醋酸戈那瑞林(Gonadorelin Acetate) - 药物靶点：GnRHR_在研适应症：子宫内膜异位症，性腺机能减退，多囊卵巢综合征_专利_临床

概要

基本信息

药物类型

合成多肽

别名

Gonadorelin (INN)、ABBOTT-41070、Fertagyl

+ [8]

靶点

GnRHR

作用机制

GnRHR激动剂(促性腺激素释放激素受体激动剂)

治疗领域

肿瘤内分泌与代谢疾病泌尿生殖系统疾病

在研适应症

子宫内膜异位症性腺机能减退多囊卵巢综合征+ [1]

非在研适应症

女性不育伴无排卵不孕继发性睾丸衰竭

原研机构

Mitsubishi Tanabe Pharma Corp.

在研机构

Nipro ES Pharma KK

Mitsubishi Tanabe Pharma Corp.

非在研机构

Ferring Pharmaceuticals A/S

Handok, Inc.Ferring Pharmaceuticals, Inc.

最高研发阶段批准上市

首次获批日期

日本 (1989-01-17),

子宫内膜异位症性腺机能减退多囊卵巢综合征+ [1]

最高研发阶段(中国)-

特殊审评孤儿药 (美国)

登录后查看时间轴

结构/序列

分子式C57H81N17O15

InChIKeyJYBUTQCEURWWJD-VIRDRFNDSA-N

CAS号52699-48-6

Sequence Code 526451482

关联

7

项与醋酸戈那瑞林相关的临床试验

JPRN-jRCT2031240219

/ Suspended临床2期IIT

Phase II Trial of Endocrine therapy for patients with Metastatic extramammary Paget's disEase using daRolutAmide with/without LH-RH agonist. - EMPERAR trial

开始日期2024-08-01

申办/合作机构-

NCT04390646

/ Recruiting临床2/3期IIT

Effect of Pulsatile GnRH Therapy on Cognition in Down Syndrome: Randomized Placebo Control Study

Down syndrome (DS) is the most common chromosomal disorder; with the increasing life expectancy, about 80% of DS adults reach age 65 years old. Early Alzheimer's disease (AD) is the most common cause of death within this population. DS individuals already show AD neuropathology by the age of 30, while it becomes clinically recognized in their late forties. DS subjects also exhibit olfaction defects in adulthood.
To date, there is no treatment available for the cognitive or olfactory defects in DS. The development of an effective treatment targeting cognitive dysfunction in DS adolescents/adults would be warranted.
GnRH, a decapeptide secreted by hypothalamic neurons is the pilot light of reproduction in all mammals. Pulsatile GnRH acts on the gonadotrophs via the GnRH receptor (GNRHR) in the pituitary gland to stimulate LH and FSH, which themselves will act on the gonads to produce gametes and steroids. However, GNRHR are also expressed in cerebral cortex, hippocampus, amygdala, habenula, olfactory structures, and adrenal gland, suggesting that GnRH may have a role beyond reproduction.
Recently, GnRH has been shown to be involved in the process of ageing and lifespan control. Notably, in murine models, GnRH acts as an anti-ageing factor, independent of sex hormones. While ageing is characterized by hypothalamic inflammation and diminished neurogenesis, particularly in the hypothalamus and the hippocampus, GnRH was able to promote adult neurogenesis.
The regulation of GnRH secretion is complex and involves hormonal, neuronal input, and environmental factors.
Prévot et al. recently explored cognition within the Ts65Dn model and showed an age-dependent loss of the ability to recognize new objects. Also, these mice exhibit defects in olfaction. Given the role of GnRH in anti-aging mice model, pulsatile GnRH or continuous GnRH infusion (leading to desensitization of the GNRHR) were given to the Ts65Dn mice for two weeks. Amazingly, pulsatile but not continuous GnRH therapy was able to recover cognitive and olfaction defects.

开始日期2020-08-27

申办/合作机构

Centre Hospitalier Universitaire Vaudois

NCT04037605

/ Active, not recruiting早期临床1期IIT

Hormonal Mechanisms of Sleep Restriction - Axis Study in Older Men and Postmenopausal Women

The purpose of this study is to 1) determine how hypothalamic-pituitary-adrenal axis (HPA axis) activation occurs with sleep restriction and 2) evaluate how hypothalamic-pituitary-gonadal axis (HPG axis) deactivation occurs with sleep restriction. The investigator will also examine the cognitive function associated with sleep restriction, including food intake and food cravings.

开始日期2020-02-09

申办/合作机构

The Lundquist Institute

100 项与醋酸戈那瑞林相关的临床结果

登录后查看更多信息

100 项与醋酸戈那瑞林相关的转化医学

登录后查看更多信息

100 项与醋酸戈那瑞林相关的专利（医药）

登录后查看更多信息

2,654

项与醋酸戈那瑞林相关的文献（医药）

2025-03-01·THERIOGENOLOGY

Presynchronization with a progesterone device and prostaglandin F2α enhances ovulatory response to first GnRH, estrus expression and tended to increase fertility in beef heifers submitted to a 5-day CO-Synch protocol

Article

作者: Rojas Canadas, E ; Sánchez, J M ; Flores, T ; Lopez-Helguera, I

The main objectives of the present study were to determine the effects of presynchronizing with a 1.0 g intravaginal progesterone device (IVPD) and prostaglandin F2α and to assess the effects of re-utilization of IVPD in a 2x2 factorial design, on the ovulatory response to first GnRH, ovarian status at different protocol stages, estrus expression and fertility in beef heifers submitted to a 5d-CO-Synch + Progesterone (P4) protocol. Beef heifers (n = 564) were assigned to 1 of 2 treatments at D-15: Pres5 (n = 283), where heifers received a (IVPD) for 5 days and administration of prostaglandin F2α (25 mg of dinoprost) at D-10; and Control (n = 281), where heifers received no treatment. At D-8, all heifers received 100 μg of GnRH (gonadorelin acetate) and were assigned to 1 of 2 IVPD-use treatments: new-IVPD (n = 279), where animals received a new IVPD for 5 days, and once-used IVPD (n = 285), where heifers received a once-used IVPD for 5 days (used previously for 5 days). On D-3, IVPD was removed and 50 mg of prostaglandin F2α was administered. All heifers were timed artificially inseminated (AI; D0) 62 h after IVPD removal concomitant with an administration of 100 μg of GnRH. Estrus detection patches were placed on heifers at D-3 and evaluated at the time of AI. In a subset of heifers (n = 278), transrectal ultrasonography of the ovaries was carried out at D-8 and D-3 to assess presence and diameter of CL and largest follicle diameter (LFD). A blood sample was collected on D-3 to determine serum P4 concentration. Heifers with a once-used IVPD had a greater (P = 0.01) pregnancy per AI (P/AI) than heifers treated with a new-IVPD [62.8 % (179/285) vs 51.2 % (143/279)]. There was a lower percentage of animals (P = 0.002) having a corpus luteum (CL) on D-8 in Pres5 group compared to Control [16.4 % (22/134) vs 69.4 % (100/144)]. Similarly, a greater percentage of Pres5 heifers had a dominant follicle on D-8 (P < 0.0001) than Control heifers [97.7 % (131/134) vs 75.7 % (109/144)]. At D-3, Pres5 heifers had a greater ovulatory response to D-8 GnRH (P < 0.0001) compared to Control animals [82.8 % (111/134) vs 49.3 % (71/144)]. In addition, Pres5 heifers had a greater estrus expression behavior [87.6 % (248/283) vs 72.9 % (205/281); P < 0.0001] and tended to have (P = 0.10) a greater P/AI [61.8 % (175/283) vs 52.3 % (147/281)] than Control heifers. In conclusion, the tendency for a greater fertility observed in Pres5 heifers (∼10 %) justifies the extra animal handling required for presynchronization. A once-used IVPD represents a viable strategy to enhance P/AI and reduce the cost in beef heifers submitted to timed AI.

2024-11-01·INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES

Physicochemical and bioactive modifications of lotus root polysaccharides associated with probiotic fermentation

Article

作者: Wang, Hongxun ; Jiang, Xueyu ; Li, Mengzi ; Yi, Yang ; Sun, Ying ; Peng, Kaidi ; Jia, Chunlan

The physicochemical properties and bioactivities of lotus root polysaccharides (LRP) were investigated by examining the effects of probiotic fermentation. Five polysaccharides, namely LRP, LRP-Pl, LRPRh, LRPPa, and LRPAc, were extracted from unfermented and fermented lotus roots using Lactobacillus plantarum, Lactobacillus rhamnosus, Lactobacillus paracasei and Lactobacillus acidophilus, respectively. The results revealed that the yield of LRP-Ac (3.28 %) was 3.34 times higher than that of LRP (0.98 %), with its total sugar content and glucose content in the monosaccharide composition being the highest among the five polysaccharides. Probiotic fermentation led to an increase in Mw, as well as alterations in surface morphology and glycosidic bonds of LRPs, depending on the bacterial strains. Moreover, the five polysaccharides showed differences in antioxidant, α-amylase/α-glucosidase inhibitory, prebiotic, and macrophage-stimulating activities. Specifically, LRP-Pl exhibited the strongest DPPH radical scavenging ability; LRP-Rh showed the highest ABTS radical scavenging ability along with FRAP capacities; LRP-Ac possessed the greatest α-glucosidase inhibitory as well as prebiotic activities. However, the fermented polysaccharides showed relatively weak macrophage-stimulating ability compared to unfermented ones. Finally, the structure-activity relationship analysis revealed a close correlation between the chemical composition, Mw, and monosaccharide composition of LRPs and their bioactivities. These results are useful for the preparation of high-value LRPs.

2024-08-01·ANIMAL REPRODUCTION SCIENCE

Effect of hormonal treatment on artificial propagation, spawning performance and embryonic development of striped snakehead Channa striata (Bloch, 1793).

Article

作者: Tanu, Mohosena Begum ; Bhadra, Anuradha ; Rabiul Awal, Md ; Parvez, Imran ; Mahmud, Yahia ; Ashikur Rahman, Md ; Pervin, Rubaiya

Present study describes the spawning induction of striped Snakehead, Channa striata using carp pituitary extract (CPE) and LH-RH agonist i.e. Buserelin (Glp-His-Trp-Ser-Tyr-Ser-tBu-Leu-Arg-Pro-NHEt). Total four treatments were designed under both hormones trail and treated as control group, T₁, T₂, and T₃ with three replications of each treatment. While breeders under all hormone treatments showed spawning performances, no spawning performance was observed in control group. Latency time after hormonal treatment was lowest (20-24 hrs) in case of CPE than Buserelin (25-30 hrs). Regarding to CPE, spawning, fertilization and hatching rate were higher with the increasing doses of CPE in different treatments. The highest mean ± Standard deviation spawning, fertilization and hatching rate were 85.60±8.58 %, 79.38±4.89 % and 64.33±6.60 % respectively in T₃ where dose of CPE was 80 mg kg^-1. Similarly, in case of Buserelin hormone highest spawning rate was found in T₃ (80.61±5.59) where dose of Buserelin was 0.80 µg kg^-1 body weight. Fertilization rate was on the level 48.57±5.99, 70.62±5.33 and 90.32±4.79 respectively for T₁, T₂, and T₃.Whilst, hatching rate was found 20.81±4.91, 37.11±4.50 and 61.33±6.61 in T₁, T₂, and T₃ treatments respectively. However, T₃ exhibited best performance regarding spawning, fertilization and hatching rate which were significantly higher than other two treatments.The current study revealed that spawning induction using carp pituitary extract and Buserelin is effective and might be useful for artificial breeding of Channa striata. Regarding to dose application i.e. 80 mg kg^-1 of CPE and 0.80 µg kg^-1 of Buserelin may be successfully applied to ovulation stimulation of Channa striata.

100 项与醋酸戈那瑞林相关的药物交易

登录后查看更多信息

外链

KEGG	Wiki	ATC	Drug Bank
D08027	-	H01CA01 V04CM01	DB00644

研发状态

批准上市

10 条最早获批的记录,

登录

后查看更多信息

适应症	国家/地区	公司	日期
不孕	韩国	Handok, Inc.	1992-12-19
子宫内膜异位症	日本	Mitsubishi Tanabe Pharma Corp.	1989-01-17
性腺机能减退	日本	Nipro ES Pharma KK	1989-01-17
多囊卵巢综合征	日本	Mitsubishi Tanabe Pharma Corp.	1989-01-17
前列腺增生症	日本	Mitsubishi Tanabe Pharma Corp.	1989-01-17

未上市

10 条进展最快的记录,

登录

后查看更多信息

适应症	最高研发状态	国家/地区	公司	日期
继发性睾丸衰竭	临床3期	美国	Ferring Pharmaceuticals A/S	2014-04-01
继发性睾丸衰竭	临床3期	加拿大	Ferring Pharmaceuticals A/S	2014-04-01
女性不育伴无排卵	临床3期	美国	Ferring Pharmaceuticals A/S	2005-02-01

登录后查看更多信息

临床结果

适应症

分期

评价

查看全部结果

研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


ESPE2022	N/A	性早熟 kisspeptin-1 \| ghrelin \| estradiol ... 更多	-	Relefact LHRH®	壓獵願衊製蓋艱窪鬱範(築淵廠餘築願蓋襯艱獵) = 鑰壓築鹽築鬱遞觸築簾遞憲鬱淵壓獵觸遞壓蓋 (鏇餘鹽齋鬱艱簾蓋憲醖 )	-	2022-09-15
NCT01976728 (CTgov)	临床3期	继发性睾丸衰竭	39	Gonadorelin acetate subcutaneous (SC) 10 μg/pulse as a fixed dose, administered via. OmniPod pump (LutrePulse 10 µg/Pulse)	鑰築鹽窪遞鹽鬱鹹願憲(遞繭觸簾鹽蓋鑰選醖鑰) = 糧願獵鏇餘築製鑰餘獵範繭餘繭獵構餘鑰願鹹 (壓遞膚糧願顧顧鬱選選, 範選衊糧遞膚積襯衊鹹 ~ 鬱醖蓋鹹鏇襯襯顧餘鏇) 更多	-	2021-03-03
				Gonadorelin acetate SC 15 μg/pulse as a fixed dose, administered via. OmniPod pump (LutrePulse 15 µg/Pulse)	鑰築鹽窪遞鹽鬱鹹願憲(遞繭觸簾鹽蓋鑰選醖鑰) = 衊齋顧積鑰餘觸鹽襯廠範繭餘繭獵構餘鑰願鹹 (壓遞膚糧願顧顧鬱選選, 齋膚鹹襯選淵顧製餘餘 ~ 獵鏇壓廠構繭遞築築鹹) 更多
ASCO_GU2016	N/A	前列腺癌新辅助 \| 辅助	670	Buserelin	艱齋襯遞餘淵願窪鹽選(鑰鏇齋顧簾憲顧蓋夢積) = 糧製網糧鹹淵築選願鹽餘鏇選齋繭衊範壓構醖 (膚願壓築蓋獵顧齋淵壓 )	-	2016-01-10
				Goserelin	艱齋襯遞餘淵願窪鹽選(鑰鏇齋顧簾憲顧蓋夢積) = 獵廠蓋網蓋醖憲艱襯膚餘鏇選齋繭衊範壓構醖 (膚願壓築蓋獵顧齋淵壓 )
ASCO2015	N/A	早期乳腺癌	827	GnRHa	廠顧繭網廠鏇範鹽醖鬱(鏇網糧選遞夢範餘廠襯): OR = 1.79 (95% CI, 0.97 ~ 3.31)	-	2015-05-20
				Placebo
NCT01457703 (CTgov)	N/A	肥胖	62	Recombinant LH+Cetrorelix+Letrozole+Gonadorelin-GnRH (BMI ≥30 kg/m2)	製網選壓築醖齋鬱糧糧(網糧壓醖壓簾襯衊顧夢) = 鹽觸膚簾製餘選淵糧衊築觸鬱艱繭製醖廠鹽廠 (願顧窪鹹糧遞製鏇遞鹽, 淵衊襯觸願製積願蓋構 ~ 鏇齋鹹顧範糧願蓋範齋) 更多	-	2015-03-25
				Recombinant LH+Cetrorelix+Letrozole+Gonadorelin-GnRH (BMI 18-25 kg/m2)	製網選壓築醖齋鬱糧糧(網糧壓醖壓簾襯衊顧夢) = 襯蓋築糧窪鹽壓蓋繭構築觸鬱艱繭製醖廠鹽廠 (願顧窪鹹糧遞製鏇遞鹽, 觸鑰鏇淵醖繭憲遞積獵 ~ 醖糧製醖夢壓網範夢醖) 更多
JMTO BC08-01 (ASCO2012)	临床2期	晚期乳腺癌	37	LH-RH analogue (GOS) + Aromatase inhibitor (ANA)	願餘積淵網壓廠醖艱網(鹹鏇鏇憲範蓋廠鹹鹹獵) = 壓廠膚觸簾憲鏇襯衊艱觸遞夢襯願繭醖艱選製 (醖顧獵蓋壓觸夢繭鬱醖, 8.0 ~ 35.2) 更多	-	2012-05-20