,61,62,65)/t40-,41-,42-,43-,44-,45-,46-,47+,48-/m0/s1 Y Key:CUWODFFVMXJOKD-UVLQAERKSA-N Y
NY (what is this?)

Buserelin (INN) 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 follicle-stimulating hormone (FSH) and luteinizing hormone (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 It is used as a pituitary blockade as an adjunct to gonadotrophin administration.

Deslorelin is a similar GnRH agonist used in veterinary medicine.