Abarelix - CAS 183552-38-7
Not Intended for Therapeutic Use. For research use only.
Category:
Inhibitor
Product Name:
Abarelix
Catalog Number:
183552-38-7
Synonyms:
Plenaxis, PPI-149, R-3827
CAS Number:
183552-38-7
Description:
Abarelix is a synthetic decapeptide and antagonist of naturally occurring gonadotropin-releasing hormone (GnRH). Abarelix directly and competitively binds to and blocks the gonadotropin releasing hormone receptor in the anterior pituitary gland, thereby inhibiting the secretion and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone. As a result, this may relieve symptoms associated with prostate hypertrophy or prostate cancer, since testosterone is required to sustain prostate growth. Check for active clinical trials or closed clinical trials using this agent.
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Chemical Structure
CAS 183552-38-7 Abarelix

Reference Reading


1.Degarelix, a novel GnRH antagonist, causes minimal histamine release compared with cetrorelix, abarelix and ganirelix in an ex vivo model of human skin samples.
Koechling W1, Hjortkjaer R, Tankó LB. Br J Clin Pharmacol. 2010 Oct;70(4):580-7. doi: 10.1111/j.1365-2125.2010.03730.x.
AIMS: Early studies on gonadotrophin-releasing hormone (GnRH) antagonists pointed out histamine-mediated anaphylactic reactions as a potential adverse effect of these drug candidates. In this study we have compared the histamine-releasing potential of four approved and marketed antagonists, degarelix, cetrorelix, abarelix and ganirelix in an ex vivo model of human skin samples.
2.New treatment paradigm for prostate cancer: abarelix initiation therapy for immediate testosterone suppression followed by a luteinizing hormone-releasing hormone agonist.
Garnick MB1, Mottet N. BJU Int. 2012 Aug;110(4):499-504. doi: 10.1111/j.1464-410X.2011.10708.x. Epub 2011 Nov 16.
Study Type - Therapy (prospective cohort). Level of Evidence 2a. What's known on the subject? and What does the study add? The sequential administration of a GnRH antagonist followed by an LHRH agonist in the management of prostate cancer patients has not been studied, but such a program would provide a more physiologic method of achieving testosterone suppression and avoid the obligatory testosterone surge and need for concomitant antiandrogens that accompany LHRH agonist therapy. The current study which uses abarelix initiation therapy for 12 weeks followed by either leuprolide or goserelin demonstrates the ability to more rapidly achieve testosterone suppression, avoid the obligatory LHRH induced testosterone surge, avoid the necessity of antiandrogens, all of which were accomplished safely, without inducing either additional or novel safety issues.