World Library  
Flag as Inappropriate
Email this Article

Goserelin

Article Id: WHEBN0001269468
Reproduction Date:

Title: Goserelin  
Author: World Heritage Encyclopedia
Language: English
Subject: AstraZeneca, Gonadotropin-releasing hormone agonist, Leuprorelin, Antigonadotropin, Relugolix
Collection: Astrazeneca, Depressogenics, Gnrh Agonists, Peptides
Publisher: World Heritage Encyclopedia
Publication
Date:
 

Goserelin

Goserelin
Systematic (IUPAC) name
N-(21-((1H-indol-3-yl)methyl)-1,1-diamino-12-(tert-butoxymethyl)-6-(2-(2-carbamoylhydrazinecarbonyl)cyclopentanecarbonyl)-15-(4-hydroxybenzyl)-18-(hydroxymethyl)-25-(1H-imidazol-5-yl)-9-isobutyl-8,11,14,17,20,23-hexaoxo-2,7,10,13,16,19,22-heptaazapentacos-1-en-24-yl)-5-oxopyrrolidine-2-carboxamide
Clinical data
Trade names Zoladex
AHFS/Drugs.com
MedlinePlus
Pregnancy
category
  • D (3.6mg) / X (10.8mg) (USA)
Legal status
  • (Prescription only)
Routes of
administration
implant
Pharmacokinetic data
Protein binding 27.3%
Biological half-life 4-5 hours
Excretion hepatic
Identifiers
CAS Registry Number  Y
ATC code L02
PubChem CID:
IUPHAR/BPS
DrugBank  Y
ChemSpider  Y
UNII  Y
KEGG  Y
ChEBI
ChEMBL  N
Synonyms D-Ser(But)6Azgly10LHRH
Chemical data
Formula C59H84N18O14
Molecular mass 1269.410 g/mol
 N   

Goserelin acetate (Zoladex, AstraZeneca[1]) is an injectable gonadotropin releasing hormone superagonist (GnRH agonist), also known as a luteinizing hormone releasing hormone (LHRH) agonist. Structurally, it is a decapeptide. Goserelin acetate is used to suppress production of the sex hormones (testosterone and estrogen), particularly in the treatment of breast and prostate cancer.

Goserelin acetate stimulates the production of the sex hormones testosterone and estrogen in a non-pulsatile (non-physiological) manner. This causes the disruption of the endogenous hormonal feedback systems, resulting in the down-regulation of testosterone and estrogen production.

Zoladex was approved by the U.S. Food and Drug Administration in 1989[2] for treatment of prostate cancer.

Contents

  • Pharmacokinetics 1
  • Indications 2
  • Side effects 3
  • References 4
  • External links 5

Pharmacokinetics

Goserelin is a synthetic analogue of a naturally occurring luteinizing-hormone releasing hormone (LHRH). Bioavailability is almost complete. Goserelin is poorly protein bound and has a serum elimination half-life of two to four hours in patients with normal renal function. The half-life increases with patients with impaired renal function. There is no significant change in pharmacokinetics in subjects with liver failure. After administration, peak serum concentrations are reached in about two hours. It rapidly binds to the LHRH receptor cells in the pituitary gland thus leading to an initial increase in production of luteinizing hormone and thus leading to an initial increase in the production of corresponding sex hormones. This initial flare may be treated by co-prescribing/co-administering an androgen receptor antagonist such as Bicalutamide (Casodex). Eventually, after a period of about 14–21 days, production of LH is greatly reduced due to receptor downregulation, and sex hormones are generally reduced to castrate levels.[3]

Indications

10.8mg implant syringe

Goserelin Acetate is used to treat hormone-sensitive cancers of the breast (in pre- and peri- menopausal women) and prostate, and some benign gynaecological disorders (endometriosis, uterine fibroids and endometrial thinning). In addition, goserelin is used in assisted reproduction and in the treatment of precocious puberty. It may also be used in the treatment of male-to-female transsexuals[4] and is favoured above other anti-androgens in some countries, such as the UK. It is available as a 1-month depot and a long-acting 3-month depot.

Side effects

Goserelin Acetate may cause a temporary increase in bone pain and symptoms of prostatic cancer during the first few weeks of treatment. This is known as the tumour flare effect, and is the result of an initial increase in luteinizing hormone production, before the receptors are desensitised and hormonal production is inhibited. The symptoms will disappear, with hormonal inhibition. It is therefore advisable to co-treat with an antiandrogen during the first 2–3 weeks of Gosrelin treatment, particularly in patients with pre-existing bone symptoms. Goserelin may cause bone pain, hot flushes, headache, stomach upset, depression, difficulty urinating (isolated cases), weight gain, swelling and tenderness of breasts (infrequent), decreased erections and reduced sexual desire. Bone pain can be managed symptomatically, and erectile dysfunction can be treated by Levitra (Vardenafil) or other similar oral therapies, although they will not treat the reduced sexual desire.

References

  1. ^ AstraZeneca official Zoladex site
  2. ^ FDA Approval for Zoladex 3.6 mg
  3. ^ Kotake, Toshihiko; Michiyuki Usami; et al. (August 1999). "Goserelin Acetate with or without Antiandrogen or Estrogen in the Treatment of Patients with Advanced Prostate Cancer: a Multicenter, Randomized, Controlled Trial in Japan". Japanese Journal of Clin. Oncol. 29 (11): 562–570.  
  4. ^ Dittrich R, Binder H, Cupisti S, Hoffmann I, Beckmann MW, Mueller A. Endocrine treatment of male-to-female transsexuals using gonadotropin-releasing hormone agonist. Exp Clin Endocrinol Diabetes 2005;113:586–92.

External links

  • One man's experience of prostate cancer treatment using goserelin - BBC News


This article was sourced from Creative Commons Attribution-ShareAlike License; additional terms may apply. World Heritage Encyclopedia content is assembled from numerous content providers, Open Access Publishing, and in compliance with The Fair Access to Science and Technology Research Act (FASTR), Wikimedia Foundation, Inc., Public Library of Science, The Encyclopedia of Life, Open Book Publishers (OBP), PubMed, U.S. National Library of Medicine, National Center for Biotechnology Information, U.S. National Library of Medicine, National Institutes of Health (NIH), U.S. Department of Health & Human Services, and USA.gov, which sources content from all federal, state, local, tribal, and territorial government publication portals (.gov, .mil, .edu). Funding for USA.gov and content contributors is made possible from the U.S. Congress, E-Government Act of 2002.
 
Crowd sourced content that is contributed to World Heritage Encyclopedia is peer reviewed and edited by our editorial staff to ensure quality scholarly research articles.
 
By using this site, you agree to the Terms of Use and Privacy Policy. World Heritage Encyclopedia™ is a registered trademark of the World Public Library Association, a non-profit organization.
 


Copyright © World Library Foundation. All rights reserved. eBooks from Project Gutenberg are sponsored by the World Library Foundation,
a 501c(4) Member's Support Non-Profit Organization, and is NOT affiliated with any governmental agency or department.