"目录号: HY-13665

GPCR/G Protein-

Leuprolide(Leuprorelin)醋酸盐是GnRH类似物，是脑垂体GnRH受体激动剂。

GNRH Receptor

相关产品

Degarelix-Alarelin Acetate-Goserelin acetate-Triptorelin-Nafarelin-Deslorelin-Relugolix-Abarelix-Cetrorelix Acetate-Elagolix-Gonadorelin acetate-Lecirelin-Buserelin Acetate-Leuprorelin-

生物活性

Description

Leuprolide acetate (Leuprorelin) is a GnRH analog; leuprolide acetate acts as an agonist at pituitary GnRH receptors.IC50 Value:Target: GnRH receptorBy interrupting the normal pulsatile stimulation of, and thus desensitizing, the GnRH receptors, it indirectly downregulates the secretion of gonadotropins luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to hypogonadism and thus a dramatic reduction in estradiol andtestosterone levels in both sexes.in vitro:  The number of DNA 3'-end-labeled cells/cm2 in leiomyomas of control patients and in leiomyomas at the 2nd, 8th, 12th, and 16th weeks of Leuprolide Acetate treatment were at low levels [1]. Testosterone, estradiol and progesterone were also reduced by LA, even though this reduction occurred for progesterone only at the highest LA dosage (10(-6)M; 606.0+/-114.3 ng/ml versus 1524.0+/-246.5 ng/ml; p=0.02) [2]. in vivo: Leuprolide acetate treatment decreases the severity of clinical signs of locomotion, induces a significantly greater body weight gain, increases the MBP and NFs expression, axonal area and cell infiltration in EAE animals [3]. Leuprolide (200 and 300 microg kg(-1) s.c.) per se showed anti-compulsive effect, causing statistically significant inhibition of marble-burying behavior of mice [4].Clinical trial: Neoadjuvant Abiraterone Acetate Plus Leuprolide Acetate in Men With Localized High Risk Prostate Cancer . Phase 2

Clinical Trial

NCT02154139

Takeda

Breast Cancer

December 2005

NCT02167893

Takeda

Prostate Cancer

October 2005

NCT02134977

Takeda

Breast Cancer

September 2011

NCT01442246

UNICANCER

Metastases

July 2011

Phase 3

NCT02920359

Parc de Salut Mar

There Are no Conditions Under Study. Healthy Volunteers

November 17, 2016

Phase 1

NCT03209492

Takeda

Prostate Cancer

April 1, 2016

NCT03209518

Takeda

Premenopausal Breast Cancer

March 1, 2016

NCT00378690

Astellas Pharma Inc

Prostate Cancer

March 2006

Phase 3

NCT01767090

Astellas Pharma Europe B.V.-Astellas Pharma Inc

Endometriosis

December 2012

Phase 2

NCT01458301

Takeda

Endometriosis

October 2011

Phase 2

NCT01452685

Takeda

Endometriosis

March 2012

Phase 2

NCT02778919

Kissei Pharmaceutical Co., Ltd.

Endometriosis

Phase 2

NCT00193856

Trans-Tasman Radiation Oncology Group (TROG)-National Health and Medical Research Council, Australia-Hunter Medical Research Institute (HMRI)-Health Research Council, New Zealand-Novartis Pharmaceuticals-Cancer Society of New Zealand-University of Newcastle, Australia-Calvary Mater Newcastle, Australia-Maitland Cancer Appeal-Abbott

Prostate Cancer

October 2003

Phase 3

NCT02393482

University of Cagliari

Amenorrhea-Endometriosis-Quality of Life

June 2016

Phase 4

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References

[1].Mizutani T, Sugihara A, Nakamuro K, Suppression of cell proliferation and induction of apoptosis in uterine leiomyoma by gonadotropin-releasing hormone agonist (leuprolide acetate). J Clin Endocrinol Metab. 1998 Apr;83(4):1253-5.

[2].Silva AL, Abreu LG, Rosa-e-Silva AC, Leuprolide acetate reduces both in vivo and in vitro ovarian steroidogenesis in infertile women undergoing assisted reproduction. Steroids. 2008 Dec 22;73(14):1475-84.

[3].Guzmán-Soto I, Salinas E, Hernández-Jasso I, Leuprolide acetate, a GnRH agonist, improves experimental autoimmune encephalomyelitis: a possible therapy for multiple sclerosis. Neurochem Res. 2012 Oct;37(10):2190-7.

[4].Gaikwad U, Parle M, Kumar A, Effect of ritanserin and leuprolide alone and combined on marble-burying behavior of mice. Acta Pol Pharm. 2010 Sep-Oct;67(5):523-7.