関: goserelin

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a salt or ester of acetic acid (同)ethanoate

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酢酸(さくさん)塩;アセテート(酢酸人造絹糸)

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2017/09/03 05:43:35」(JST)

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Goserelin (INN, USAN, BAN) (brand name Zoladex, by AstraZeneca^[1]), or goserelin acetate,^[2]^[3] is a drug used to suppress production of the sex hormones (testosterone and estrogen), particularly in the treatment of breast and prostate cancer. It is an injectable gonadotropin releasing hormone superagonist (GnRH agonist), also known as a luteinizing hormone releasing hormone (LHRH) agonist.

Structurally, it is a decapeptide. It is the natural LHRH/GnRH decapeptide with two substitutions to inhibit rapid degradation.

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^[4] for treatment of prostate cancer.

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.^[5]

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 transgender people^[6] 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.

Dosage

Goserelin is administered by subcutaneous injection as an implant of 3.6mg or 10.8mg every 28 days for the duration of treatment.^[7]

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 goserelin 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.

Memory loss may be severe and may not return to normal levels.^[8]^[9]

References

^ AstraZeneca official Zoladex site
^ Dictionary of Organic Compounds. CRC Press. pp. 3372–. ISBN 978-0-412-54090-5.
^ I.K. Morton; Judith M. Hall (6 December 2012). Concise Dictionary of Pharmacological Agents: Properties and Synonyms. Springer Science & Business Media. pp. 136–. ISBN 978-94-011-4439-1.
^ FDA Approval for Zoladex 3.6 mg
^ 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. ISSN 1465-3621. PMID 10678560. doi:10.1093/jjco/29.11.562. Retrieved 2007-02-26.
^ 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.
^ "Goserelin". NICE (National Institute for Health and Care Excellence). 2016. Retrieved 19 November 2016.
^ Newton CR, Yuzpe AA, Timmon IS, Slota MD. Memory complaints: a side effect of continued exposure to gonadotropin-releasing hormone agonists (GnRHa). Paper presented at: Conjoint Annual Meetings of the American Fertility Society and the Canadian Fertility and Andrology Society; October 11–14, 1993; Montreal, Canada.
^ Friedman AJ, Juneau-Norcross M, Rein MS. Adverse effects of leuprolide acetate depot treatment. Fertil Steril. 1993;59(2):448-450.)

External links

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

UpToDate Contents

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1. 転移性ホルモン受容体陽性乳癌に対する治療アプローチ：内分泌療法 treatment approach to metastatic hormone receptor positive breast cancer endocrine therapy
2. 去勢感受性前立腺癌の初期全身療法 initial systemic therapy for castration sensitive prostate cancer
3. Endometriosis: Treatment of pelvic pain
4. 非転移性ホルモン受容体陽性乳癌に対する補助内分泌療法 adjuvant endocrine therapy for non metastatic hormone receptor positive breast cancer
5. アンドロゲン除去療法による副作用 side effects of androgen deprivation therapy

English Journal

Endometrial expression of LIF and its receptor and peritoneal fluid levels of IL-1α and IL-6 in women with endometriosis are associated with the probability of pregnancy.

Moberg C1, Bourlev V, Ilyasova N, Olovsson M.
Archives of gynecology and obstetrics.Arch Gynecol Obstet.2015 Aug;292(2):429-37. doi: 10.1007/s00404-015-3626-0. Epub 2015 Jan 29.
PURPOSE: To investigate whether eutopic endometrial expression of leukaemia inhibitory factor (LIF), LIF receptor (LIFR) and glycoprotein 130 (gp130) in subfertile women with endometriosis and in healthy controls is related to the probability of spontaneous pregnancy. In addition, we aimed to study
PMID 25631342

Long-term oncological outcomes of a phase II trial of neoadjuvant chemohormonal therapy followed by radical prostatectomy for patients with clinically localised, high-risk prostate cancer.

Silberstein JL1, Poon SA2, Sjoberg DD3, Maschino AC3, Vickers AJ3, Bernie A4, Konety BR5, Kevin Kelly W6, Eastham JA4.
BJU international.BJU Int.2015 Jul;116(1):50-6. doi: 10.1111/bju.12676. Epub 2015 Apr 17.
OBJECTIVE: To determine long-term oncological outcomes of radical prostatectomy (RP) after neoadjuvant chemohormonal therapy (CHT) for clinically localised, high-risk prostate cancer.PATIENTS AND METHODS: In this phase II multicentre trial of patients with high-risk prostate cancer (PSA level >20
PMID 24552276

Subjective and Objective Effects of Androgen Ablation Therapy on Voice.

Salturk Z1, Çakır O2, Kumral TL2, Yıldırım G2, Ötünçtemur A3, Aydoğdu Ï2, Uyar Y2.
Journal of voice : official journal of the Voice Foundation.J Voice.2015 Jul;29(4):490-3. doi: 10.1016/j.jvoice.2014.09.010. Epub 2015 Feb 19.
OBJECTIVES: The aim of present study was to evaluate possible side effects of androgen deprivation therapy (ADT) on voice quality by means of objective and subjective measures.STUDY DESIGN: Cross-sectional.METHODS: Thirty-five male patients who had been diagnosed with prostate cancer and who had bee
PMID 25704476

Japanese Journal

酢酸リュープロレリン皮下注射による皮下硬結形成の検討

泌尿器科紀要 = Acta urologica Japonica 61(2), 55-59, 2015-02
NAID 120005575175

内分泌療法中に虚血性心疾患を発症した去勢抵抗性前立腺がんの1症例

医療薬学 41(10), 695-700, 2015
NAID 130005249592

ゴセレリン酢酸塩デポ製剤皮下注射による巨大皮下血腫で出血性ショックが生じた前立腺癌の1例

泌尿器科紀要 = Acta urologica Japonica 60(9), 455-458, 2014-09
NAID 40020204108

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リンク元

「ゴセレリン」

Goserelin
Clinical data
Trade names	Zoladex
Synonyms	D-Ser(But)6Azgly10LHRH
AHFS/Drugs.com	Monograph
MedlinePlus	a601002
Pregnancy; category	D (3.6mg) / X (10.8mg) (USA);
Routes of; administration	implant
ATC code	L02AE03 (WHO);
Legal status
Legal status	In general: ℞ (Prescription only);
Pharmacokinetic data
Protein binding	27.3%
Biological half-life	4-5 hours
Excretion	hepatic
Identifiers
	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;
CAS Number	65807-02-5 ;
PubChem CID	5311128;
IUPHAR/BPS	3879;
DrugBank	DB00014 ;
ChemSpider	4470656 ;
UNII	0F65R8P09N;
KEGG	D04405 ;
ChEBI	CHEBI:5523 ;
ChEMBL	CHEMBL1201247 ;
ECHA InfoCard	100.212.024
Chemical and physical data
Formula	C59H84N18O14
Molar mass	1269.410 g/mol
3D model (JSmol)	Interactive image;
	SMILES CC(C)C[C@H](NC(=O)[C@@H](COC(C)(C)C)NC(=O)[C@H](CC1=CC=C(O)C=C1)NC(=O)[C@H](CO)NC(=O)[C@H](CC1=CNC2=CC=CC=C12)NC(=O)[C@H](CC1=CN=CN1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NNC(N)=O ;
	InChI InChI=1S/C59H84N18O14/c1-31(2)22-40(49(82)68-39(12-8-20-64-57(60)61)56(89)77-21-9-13-46(77)55(88)75-76-58(62)90)69-54(87)45(29-91-59(3,4)5)74-50(83)41(23-32-14-16-35(79)17-15-32)70-53(86)44(28-78)73-51(84)42(24-33-26-65-37-11-7-6-10-36(33)37)71-52(85)43(25-34-27-63-30-66-34)72-48(81)38-18-19-47(80)67-38/h6-7,10-11,14-17,26-27,30-31,38-46,65,78-79H,8-9,12-13,18-25,28-29H2,1-5H3,(H,63,66)(H,67,80)(H,68,82)(H,69,87)(H,70,86)(H,71,85)(H,72,81)(H,73,84)(H,74,83)(H,75,88)(H4,60,61,64)(H3,62,76,90)/t38-,39-,40-,41-,42-,43-,44-,45+,46-/m0/s1 ; Key:BLCLNMBMMGCOAS-URPVMXJPSA-N ;
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　　[★]

英: goserelin
化: 酢酸ゴセレリン goserelin acetate
商: ゾラデックス

LH-RH作動薬;前立腺癌および閉経前乳癌治療;子宮内膜症治療

[1] AstraZeneca official Zoladex site

[2] Dictionary of Organic Compounds. CRC Press. pp. 3372–. ISBN 978-0-412-54090-5.

[MortonHall2012-3] I.K. Morton; Judith M. Hall (6 December 2012). Concise Dictionary of Pharmacological Agents: Properties and Synonyms. Springer Science & Business Media. pp. 136–. ISBN 978-94-011-4439-1.

[4] FDA Approval for Zoladex 3.6 mg

[5] 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. ISSN 1465-3621. PMID 10678560. doi:10.1093/jjco/29.11.562. Retrieved 2007-02-26.

[6] 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.

[7] "Goserelin". NICE (National Institute for Health and Care Excellence). 2016. Retrieved 19 November 2016.

[8] Newton CR, Yuzpe AA, Timmon IS, Slota MD. Memory complaints: a side effect of continued exposure to gonadotropin-releasing hormone agonists (GnRHa). Paper presented at: Conjoint Annual Meetings of the American Fertility Society and the Canadian Fertility and Andrology Society; October 11–14, 1993; Montreal, Canada.

[9] Friedman AJ, Juneau-Norcross M, Rein MS. Adverse effects of leuprolide acetate depot treatment. Fertil Steril. 1993;59(2):448-450.)

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goserelin acetate