abarelix

Abarelix
Systematic (IUPAC) name
	acetyl-D-β-naphthylalanyl- D-4-chlorophenylalanyl-D-3-pyridylalanyl-L-seryl-L- N-methyl- tyrosyl-D-asparagyl-L-leucyl-L-N(e )-isopropyl-lysyl-L-prolyl-D-alanyl-amide
Clinical data
Trade names	Plenaxis
AHFS/Drugs.com	monograph
Pregnancy cat.	X (US)
Legal status	?
Routes	Intramuscular injection
Pharmacokinetic data
Protein binding	96–99%
Identifiers
CAS number	183552-38-7
ATC code	L02BX01
PubChem	CID 16131215
IUPHAR ligand	1188
DrugBank	DB00106
ChemSpider	10482301
UNII	W486SJ5824
KEGG	D02738
ChEBI	CHEBI:337298
ChEMBL	CHEMBL1252
Chemical data
Formula	C72H95ClN14O14
Mol. mass	1416.06 g/mol
	SMILES O=C(N[C@H](C)C(N)=O)[C@@H]6CCCN6C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)N(C)C(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@@H](\nCc4ccc5ccccc5c4)NC(=O)C;
	InChI InChI=1S/C72H95ClN14O14/c1-41(2)32-54(64(93)80-53(17-10-11-30-77-42(3)4)72(101)87-31-13-18-60(87)69(98)78-43(5)63(75)92)81-68(97)58(38-62(74)91)84-70(99)61(37-46-22-27-52(90)28-23-46)86(7)71(100)59(40-88)85-67(96)57(36-48-14-12-29-76-39-48)83-66(95)56(34-45-20-25-51(73)26-21-45)82-65(94)55(79-44(6)89)35-47-19-24-49-15-8-9-16-50(49)33-47/h8-9,12,14-16,19-29,33,39,41-43,53-61,77,88,90H,10-11,13,17-18,30-32,34-38,40H2,1-7H3,(H2,74,91)(H2,75,92)(H,78,98)(H,79,89)(H,80,93)(H,81,97)(H,82,94)(H,83,95)(H,84,99)(H,85,96)/t43-,53+,54+,55-,56-,57-,58-,59+,60+,61+/m1/s1 ; Key:AIWRTTMUVOZGPW-HSPKUQOVSA-N ;
(what is this?) (verify);

アバレリックス

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2012/11/27 18:24:57」(JST)

wiki en

[Wiki en表示]

Abarelix (trade name Plenaxis) is an injectable gonadotropin-releasing hormone antagonist (GnRH antagonist). It is primarily used in oncology to reduce the amount of testosterone made in patients with advanced symptomatic prostate cancer for which no other treatment options are available.^[1]^[2]

It was originally marketed by Praecis Pharmaceuticals as Plenaxis,^[1] and is now marketed by Speciality European Pharma in Germany^[3] after receiving a marketing authorisation in 2005.

References

^ ^a ^b Drugs.com: Abarelix
^ Boccon-Gibod, L.; Van Der Meulen, E.; Persson, B. -E. (2011). "An update on the use of gonadotropin-releasing hormone antagonists in prostate cancer". Therapeutic Advances in Urology 3 (3): 127–140. doi:10.1177/1756287211414457. PMC 3159401. PMID 21904569. //www.ncbi.nlm.nih.gov/pmc/articles/PMC3159401/. edit
^ Pharmazeutische Zeitung online: Abarelix (German)

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

1. 患者情報：体外受精（IVF）（詳細） in vitro fertilization ivf beyond the basics

English Journal

Utility of LHRH antagonists for advanced prostate cancer.

Moul JW1.
The Canadian journal of urology.Can J Urol.2014 Apr;21(2 Supp 1):22-7.
INTRODUCTION: Androgen deprivation therapy (ADT) is the lynchpin of treatment for advanced prostate cancer. Prescribing physicians and patients have a choice between orchiectomy, luteinizing hormone releasing hormone (LHRH) agonists, combined androgen deprivation (CAD) or LHRH antagonists.MATERIALS
PMID 24775720

Effects of GnRH antagonists vs agonists in domestic carnivores, a review.

Gobello C1.
Reproduction in domestic animals = Zuchthygiene.Reprod Domest Anim.2012 Dec;47 Suppl 6:373-6. doi: 10.1111/rda.12025.
Gonadotrophin-releasing hormone (GnRH) stimulates the pituitary secretion of both luteinizing and follicle-stimulating hormones, and thus controls the hormonal and reproductive functions of the gonads. GnRH analogs, which include agonists and antagonists, have been produced by amino acid substitutio
PMID 23279542

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 international.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 provi
PMID 22093775