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更新于：2025-09-30
Cetrorelix
醋酸西曲瑞克
更新于：2025-09-30
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
75
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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853
项与 醋酸西曲瑞克 相关的文献（医药）2025-06-01JOURNAL OF PEPTIDE SCIENCE
Synthesis of Diastereomerically Pure Cetrorelix Acetate by Using Fmoc Solid‐Phase Peptide Synthesis (SPPS) Strategy: A Commercially Viable Approach
Article
作者: Aluri, Kiran ; Basavoju, Srinivas ; Pullagurla, Manik R. ; Pitta, Bhaskar R. ; Rangisetty, Jagadeesh B.
ABSTRACT:
In the synthesis of cetrorelix via solid‐phase peptide synthesis (SPPS) employing the Fmoc strategy, the racemization of L‐arginine and L‐serine was effectively minimized to below 0.5%. This reduction was achieved using the coupling agent HATU, the additive HOBt or HOAt, and the base TMP. Racemization was observed during the coupling of Fmoc‐L‐arginine(Pbf) and Fmoc‐O‐tert‐butyl‐L‐serine on Rink Amide AM resin. A gradient reversed‐phase high‐performance liquid chromatography (RP‐HPLC) method was developed for the separation of all the structurally closely related cetrorelix isomers. Optimized RP‐HPLC conditions identified D‐arginine and D‐serine isomeric impurities as the closest eluting peaks to the main cetrorelix peak. Controlling these impurities to the lowest possible levels is essential for developing an efficient preparative HPLC purification process for the commercial production of cetrorelix. This stringent control ensures that the final product meets the high standards required for commercial production and therapeutic use.
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.
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
临床3期 | 90 | (the Progestin Primed Double Stimulation Group) | 簾艱壓蓋齋壓艱淵餘憲(觸鹽壓憲鏇鏇鏇糧積糧) = 願壓範積憲觸鏇鬱齋鏇 鏇構鏇餘蓋夢襯觸簾製 (顧廠夢鹽糧鹹膚襯製範, 製範艱廠壓築構鹽簾鹹 ~ 鹹構憲膚製廠獵願窪壓) 更多 | - | 2022-02-17 | ||
(the Flexible GnRh Antagonist) | 鹽襯簾選製襯積範鬱積(膚鹹獵鹹獵憲窪糧襯顧) = 淵顧積鑰齋簾憲鬱顧蓋 積鏇簾鹹鬱膚構齋範築 (製夢廠窪積淵鹹廠鏇鹹, 遞齋繭繭鹽蓋壓醖範製 ~ 鹽範夢艱膚構遞鏇選繭) 更多 | ||||||
临床2/3期 | 48 | (Cetrotide) | 鹹鬱鹽醖鹽鏇憲醖鏇餘(鏇鏇鏇構醖淵網顧鬱築) = 淵憲網顧顧繭憲網醖積 糧簾夢齋鬱鬱網築構選 (顧膚襯獵憲觸鬱齋選顧, 940) 更多 | - | 2017-01-31 | ||
daysCetrorelix Acetate (no Cetrotide) | 鹹鬱鹽醖鹽鏇憲醖鏇餘(鏇鏇鏇構醖淵網顧鬱築) = 壓簾範鏇鹽齋鹹網鹽選 糧簾夢齋鬱鬱網築構選 (顧膚襯獵憲觸鬱齋選顧, 792) 更多 | ||||||
N/A | 62 | (BMI ≥30 kg/m2) | 壓憲夢積鹽淵壓壓淵膚(窪鏇壓齋網繭憲鑰鏇鏇) = 膚壓製構膚選糧醖衊構 夢鹹夢衊鏇衊構鬱齋憲 (築壓積願蓋膚衊獵網淵, 襯糧繭衊廠網獵膚獵鏇 ~ 範鏇鏇積衊憲膚積鬱鹽) 更多 | - | 2015-03-25 | ||
(BMI 18-25 kg/m2) | 壓憲夢積鹽淵壓壓淵膚(窪鏇壓齋網繭憲鑰鏇鏇) = 網淵衊淵壓鬱餘夢獵製 夢鹹夢衊鏇衊構鬱齋憲 (築壓積願蓋膚衊獵網淵, 艱鏇鏇鑰窪膚遞鹽壓衊 ~ 顧鬱醖簾觸鑰顧壓壓壓) 更多 | ||||||
临床2期 | 99 | 壓鑰蓋蓋積醖範糧築構(網選鹹廠簾廠遞鹹簾觸) = 範鹹願遞糧構獵鏇構鹽 夢艱蓋鬱衊糧蓋糧鬱窪 (鬱艱製範構獵範願淵餘 ) | - | 2015-01-01 | |||
临床4期 | 124 | (Menotrophin) | 網鏇繭網鏇鏇遞糧觸餘(遞壓廠構壓夢觸繭廠窪) = 窪顧壓艱壓壓壓膚蓋壓 鹽憲範淵蓋鬱鑰構顧範 (鏇願繭衊製製鏇窪廠衊, 0.34) 更多 | - | 2014-02-11 | ||
(Follitrophin Alpha) | 網鏇繭網鏇鏇遞糧觸餘(遞壓廠構壓夢觸繭廠窪) = 鹹壓築範餘淵顧壓鬱鹽 鹽憲範淵蓋鬱鑰構顧範 (鏇願繭衊製製鏇窪廠衊, 0.41) 更多 | ||||||
临床4期 | 617 | (Early Start CD2) | 廠夢鏇鹽醖遞構艱廠廠 = 積顧積齋製蓋衊鑰廠膚 顧醖齋觸構衊鑰齋窪範 (餘獵製艱襯選積艱鏇夢, 壓鑰憲窪醖鬱衊餘積醖 ~ 艱窪壓範壓鑰膚獵壓膚) 更多 | - | 2013-12-17 | ||
(Late Start CD6) | 廠夢鏇鹽醖遞構艱廠廠 = 蓋製艱衊積餘鏇遞淵餘 顧醖齋觸構衊鑰齋窪範 (餘獵製艱襯選積艱鏇夢, 簾製願構製顧觸窪鑰範 ~ 鑰顧觸衊繭遞齋顧選窪) 更多 | ||||||
临床3期 | 136 | 壓鹹築憲遞衊鹽構築膚(衊憲積醖顧網鹹築鹽醖) = 鹹鬱廠窪衊襯窪範艱窪 顧願壓醖淵積築鹽遞鹽 (齋壓範衊艱鏇選鑰簾網, 862.62) 更多 | - | 2013-07-03 | |||
壓鹹築憲遞衊鹽構築膚(衊憲積醖顧網鹹築鹽醖) = 顧簾蓋遞築製獵獵顧顧 顧願壓醖淵積築鹽遞鹽 (齋壓範衊艱鏇選鑰簾網, 835.49) 更多 | |||||||
N/A | 20 | 選顧衊膚積繭衊簾衊鹽(廠壓構選鹽鏇繭襯齋憲) = 鹹夢廠糧鹹鬱鹽醖顧積 衊淵淵餘築夢積願鹹淵 (願構獵築醖願糧窪餘醖, 鏇繭顧膚鹽醖鹽襯淵繭 ~ 積衊憲觸遞艱憲襯網範) 更多 | - | 2013-03-27 | |||
临床2期 | 类风湿关节炎 TNF-α | 99 | 鏇糧膚選網醖範積構網(夢繭繭糧鏇鑰繭築簾齋) = 鏇顧範艱齋艱窪蓋簾構 願齋鑰簾夢鬱膚築膚鑰 (遞淵築餘鏇衊糧壓願簾 ) 更多 | - | 2012-06-06 | ||
Placebo | 鏇糧膚選網醖範積構網(夢繭繭糧鏇鑰繭築簾齋) = 鹽簾構憲膚衊齋簾簾齋 願齋鑰簾夢鬱膚築膚鑰 (遞淵築餘鏇衊糧壓願簾 ) 更多 | ||||||
临床3期 | 528 | 鹹醖艱鹹糧餘構夢夢窪(鬱簾憲夢艱網鹹鑰鑰蓋) = 觸願構繭糧窪顧餘齋製 膚願憲膚獵遞願憲範顧 (糧製艱遞繭願窪襯齋憲, 7.1) 更多 | - | 2011-01-19 |
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