関: Decapeptyl

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/05/26 18:02:16」(JST)

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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 for gender identity disorder. 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

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.

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1. Initial systemic therapy for castration sensitive prostate cancer
2. 思春期早発症の治療 treatment of precocious puberty
3. 開腹および腹腔鏡下筋腫核出術中の失血量減少手技 techniques to reduce blood loss during abdominal or laparoscopic myomectomy
4. アンドロゲン過剰症および男性型多毛症治療におけるGnRHアゴニストの使用 use of gnrh agonists in the treatment of hyperandrogenism and hirsutism
5. 播種性前立腺癌に対する治療の概要 overview of the treatment of disseminated prostate cancer

English Journal

Gonadotropin‑releasing hormone inhibits the proliferation and motility of nasopharyngeal carcinoma cells.

Teng LH1, Ahmad M1, Ng WT1, Sabaratnam S2, Rasan MI3, Parhar I4, Khoo AS1.
Molecular medicine reports.Mol Med Rep.2015 Oct;12(4):4909-16. doi: 10.3892/mmr.2015.4043. Epub 2015 Jul 3.
Gonadotropin‑releasing hormone (GnRH), or its analogues have been demonstrated to exhibit anti‑proliferative effects on tumour cells in ovarian, endometrial and breast cancer through GnRH‑receptors (GnRH‑R). However, the role of GnRH in nasopharyngeal carcinoma (NPC) remains to be elucidated
PMID 26151677

Are we ready to change clinical practice after the 'soft and text' results?

De Iuliis F1, Lanza R2, Scarpa S1.
Future oncology (London, England).Future Oncol.2015 Sep 25. [Epub ahead of print]
PMID 26403651

Characterization of 12 GnRH peptide agonists - a kinetic perspective.

Nederpelt I1, Schuldt V2, Schiele F2, Nowak-Reppel K2, Fernández-Montalván AE2, IJzerman AP1, Heitman LH1.
British journal of pharmacology.Br J Pharmacol.2015 Sep 23. doi: 10.1111/bph.13342. [Epub ahead of print]
BACKGROUND AND PURPOSE: Drug-target residence time is an important, yet often overlooked, parameter in drug discovery. Multiple studies have proposed an increased residence time to be beneficial for improved drug efficacy and/or longer duration of action. Currently there are many drugs on the market
PMID 26398856

Japanese Journal

Comparable clinical outcome using the GnRH antagonist ganirelix or a long protocol of the GnRH agonist triptorelin for the prevention of premature LH surges in women undergoing ovarian stimulation

The European and Middle East Orgalutran Study Group
Hum. Reprod. 16, 644-651, 2001
NAID 30018427192

Use of a single bolus of GnRH agonist triptorelin to trigger ovulation after GnRH antagonist ganirelix treatment in women undergoing ovarian stimulation for assisted reproduction, with special reference to the prevention of ovarian hyperstimulation syndrome : preliminary report : short communication

ITSKOVITZ-ELDOR J.
Hum. Reprod. 15, 1965-1968, 2000
NAID 30018426834

Effects of triptorelin versus placebo on the symptoms of endometriosis

BERGQVIST A.
Fertil. Steril. 69, 702-708, 1998
NAID 30007624916

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★リンクテーブル★

リンク元	「トリプトレリン」「Decapeptyl」

「トリプトレリン」

Triptorelin
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;
Legal status	℞ (Prescription only);
Routes of; administration	Implant
Pharmacokinetic data
Excretion	Renal
Identifiers
CAS Registry Number	57773-63-4
ATC code	L02AE04
ChemSpider	13835459
UNII	9081Y98W2V
ChEBI	CHEBI:28568
ChEMBL	CHEMBL1201334
Chemical data
Formula	C64H82N18O13
Molecular mass	1311.5 g/mol
	InChI InChI=1S/C64H82N18O13/c1-34(2)23-46(56(88)75-45(13-7-21-69-64(66)67)63(95)82-22-8-14-52(82)62(94)72-31-53(65)85)76-58(90)48(25-36-28-70-42-11-5-3-9-40(36)42)78-57(89)47(24-35-15-17-39(84)18-16-35)77-61(93)51(32-83)81-59(91)49(26-37-29-71-43-12-6-4-10-41(37)43)79-60(92)50(27-38-30-68-33-73-38)80-55(87)44-19-20-54(86)74-44/h3-6,9-12,15-18,28-30,33-34,44-52,70-71,83-84H,7-8,13-14,19-27,31-32H2,1-2H3,(H2,65,85)(H,68,73)(H,72,94)(H,74,86)(H,75,88)(H,76,90)(H,77,93)(H,78,89)(H,79,92)(H,80,87)(H,81,91)(H4,66,67,69)/t44-,45-,46-,47-,48+,49-,50-,51-,52-/m0/s1 ; Key:VXKHXGOKWPXYNA-PGBVPBMZSA-N ;
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