関: cetrorelix acetate

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/05/27 18:19:30」(JST)

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Cetrorelix acetate is an injectable gonadotropin-releasing hormone antagonist (GnRH antagonist). A synthetic decapeptide, it is used to treat hormone-sensitive cancers of the prostate and breast (in pre-/perimenopausal women) and some benign gynaecological disorders (endometriosis, uterine fibroids and endometrial thinning). In addition, cetrorelix is used in assisted reproduction to inhibit premature luteinizing hormone surges. The drug works by blocking the action of GnRH upon the pituitary, thus rapidly suppressing the production and action of LH and FSH. It is administered as either multiple 0.25 mg daily subcutaneous injections or as a single-dose 3 mg subcutaneous injection. The duration of the 3 mg single dose is four days; if hCG is not administered within four days, a daily 0.25 mg dose is started and continued until hCG is administered.

Use in IVF [edit]

Cetrorelix is marketed by Merck Serono as Cetrotide for use in in-vitro fertilization in all countries except Japan, where it is marketed by Shionogi and Nippon Kayaku.^[1] Aeterna Zentaris receives royalties on these sales and retains rights to develop cetrorelix for other indications. In IVF use it is injected daily after follicle stimulation has been initiated and evidence of follicle maturation is approaching; given daily it prevents an endogenous LH surge that would trigger an untimely ovulation prior to the hCG administration by the treating physician. As an alternative to the GNRH antagonist, also a GNRH agonist could be given, but agonist have to be started earlier to overcome the agonistic effect. Cetrorelix can be mixed with follitropin alpha without compromising their reported safety and efficacy.^[2]

Implications [edit]

Over a period of 3 weeks, daily injections of Cetrorelix were administered to 12 men in order to suppress testosterone levels. Testosterone levels were significantly suppressed as compared to a control group. During this time of suppression, increases in High Density Lipoproteins (HDL's) were seen. HDL's are responsible for removing cholesterol from the blood and higher amounts are correlated with increased cardivascular health. (von Eckardstein, 1997)

Contraindications [edit]

The use of Cetrorelix is contraindicated in severe renal impairment. It is not intended for women aged 65 years or older. Use in women with severe allergic conditions is not recommended. Use with caution in women with active allergies or history of allergies.

References [edit]

^ Aeternia Zentaris product page
^ Lin, Y.; Wen, Y.; Chang, Y.; Seow, K.; Hsieh, B.; Hwang, J.; Tzeng, C. (2010). "Safety and efficacy of mixing cetrorelix with follitropin alfa: a randomized study". Fertility and Sterility 94 (1): 179–183. doi:10.1016/j.fertnstert.2009.02.062. PMID 19339001. edit

von Eckardstein, A. “Suppression of Endogenous Testosterone in Young Men Increases Serum Levels of High Density Lipoprotein Subclass Lipoprotein A-I and Lipoprotein(a).” Journal of Clinical Endocrinology, v. 82 issue 10, 1997, p. 3367.

UpToDate Contents

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1. 原因不明の不妊症 unexplained infertility
2. 患者情報：体外受精（IVF）（詳細） in vitro fertilization ivf beyond the basics

English Journal

Gonadotropin-releasing hormone (GnRH) agonist leuprolide acetate and GnRH antagonist cetrorelix acetate directly inhibit leiomyoma extracellular matrix production.

Britten JL, Malik M, Levy G, Mendoza M, Catherino WH.SourceDepartment of Obstetrics and Gynecology, Uniformed Services University of the Health Sciences, Bethesda, Maryland.
Fertility and sterility.Fertil Steril.2012 Nov;98(5):1299-307. doi: 10.1016/j.fertnstert.2012.07.1123. Epub 2012 Aug 14.
OBJECTIVE: To determine the direct effect that GnRH analogues leuprolide acetate and cetrorelix acetate have on extracellular matrix in human leiomyoma and patient-matched myometrial cells.DESIGN: Laboratory study.SETTING: University hospital.PATIENT(S): None.INTERVENTION(S): Cell culture, prolifera
PMID 22901846

Reply to Kaplan SA: Re: LHRH Antagonist Cetrorelix Reduces Prostate Size and Gene Expression of Proinflammatory Cytokines and Growth Factors in a Rat Model of Benign Prostatic Hyperplasia.

Rick FG, Block NL, Schally AV.SourceEndocrine, Polypeptide and Cancer Institute, Veterans Affairs Medical Center and South Florida Veterans Affairs Foundation for Research and Education, 1201 N.W. 16th Street, Miami, Miami, FL 33125, USA; Department of Pathology, University of Miami, Miller School of Medicine, 1800 N.W. 10th Ave, Miami, FL 33125, USA.
The Journal of urology.J Urol.2012 Oct 23. pii: S0022-5347(12)05343-8. doi: 10.1016/j.juro.2012.10.062. [Epub ahead of print]
PMID 23103799

Japanese Journal

Comparison of the effects of cetrorelix, a GnRH antagonist, and leuprolide, a GnRH agonist, on experimental endometriosis

ALTINTAS Devrim,KOKCU Arif,TOSUN Migraci,CETINKAYA Mehmet B.,KANDEMIR Bedri
The journal of obstetrics and gynaecology research 34(6), 1014-1019, 2008-12-01
NAID 10023917711

Stimulation of Annexin A5 Expression by Gonadotropin Releasing Hormone (GnRH) in the Leydig Cells of Rats

YAO Bing,KAWAMINAMI Mitsumori
The Journal of reproduction and development 54(4), 259-264, 2008-08-01
… We found that des-Gly10 [Pro9]-GnRH ethylamide (100 nM), a GnRH agonist, increased annexin A5 expression in cultured testis cells and that Cetrorelix (100 nM), a GnRH antagonist, inhibited the effect of hCG on annexin A5 expression. …
NAID 10024289369

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リンク元	「セトロレリックス」「セトロレリクス」
拡張検索	「cetrorelix acetate」

「セトロレリックス」

Cetrorelix
Systematic (IUPAC) name
	Acetyl-D-3-(2´-naphtyl)-alanine- D-4-chlorophenylalanine-D-3-(3´-pyridyl)- alanine-L-serine-L-tyrosine-D-citrulline-L- leucine-L-arginine-L-proline-D- alanine-amide
Clinical data
AHFS/Drugs.com	Micromedex Detailed Consumer Information
Pregnancy cat.	X (US)
Legal status	℞-only (US)
Routes	Subcutaneous injection
Pharmacokinetic data
Bioavailability	85%
Protein binding	86%
Half-life	62.8 hours / 3mg single dose; 5 hours / 0.25 mg single dose; 20.6 hours / 0.25mg multiple doses
Excretion	feces (5% to 10% as unchanged drug and metabolites); urine (2% to 4% as unchanged drug)
Identifiers
CAS number	120287-85-6
ATC code	H01CC02
PubChem	CID 16130924
DrugBank	DB00050
ChemSpider	10482082
UNII	OON1HFZ4BA
KEGG	D07665
ChEBI	CHEBI:59224
ChEMBL	CHEMBL1200490
Chemical data
Formula	C70H92ClN17O14
Mol. mass	1431.06 g/mol
	InChI InChI=1S/C70H92ClN17O14/c1-39(2)31-52(61(94)82-51(15-9-28-77-69(73)74)68(101)88-30-10-16-58(88)67(100)79-40(3)59(72)92)83-60(93)50(14-8-29-78-70(75)102)81-63(96)54(34-43-20-25-49(91)26-21-43)86-66(99)57(38-89)87-65(98)56(36-45-11-7-27-76-37-45)85-64(97)55(33-42-18-23-48(71)24-19-42)84-62(95)53(80-41(4)90)35-44-17-22-46-12-5-6-13-47(46)32-44/h5-7,11-13,17-27,32,37,39-40,50-58,89,91H,8-10,14-16,28-31,33-36,38H2,1-4H3,(H2,72,92)(H,79,100)(H,80,90)(H,81,96)(H,82,94)(H,83,93)(H,84,95)(H,85,97)(H,86,99)(H,87,98)(H4,73,74,77)(H3,75,78,102)/t40-,50-,51+,52+,53-,54+,55-,56-,57+,58+/m1/s1 ; Key:SBNPWPIBESPSIF-MHWMIDJBSA-N ;
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