Triptorelin

From Wikipedia, the free encyclopedia
Jump to: navigation, search
Triptorelin
Triptorelin.png
Systematic (IUPAC) name
5-oxo-D-prolyl-L-histidyl-Ltryptophyl-L-seryl-Ltyrosyl-3-(1H-indol-2-yl)-L-alanylleucyl-L-arginyl-L-prolylglycinamide
Clinical data
Trade names Trelstar
AHFS/Drugs.com Micromedex Detailed Consumer Information
MedlinePlus a697045
Pregnancy
category
  • D
Routes of
administration
Implant
Legal status
Legal status
  • ℞ (Prescription only)
Pharmacokinetic data
Excretion Renal
Identifiers
CAS Number 57773-63-4 N
ATC code L02AE04 (WHO) QH01CA97 (WHO)
PubChem CID 25074470
IUPHAR/BPS 1177
DrugBank DB06825
ChemSpider 17290424 YesY
UNII 9081Y98W2V YesY
KEGG D06247 YesY
ChEBI CHEBI:63633 YesY
ChEMBL CHEMBL1201334 N
Chemical data
Formula C64H82N18O13
Molar mass 1311.5 g/mol
 NYesY (what is this?)  (verify)

Triptorelin, a decapeptide (pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2), is a gonadotropin-releasing hormone agonist (GnRH agonist) used as the acetate or pamoate salts. By causing constant stimulation of the pituitary, it decreases pituitary secretion of gonadotropins luteinizing hormone (LH) and follicle stimulating hormone (FSH). Like other GnRH agonists, triptorelin may be used in the treatment of hormone-responsive cancers such as prostate cancer or breast cancer, precocious puberty, estrogen-dependent conditions (such as endometriosis or uterine fibroids), and in assisted reproduction. It is also used as therapy in cases of gender dysphoria. Triptorelin is marketed under the brand names Decapeptyl (Ipsen) and Diphereline and Gonapeptyl (Ferring Pharmaceuticals). In the United States, it is sold by Watson Pharmaceuticals as Trelstar. In Iran Triptorelin is marketed under the brand name Variopeptyl (Varian Darou Pajooh).

During the treatment of prostate cancer it does cause a surge of testosterone (an initial uplevel of testosterone levels), known as a flare effect. In men a reduction of serum testosterone levels into the range normally seen after surgical castration occurs approximately two to four weeks after initiation of therapy. In contrast, gonadotropin-releasing hormone antagonists do not cause a surge, but a sudden reduction of testosterone levels.
Systematic IUPAC Name: [d-Trp6]GnRH

References[edit]

  • Lahlou N, Carel JC, Chaussain JL, Roger M (July 2000). "Pharmacokinetics and pharmacodynamics of GnRH agonists: clinical implications in pediatrics". J Pediatr Endocrinol Metab. 13 Suppl 1: 723–37. PMID 10969915. 
  • Padula AM (August 2005). "GnRH analogues—agonists and antagonists". Anim Reprod Sci 88 (1–2): 115–26. doi:10.1016/j.anireprosci.2005.05.005. PMID 15955640.