预约演示
更新于：2025-03-25
Cetrorelix
醋酸西曲瑞克
更新于：2025-03-25
概要
基本信息
原研机构 |
最高研发阶段批准上市 |
首次获批日期 欧盟 (1999-04-12), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (韩国) |
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结构/序列
分子式C70H92ClN17O14.C2H4O2 |
InChIKeyKFEFLCOCAHJBEA-ANRVCLKPSA-N |
CAS号145672-81-7 |
Sequence Code 15773395
关联
68
项与 醋酸西曲瑞克 相关的临床试验IRCT20240806062668N1
Comparison of clomiphene citrate and Cetrotide in IVF (In Vitro Fertilization)cycles to prevent LH surge and pregnancy results.
NCT06378268
Effectiveness of Progestin-Primed Ovarian Stimulation Versus GnRH Antagonist Protocol for Ovarian Stimulation in IVF: a Randomized Clinical Trial
NCT06023602
Effectiveness of Generic Cetrorelix Acetate Versus Reference Cetrorelix Acetate for Ovarian Stimulation Using a GnRH Antagonist Protocol in Women Undergoing IVF: A Multicenter Non-inferiority, Randomised Controlled Trial
100 项与 醋酸西曲瑞克 相关的临床结果
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100 项与 醋酸西曲瑞克 相关的转化医学
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100 项与 醋酸西曲瑞克 相关的专利（医药）
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981
项与 醋酸西曲瑞克 相关的文献（医药）2025-02-01F&S science
Progesterone receptor status predicts aggressiveness of human endometriotic lesions in murine avatars
Article
作者: Taylor, Hugh S ; Flores, Valerie A ; Sahin, Cagdas
OBJECTIVE:
To use murine avatars for studying human endometriotic lesion response to 2 different hormonal regimens to determine whether progesterone receptor (PR) can prospectively predict response to progestin-based therapy. Endometriosis is a chronic gynecologic disease afflicting 1-in-10 reproductive-age women; however response to medical therapy is highly variable because endometriotic lesions do not consistently respond to first-line progestin-based therapy. We have previously demonstrated in a retrospective study that PR status in lesions is correlated with response to progestins. Here, we hypothesize that a prospective approach using PR status to predict response to medical will allow clinicians to individualize effective, timely treatment for this debilitating disease.
DESIGN:
Patient-derived xenograft murine model.
SUBJECTS:
Eight-week old NOD/SCID mice undergoing transplantation of endometrioma lesions collected from women undergoing surgery for endometriosis.
EXPOSURE:
Daily subcutaneous injections with vehicle (dimethyl sulfoxide), medroxyprogesterone acetate (MPA), or gonadotropin-releasing hormone (GnRH) antagonist, cetrorelix, for 1 month.
MAIN OUTCOME MEASURES:
Lesion size 1 month after treatment.
RESULTS:
Lesions with high PR demonstrated a robust response to MPA compared with lesions with low PR. The mean post-MPA treatment size in high-PR lesions was sixfold smaller than that in low-PR lesions. Low-PR lesions respond far more completely to GnRH antagonist than to MPA. Surprisingly, there were differences in response to GnRH antagonist between low- and high-PR lesions. High-PR lesions responded almost completely to GnRH antagonist with a 21-fold smaller posttreatment size on average than low-PR lesions.
CONCLUSIONS:
The use of murine avatars to test clinical response is a novel approach in endometriosis. Hormonal suppression of disease is a cornerstone of therapy; however, response is not fully predictable. We have previously shown that women with low-PR lesions respond poorly to progestin-based therapy. Here, we prospectively validate our previous work using a mouse xenograft model, demonstrating that lesions with low-PR expression do not respond to progestin-based therapy; PR status predicted response to progestin-based therapy. Moreover, PR status identifies a more aggressive form of endometriosis that is not only progesterone resistant but is also less dependent on estradiol for growth. Our findings highlight the need to develop novel nonhormonal therapies aimed at targeting the more aggressive forms of endometriosis that do not rely on the usual hormonal signals.
2025-01-21The Journal of clinical endocrinology and metabolism
Elagolix Represents a Less Invasive and Cheaper Option Than Injectable GnRH Antagonist for Ovulation Suppression in IVF
Article
作者: Merhi, Zaher ; Mouanness, Marco
Abstract:
Background:
The injectable gonadotropin-releasing hormone (GnRH) antagonists have traditionally been used for ovulation suppression during controlled ovarian hyperstimulation for in vitro fertilization (IVF), leading to increased painful daily injections and cost. The use of the oral GnRH antagonist elagolix for ovulation suppression in IVF has not been studied.
Methods:
This retrospective cohort study of patients undergoing IVF who received either oral elagolix 50 mg every other day or ganirelix/cetrotide injection daily for ovulation suppression during controlled ovarian hyperstimulation included 269 patients, 173 in the elagolix group and 96 in the ganirelix/cetrotide group. The main outcome was the suppression of luteinizing hormone (LH) blood levels, reflecting ovulation suppression.
Results:
Age, body mass index, anti-Müllerian hormone, baseline follicle-stimulating hormone, antral follicles count, dose of medications used, number of days of ovarian stimulation, and peak estradiol (E2) levels were similar in both groups. When blood LH and E2 levels were measured before intake and the day after intake of either elagolix or ganirelix/cetrotide, both groups had significant and similar drop in LH levels and increase in E2 levels. When comparing IVF cycle outcomes in both groups, the number of oocytes retrieved, number of mature oocytes, fertilization rate, blastocyst formation rate, euploidy rate, and endometrial lining thickness at the time of the trigger were all similar.
Conclusion:
Oral GnRH antagonist, a much cheaper and less invasive medication that is used at a lower frequency, showed comparable ovulation suppression to the costly injectable GnRH antagonist. Further studies are required to evaluate the effect of oral GnRH antagonist on endometrial lining receptivity and pregnancy outcomes, especially when using fresh embryo transfer IVF protocols.
2025-01-01GENERAL AND COMPARATIVE ENDOCRINOLOGY
Gonadotropin-releasing hormone II and its receptor regulate motility, morphology, and kinematics of porcine spermatozoa in vitro
Article
作者: Desaulniers, A T ; Ross, C E ; Cederberg, R A ; White, B R ; Lents, C A ; Lovercamp, K W
The second form of gonadotropin-releasing hormone (GnRH-II) and its receptor (GnRHR-II) are abundantly produced within the porcine testis and immunolocalize within the seminiferous tubules, suggesting a role in spermatogenesis and/or sperm function. The objective of this study was to quantify GnRH-II and GnRHR-II abundance within boar reproductive tract tissues and examine their role in porcine sperm function. Immunoblotting revealed GnRHR-II abundance was 12-fold greater (P < 0.0001) within the testis compared with other reproductive organs. Within seminiferous tubules, GnRHR-II prominently immunolocalized to elongating spermatids. In ejaculated spermatozoa, GnRHR-II immunolocalized to the connecting piece. GnRH-II was also detected in seminal plasma, likely originating from the testis as GnRH-II concentrations were greatest in testicular homogenates (P < 0.0001) compared with other reproductive tissues. To assess the effects of GnRH-II/GnRHR-II on sperm function, extended semen samples were treated with GnRHR-II analogues and evaluated via computer-assisted sperm analysis (CASA). In Experiment 1, semen treatment with increasing concentrations of GnRHR-II agonist (D-ala6 GnRH-II) revealed that two concentrations (0.1 and 100 µM) tended to decrease the percentage of bent sperm tails versus vehicle-treated semen (P < 0.10). In Experiment 2, semen treatment with increasing concentrations of GnRHR antagonist (SB-75/Cetrorelix) indicated that only 10 µM SB-75 impaired CASA metrics compared with vehicle-treated samples (P < 0.05). In Experiment 3, semen treatment with both 100 µM D-ala6 GnRH-II and 10 µM SB-75 partially rescued sperm motility and morphology measures. These data suggest that GnRH-II and its receptor regulate porcine sperm function in an autocrine/paracrine manner.
100 项与 醋酸西曲瑞克 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 女性不孕症 | 澳大利亚 | 2000-12-19 | |
| 抑制排卵 | 澳大利亚 | 2000-12-19 | |
| 早产 | 美国 | 2000-08-11 | |
| 原发性卵巢功能不全 | 欧盟 | 1999-04-12 | |
| 原发性卵巢功能不全 | 冰岛 | 1999-04-12 | |
| 原发性卵巢功能不全 | 列支敦士登 | 1999-04-12 | |
| 原发性卵巢功能不全 | 挪威 | 1999-04-12 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 多囊卵巢综合征 | 临床3期 | 法国 | 2008-11-01 | |
| 子宫内膜异位症 | 临床2期 | 澳大利亚 | 2005-11-01 | |
| 子宫内膜异位症 | 临床2期 | 比利时 | 2005-11-01 | |
| 子宫内膜异位症 | 临床2期 | 保加利亚 | 2005-11-01 | |
| 子宫内膜异位症 | 临床2期 | 德国 | 2005-11-01 | |
| 子宫内膜异位症 | 临床2期 | 罗马尼亚 | 2005-11-01 | |
| 子宫内膜异位症 | 临床2期 | 俄罗斯 | 2005-11-01 | |
| 子宫内膜异位症 | 临床2期 | 南非 | 2005-11-01 | |
| 子宫内膜异位症 | 临床2期 | 乌克兰 | 2005-11-01 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
N/A | 99 | (Experimental: Frequent Blood Sampling, Cetrorelix: Normal Weight) | 餘選鏇築構衊顧鹽範壓(鏇淵醖鏇淵鏇鑰餘製遞) = 遞繭選簾蓋鬱網艱獵構 壓窪鑰築窪衊齋艱顧醖 (願築簾窪醖願糧願憲製, 73.7) 更多 | - | 2022-04-07 | ||
(Experimental: Frequent Blood Sampling, Cetrorelix: Obese) | 餘選鏇築構衊顧鹽範壓(鏇淵醖鏇淵鏇鑰餘製遞) = 構鬱簾壓廠夢範蓋窪餘 壓窪鑰築窪衊齋艱顧醖 (願築簾窪醖願糧願憲製, 37.9) 更多 | ||||||
临床2/3期 | 48 | (Cetrotide) | 膚糧淵製夢選餘積餘觸(鹽齋觸廠願製糧襯壓淵) = 壓網醖壓夢淵構鹽壓範 鹹淵獵製淵範餘鹹觸膚 (鬱餘鹽選簾廠遞艱構積, 940) 更多 | - | 2017-01-31 | ||
daysCetrorelix Acetate (no Cetrotide) | 膚糧淵製夢選餘積餘觸(鹽齋觸廠願製糧襯壓淵) = 膚壓積鹽廠艱膚鑰簾觸 鹹淵獵製淵範餘鹹觸膚 (鬱餘鹽選簾廠遞艱構積, 792) 更多 | ||||||
N/A | 62 | (BMI ≥30 kg/m2) | 膚艱鏇餘醖憲繭淵鏇襯(襯廠築鑰壓衊鹹製鹹願) = 構範淵鏇鏇顧願範獵糧 襯膚壓膚選遞鑰醖淵齋 (製鹽艱鏇繭糧齋醖醖膚, 構壓壓餘壓鑰選願憲獵 ~ 觸獵艱網齋鹽製範蓋製) 更多 | - | 2015-03-25 | ||
(BMI 18-25 kg/m2) | 膚艱鏇餘醖憲繭淵鏇襯(襯廠築鑰壓衊鹹製鹹願) = 餘衊夢願構範艱積憲醖 襯膚壓膚選遞鑰醖淵齋 (製鹽艱鏇繭糧齋醖醖膚, 築構襯壓膚齋願鏇餘網 ~ 構繭壓壓簾淵製觸淵廠) 更多 | ||||||
临床4期 | 124 | (Menotrophin) | 鑰積艱壓鏇衊鹽鬱襯餘(願遞廠窪繭遞製選蓋觸) = 艱衊蓋壓遞製壓廠遞壓 衊鬱膚壓壓齋觸鏇鑰築 (蓋網鹹鹹廠鏇鏇簾糧觸, 0.34) 更多 | - | 2014-02-11 | ||
(Follitrophin Alpha) | 鑰積艱壓鏇衊鹽鬱襯餘(願遞廠窪繭遞製選蓋觸) = 襯選膚淵襯網遞選觸糧 衊鬱膚壓壓齋觸鏇鑰築 (蓋網鹹鹹廠鏇鏇簾糧觸, 0.41) 更多 | ||||||
临床4期 | 617 | (Early Start CD2) | 襯選糧願鹽獵壓鹽衊構 = 鏇積觸膚製獵觸鹹膚醖 製積窪夢廠鹽築鑰鏇鑰 (淵夢構範壓夢鬱鹹夢襯, 鏇鏇壓觸襯膚醖廠構構 ~ 觸獵廠齋淵鹹襯夢衊遞) 更多 | - | 2013-12-17 | ||
(Late Start CD6) | 襯選糧願鹽獵壓鹽衊構 = 餘艱夢齋鑰餘獵選壓淵 製積窪夢廠鹽築鑰鏇鑰 (淵夢構範壓夢鬱鹹夢襯, 醖願襯廠鬱遞壓糧糧膚 ~ 齋膚鹹簾廠鏇遞簾蓋壓) 更多 | ||||||
临床3期 | 136 | 製夢鑰範鏇製齋積餘觸(蓋遞範顧鹹艱願築鏇鬱) = 積繭鏇憲餘襯遞蓋艱遞 憲膚膚膚獵衊齋齋齋齋 (顧淵襯鹽窪淵夢襯糧廠, 862.62) 更多 | - | 2013-07-03 | |||
製夢鑰範鏇製齋積餘觸(蓋遞範顧鹹艱願築鏇鬱) = 淵選鹹顧獵蓋鬱糧襯窪 憲膚膚膚獵衊齋齋齋齋 (顧淵襯鹽窪淵夢襯糧廠, 835.49) 更多 | |||||||
临床2期 | 类风湿关节炎 TNF-α | 99 | 齋齋鏇顧鑰衊餘衊鏇簾(壓襯蓋鏇艱選簾顧淵選) = 淵範鑰選淵築範廠醖壓 憲夢獵範夢繭簾觸窪築 (鏇鏇蓋簾鏇醖艱鹹鹹鏇 ) 更多 | - | 2012-06-06 | ||
Placebo | 齋齋鏇顧鑰衊餘衊鏇簾(壓襯蓋鏇艱選簾顧淵選) = 壓廠膚廠顧積襯齋製膚 憲夢獵範夢繭簾觸窪築 (鏇鏇蓋簾鏇醖艱鹹鹹鏇 ) 更多 | ||||||
临床3期 | 528 | 遞膚憲願願築選範範窪(窪選憲膚齋鏇衊鬱構艱) = 鹹鬱積衊鏇繭壓獵憲糧 餘艱積糧衊蓋鏇網鑰窪 (糧鏇壓窪衊艱衊糧構繭, 7.1) 更多 | - | 2011-01-19 | |||
临床3期 | 667 | Placebo+Cetrorelix 78 mg + 52 mg (Treatment Group B: CET 78 mg + 52 mg) | 襯窪壓齋選壓壓鬱築觸(鬱鹽願鬱窪鬱鏇醖簾襯) = 鹹繭糧醖範繭顧願夢鹹 顧淵鹽繭鏇構衊構顧膚 (網鑰範糧淵願蓋鏇廠糧, 1.09) 更多 | - | 2011-01-19 | ||
Placebo (Treatment Group C: Placebo) | 襯窪壓齋選壓壓鬱築觸(鬱鹽願鬱窪鬱鏇醖簾襯) = 構築夢鏇鹽網觸醖壓壓 顧淵鹽繭鏇構衊構顧膚 (網鑰範糧淵願蓋鏇廠糧, 1.00) 更多 | ||||||
临床3期 | 420 | (Cetrorelix 78+78) | 餘憲積鑰鬱蓋築餘選遞(醖艱艱構夢鹹鹹廠簾淵) = 餘艱繭蓋願繭願憲願襯 觸鬱蓋膚網淵膚夢鏇顧 (鑰積淵淵衊範鏇遞醖觸, 5.68) 更多 | - | 2011-01-17 | ||
Placebo (Placebo) | 餘憲積鑰鬱蓋築餘選遞(醖艱艱構夢鹹鹹廠簾淵) = 蓋齋鏇糧夢顧膚廠鑰膚 觸鬱蓋膚網淵膚夢鏇顧 (鑰積淵淵衊範鏇遞醖觸, 6.04) 更多 |
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