GnRHアナログ
WordNet
- something having the property of being analogous to something else (同)analog, parallel
- of a circuit or device having an output that is proportional to the input; "analogue device"; "linear amplifier" (同)analog, linear
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/03/25 20:28:42」(JST)
[Wiki en表示]
A gonadotropin-releasing hormone analogue (GnRH analogue or analog), also known as a luteinizing hormone releasing hormone agonist (LHRH agonist) or LHRH analogue is a synthetic peptide drug modeled after the human hypothalamic gonadotropin-releasing hormone (GnRH). A GnRH analogue is designed to interact with the GnRH receptor and modify the release of pituitary gonadotropins FSH and LH for therapeutic purposes. Shortly after the discovery of GnRH by Nobel laureates Guillemin and Schally researchers tried to modify the GnRH decapeptide with the intent to synthesize stimulating and blocking variants.
Two types of analogues have to be distinguished:
Agonists[edit]
Main article: Gonadotropin-releasing hormone agonist
A gonadotropin-releasing hormone agonist (GnRH agonist) is an analogue that activates the GnRH receptor resulting in increased secretion of FSH and LH. Initially it was thought that agonists could be used as potent and prolonged stimulators of pituitary gonadotropin release, but it was soon recognized that agonists, after their initial stimulating action – termed a “flare” effect - eventually caused a paradoxical and sustained drop in gonadotropin secretion. This second effect was termed “downregulation” and can be observed after about 10 days. While this phase is reversible upon stopping the medication, it can be maintained when GnRH agonists use is continued for a long time.
Antagonists[edit]
Main article: Gonadotropin-releasing hormone antagonist
A gonadotropin-releasing hormone antagonist (GnRH antagonist) is an analogue that blocks the GnRH receptor resulting in an immediate drop in gonadotropin (FSH, LH) secretion. The GnRH antagonist is primarily used in IVF treatments to block natural ovulation.
All GnRH analogues are contraindicated in pregnancy (pregnancy category X).
References[edit]
- Speroff L, Glass RH, Kase NG. Clinical Gynecologic Endocrinology and Infertility. Fifth Edition. Willimas 7 Wilkins, Baltimore. 1994. Pages 160-161.
- History of GnRH agonist and antagonist development
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Gonadotropins and GnRH (G03G)
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Gonadotropin
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Agonists
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- Menotropin
- Urofollitropin
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Antigonadotropins
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- Sex steroids (via negative feedback): Androgens (e.g., testosterone, oxandrolone, etc)
- Estrogens (e.g., estradiol, ethinyl estradiol, etc)
- Progestogens (e.g., progesterone, medroxyprogesterone acetate, etc)
- Steroid synthesis inhibitors: Danazol
- Gestrinone
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| GnRH analogues |
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Agonists
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- Avorelin
- Buserelin
- Deslorelin
- Gonadorelin
- Goserelin
- Histrelin
- Leuprorelin
- Lutrelin
- Nafarelin
- Peforelin
- Triptorelin
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Antagonists
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- Abarelix
- Cetrorelix
- Degarelix
- Detirelix
- Ganirelix
- Iturelix
- Ozarelix
- Prazarelix
- Ramorelix
- Teverelix
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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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.
English Journal
- Patient-reported outcomes with adjuvant exemestane versus tamoxifen in premenopausal women with early breast cancer undergoing ovarian suppression (TEXT and SOFT): a combined analysis of two phase 3 randomised trials.
- Bernhard J1, Luo W2, Ribi K3, Colleoni M4, Burstein HJ5, Tondini C6, Pinotti G7, Spazzapan S8, Ruhstaller T9, Puglisi F10, Pavesi L11, Parmar V12, Regan MM13, Pagani O14, Fleming GF15, Francis PA16, Price KN17, Coates AS18, Gelber RD19, Goldhirsch A20, Walley BA21.
- The Lancet. Oncology.Lancet Oncol.2015 Jun 16. pii: S1470-2045(15)00049-2. doi: 10.1016/S1470-2045(15)00049-2. [Epub ahead of print]
- BACKGROUND: The combined efficacy analysis of the TEXT and SOFT trials showed a significant disease-free survival benefit with exemestane plus ovarian function suppression (OFS) compared with tamoxifen plus OFS. We present patient-reported outcomes from these trials.METHODS: Between Nov 7, 2003, and
- PMID 26092816
- A randomised, double-blind study comparing the addition of bicalutamide with or without dutasteride to GnRH analogue therapy in men with non-metastatic castrate-resistant prostate cancer.
- Chu FM1, Sartor O2, Gomella L3, Rudo T4, Somerville MC5, Hereghty B5, Manyak MJ5.
- European journal of cancer (Oxford, England : 1990).Eur J Cancer.2015 Jun 2. pii: S0959-8049(15)00390-1. doi: 10.1016/j.ejca.2015.04.028. [Epub ahead of print]
- BACKGROUND: Bicalutamide blocks androgen action and is frequently used in men with non-metastatic, castration-resistant prostate cancer (CRPC). By reducing intracellular dihydrotestosterone, dutasteride (dual 5-alpha reductase inhibitor) could increase the effectiveness of bicalutamide in this setti
- PMID 26048455
- Gonadotrophin-releasing hormone analogue or dienogest plus estradiol valerate to prevent pain recurrence after laparoscopic surgery for endometriosis: a multi-center randomized trial.
- Granese R1, Perino A2, Calagna G2, Saitta S3, De Franciscis P4, Colacurci N4, Triolo O1, Cucinella G2.
- Acta obstetricia et gynecologica Scandinavica.Acta Obstet Gynecol Scand.2015 Jun;94(6):637-45. doi: 10.1111/aogs.12633. Epub 2015 Mar 29.
- OBJECTIVES: To evaluate the efficacy of dienogest + estradiol valerate (E2V) and gonadotrophin-releasing hormone analogue (GnRH-a) in reducing recurrence of pain in patients with chronic pelvic pain due to laparoscopically diagnosed and treated endometriosis.DESIGN: Multi-center, prospective, rand
- PMID 25761587
Japanese Journal
- 症例 性腺刺激ホルモン放出ホルモンアナログ投与による治療に成功した稀少部位子宮内膜症の1例
- 日本呼吸器学会誌 = Annals of the Japanese Respiratory Society 5(1), 52-56, 2016-01-10
- NAID 40020711038
- Gonadotropin-releasing hormone is prerequisite for the constitutive expression of pituitary annexin A5
- 卵巣癌術後化学療法におけるGnRHアナログの卵巣機能保護についての検討
Related Links
- GnRHアナログ( GnRHa ) は視床下部から分泌される自然のGnRHの数十倍から数百倍の強い生理活性をもつ人工ホルモンです。 GnRHアナログには、 ・ブセレリン（商品名；スプレキュア）点鼻薬・注射剤 ・ナ ...
- Question: クリニックでの誘発方法による妊娠率の統計を出しています。そこで、GnRHaの意味なのですが「ARTスタッフマニュアル」によると、GnRHaはGonadotropin releasing hormone analogueとなっているのですが文献などによると ...
★リンクテーブル★
[★]
- 英
- GnRH anonist
- 同
- (国試)GnRHアナログ GnRH analogue
GnRHアゴニスト
概念
- GnRH受容体アゴニスト。下垂体のGnRH受容体のダウンレギュレーションを狙って用いられる。GnRHよりGnRHに対する結合力が強く、継続的に使用することでGnRH受容体がダウンレギュレーションをうけてゴナドトロピンの分泌が抑制される。適応としては前立腺癌、閉経前乳癌治療、子宮内膜症治療である。
[★]
- 関
- analogue、derivate、derivative、relative
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[★]
- 関
- analog、derivative、relative
[★]
性腺刺激ホルモン放出ホルモン