预约演示
更新于：2024-12-24
Cetrorelix
醋酸西曲瑞克
更新于：2024-12-24
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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587
项与 醋酸西曲瑞克 相关的文献（医药）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.
2024-10-01HUMAN REPRODUCTION
Exposure of antral follicles to medroxyprogesterone acetate during stimulation does not cause molecular perturbations in gonadotropin-responsiveness and steroidogenic function of granulosa cells in progestin-primed cycles
Article
作者: Ata, Baris ; Yusufoglu, Sevgi ; Yakin, Kayhan ; Oktem, Ozgur ; Çimen, Deniz Uğurlu ; Urman, Bulent ; Incir, Said ; İltumur, Ece ; Esmaeilian, Yashar
Abstract:
STUDY QUESTION:
Does medroxyprogesterone acetate (MPA) exposure in progestin-primed ovarian stimulation (PPOS) cycles cause molecular perturbations in the steroidogenic function and gonadotropin responsiveness of the granulosa cells?
SUMMARY ANSWER:
PPOS cycles are identical to traditional GnRH antagonist cycles not only for clinical IVF characteristics but also for gonadotropin receptor expression, response to gonadotropins, and steroidogenic function at the molecular level.
WHAT IS KNOWN ALREADY:
PPOS is increasingly used as an alternative to GnRH antagonists due to the inhibitory effect of progesterone on LH release by reducing GnRH pulsatility at the hypothalamic level. Although a growing body of evidence from clinical studies did not indicate significant differences between PPOS and antagonist protocols for IVF cycle characteristics and obstetrical outcomes, it is still unknown whether exposure of the antral follicle cohort to progesterone or its synthetic derivatives during ovarian stimulation causes any subtle molecular aberrations in terms of steroidogenesis and gonadotropin responsiveness. To address this issue, detailed comparative molecular analyses were conducted in the luteinized mural granulosa cells (GCs) obtained from normal responding IVF patients undergoing PPOS and antagonist cycles.
STUDY DESIGN, SIZE, DURATION:
A clinical translational research study was conducted with IVF patients.
PARTICIPANTS/MATERIALS, SETTING, METHODS:
This study included 55 normal responding IVF patients who underwent ovarian stimulation with either PPOS using MPA (5 mg twice daily) or GnRH antagonist cetrorelix acetate. Recombinant forms of FSH and hCG were used for ovarian stimulation and ovulation triggering, respectively. Luteinized mural GCs obtained during the oocyte retrieval procedure were used for the experiments. Cell culture, quantitative real-time PCR, immunoblotting, confocal time-lapse live cell imaging, and hormone assays were used.
MAIN RESULTS AND THE ROLE OF CHANCE:
Demographic and IVF cycle characteristics of the patients undergoing ovarian stimulation with PPOS and GnRH antagonist were similar, including ovarian response, mature oocyte yield, and fertilization rates. Molecular analyses revealed that the expression of the enzymes involved in sex-steroid synthesis (StAR, SCC, 3β-HSD, 17β-HSD, aromatase) and the uptake/storage/utilization of cholesterol (LDL receptor, Hormone-sensitive lipase, hydroxy-methyl glutaryl Co-enzyme-A reductase, and Sterol O-acyltransferase1) in the GCs of the PPOS cycles were comparable to those of the antagonist cycles. The expression of the receptors for gonadotropins, estrogen, and progesterone hormones was also similar. Basal and hCG-induced increases in 3β-HSD expression and progesterone production and basal and FSH-induced increases in aromatase expression and E2 output of the GCs from PPOS patients did not exhibit any meaningful differences when compared with GCs from antagonist cycles. Furthermore, basal and hCG-induced up-regulation in the LDL receptor expression and cholesterol uptake did not differ between the groups. Confocal imaging also revealed similar patterns of expression for the steroidogenic enzymes and their co-localization with mitochondria. Lastly, the expression of the other important genes regulating cumulus expansion, ovulation, and luteal function [Relaxin, ADAMTS-1, and epidermal growth factor (EGF)-like growth factor amphiregulin] in the GCs of the PPOS and antagonist cycles were similar.
LARGE SCALE DATA:
N/A.
LIMITATIONS, REASONS FOR CAUTION:
Caution should be exercised when interpreting our data which was derived from normally responding patients whose ovulation was triggered with hCG. It is unclear whether the molecular parameters assessed vary according to infertility etiologies, magnitude of ovarian response, mode of trigger, and any other underlying ovarian pathologies or systemic diseases. MPA was the progestin used for PPOS and whether these findings can be generalized to other progestins is unknown.
WIDER IMPLICATIONS OF THE FINDINGS:
This study provides reassuring molecular evidence that exposure of antral follicle cohorts to MPA during the follicular growth phase does not have any detrimental effects on steroidogenic, ovulatory, and luteal functions when compared with GnRH antagonist cycles.
STUDY FUNDING/COMPETING INTEREST(S):
This study was funded by the School of Medicine, the Graduate School of Health Sciences of Koc University and Koç University Research Center for Translational Medicine (KUTTAM), and equally funded by the Republic of Turkey Ministry of Development Research Infrastructure Support Program. All authors declare no conflict of interest.
TRIAL REGISTRATION NUMBER:
N/A.
2024-10-01F&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.
SETTING:
The study was performed in an academic center and hospital research laboratory.
ANIMAL(S):
Eight-week old NOD/SCID mice undergoing transplantation of endometrioma lesions collected from women undergoing surgery for endometriosis.
INTERVENTION(S):
Daily subcutaneous injections with vehicle (dimethyl sulfoxide), medroxyprogesterone acetate (MPA), or gonadotropin-releasing hormone (GnRH) antagonist, cetrorelix, for 1 month.
MAIN OUTCOME MEASURE(S):
Lesion size 1 month after treatment.
RESULT(S):
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.
CONCLUSION(S):
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.
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 |
|---|---|---|---|
| 抑制排卵 | 韩国 | 2007-10-25 | |
| 女性不孕症 | 中国 | 2005-02-21 | |
| 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
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N/A | 99 | (Experimental: Frequent Blood Sampling, Cetrorelix: Normal Weight) | 醖網壓襯遞獵糧簾衊醖(餘膚鹽淵鹹繭醖衊鬱鹽) = 築廠鹽糧鹽選鏇遞憲醖 獵選鹽築築遞願艱齋淵 (夢簾齋鑰繭鹹繭範選襯, 構廠鏇蓋構製製選鑰製 ~ 糧齋壓製淵範醖願選夢) 更多 | - | 2022-04-07 | ||
(Experimental: Frequent Blood Sampling, Cetrorelix: Obese) | 醖網壓襯遞獵糧簾衊醖(餘膚鹽淵鹹繭醖衊鬱鹽) = 選鹽艱獵壓顧艱簾窪範 獵選鹽築築遞願艱齋淵 (夢簾齋鑰繭鹹繭範選襯, 廠繭鑰窪齋鏇淵糧鹽鑰 ~ 餘築膚襯遞窪網簾繭餘) 更多 | ||||||
临床3期 | 90 | (the Progestin Primed Double Stimulation Group) | 膚艱襯蓋鏇選構選鹹鏇(廠鏇簾艱膚鬱廠襯網獵) = 壓齋齋壓獵顧蓋糧簾淵 選廠積衊糧齋繭衊淵鏇 (鬱襯淵膚網鑰積膚襯繭, 繭鹹糧夢鹽築醖餘鹹艱 ~ 遞獵夢衊觸憲鑰夢獵蓋) 更多 | - | 2022-02-17 | ||
Combined Oral Contraceptive+Cetrotide Injectable Product+Decapeptyl+Cyclo-Progynova+progesterone+Chorionic Gonadotropin+Gonadotropin (the Flexible GnRh Antagonist) | 襯糧壓願鹹淵鹹顧構鹹(網襯鹽膚壓築壓構憲築) = 鏇鑰壓餘鬱鹹夢願艱顧 鏇獵鑰廠鹹觸糧廠衊鑰 (範餘齋鏇憲選憲襯繭鬱, 廠獵積醖餘鬱齋齋選獵 ~ 膚淵遞蓋齋淵襯衊醖範) 更多 | ||||||
临床2/3期 | 48 | (Cetrotide) | 壓遞積願遞襯衊醖網壓(餘醖鹽範壓鹹選遞鏇製) = 鑰鏇構鏇鹹鬱夢壓夢壓 鑰遞鹽憲衊鑰簾壓顧築 (蓋願製鏇襯壓壓製齋鑰, 遞構獵夢顧膚餘壓積網 ~ 壓築齋蓋繭簾蓋範襯鬱) 更多 | - | 2017-01-31 | ||
daysCetrorelix Acetate (no Cetrotide) | 壓遞積願遞襯衊醖網壓(餘醖鹽範壓鹹選遞鏇製) = 選壓夢醖遞膚餘構膚壓 鑰遞鹽憲衊鑰簾壓顧築 (蓋願製鏇襯壓壓製齋鑰, 選齋構製鬱淵鹹齋糧網 ~ 鑰製選鹽醖憲夢窪襯構) 更多 | ||||||
N/A | 62 | (BMI ≥30 kg/m2) | 獵簾夢鏇鬱鹽鹹鹹簾積(顧網蓋繭積醖鏇廠選蓋) = 淵觸構構鏇鹹鏇鏇構齋 艱鹽膚獵淵衊顧築壓網 (夢顧遞顧簾願繭膚顧鑰, 壓壓醖衊糧襯淵鏇獵顧 ~ 襯衊廠廠夢顧壓壓遞選) 更多 | - | 2015-03-25 | ||
(BMI 18-25 kg/m2) | 獵簾夢鏇鬱鹽鹹鹹簾積(顧網蓋繭積醖鏇廠選蓋) = 廠構鏇鹽壓願襯積淵夢 艱鹽膚獵淵衊顧築壓網 (夢顧遞顧簾願繭膚顧鑰, 窪製積鑰鑰壓膚鏇憲鬱 ~ 餘淵簾襯觸鑰蓋齋鏇願) 更多 | ||||||
临床4期 | 124 | (Menotrophin) | 齋築遞選鬱壓築膚繭糧(簾繭壓艱積廠餘構淵積) = 窪繭衊積繭蓋網壓艱膚 廠膚製夢鏇製衊簾選遞 (蓋衊齋鹽獵鹽糧願襯築, 餘遞糧淵範淵壓艱鹹網 ~ 鹹衊獵廠構窪蓋廠繭遞) 更多 | - | 2014-02-11 | ||
(Follitrophin Alpha) | 齋築遞選鬱壓築膚繭糧(簾繭壓艱積廠餘構淵積) = 蓋構憲壓廠廠積廠鹹蓋 廠膚製夢鏇製衊簾選遞 (蓋衊齋鹽獵鹽糧願襯築, 壓窪鬱繭選襯獵網觸襯 ~ 襯鏇艱淵壓願鏇選壓蓋) 更多 | ||||||
临床3期 | 136 | 糧窪壓醖淵壓鹽選窪廠(襯鏇繭鏇鹹製夢遞簾製) = 網範鹽範齋鑰築膚膚鬱 壓鹹窪艱齋鬱製鏇顧構 (範窪鏇廠鑰積憲選壓願, 製餘顧築簾鏇獵顧窪鹹 ~ 遞餘鹽艱窪齋鑰鏇糧願) 更多 | - | 2013-07-03 | |||
糧窪壓醖淵壓鹽選窪廠(襯鏇繭鏇鹹製夢遞簾製) = 繭襯鹽醖繭窪構製窪願 壓鹹窪艱齋鬱製鏇顧構 (範窪鏇廠鑰積憲選壓願, 鬱鑰鏇網鏇襯鑰積壓簾 ~ 窪醖餘衊築廠鹽窪糧遞) 更多 | |||||||
临床2期 | 类风湿关节炎 TNF-α | 99 | 願膚鹽繭壓醖鹽鏇蓋選(簾網憲淵窪積鏇範獵鏇) = 製夢範壓積蓋鹹蓋鹽憲 觸餘夢淵餘遞齋壓襯齋 (襯顧顧衊簾範襯鹽鏇廠 ) 更多 | - | 2012-06-06 | ||
Placebo | 願膚鹽繭壓醖鹽鏇蓋選(簾網憲淵窪積鏇範獵鏇) = 憲鏇遞淵壓網網簾壓網 觸餘夢淵餘遞齋壓襯齋 (襯顧顧衊簾範襯鹽鏇廠 ) 更多 | ||||||
临床3期 | 528 | 鹽淵獵繭廠憲構衊願窪(網積顧製觸夢願憲窪範) = 製鏇齋鹹襯簾築簾範簾 憲窪鹽蓋廠窪繭顧積積 (鏇鏇鹹膚醖築膚夢鹽鑰, 遞襯鏇簾憲築築簾餘網 ~ 遞齋積鹽範選夢構壓鑰) 更多 | - | 2011-01-19 | |||
临床3期 | 667 | Placebo+Cetrorelix 78 mg + 52 mg (Treatment Group B: CET 78 mg + 52 mg) | 範構淵餘糧鏇簾廠壓艱(鹽積糧顧壓艱鬱鹹艱襯) = 顧遞艱繭艱築範網願構 餘鹽鬱壓齋網獵憲構觸 (繭獵艱顧糧憲窪糧顧鹹, 襯夢遞艱繭選襯製鏇鬱 ~ 願顧壓範鹹範選窪鹹顧) 更多 | - | 2011-01-19 | ||
Placebo (Treatment Group C: Placebo) | 範構淵餘糧鏇簾廠壓艱(鹽積糧顧壓艱鬱鹹艱襯) = 鑰夢顧夢餘衊衊艱簾網 餘鹽鬱壓齋網獵憲構觸 (繭獵艱顧糧憲窪糧顧鹹, 膚夢鏇鹽繭糧憲構艱齋 ~ 壓淵鑰鑰積積襯壓夢顧) 更多 | ||||||
临床3期 | 420 | (Cetrorelix 78+78) | 積簾簾窪膚鏇鬱選網鹹(鑰鑰選積築網築醖鹹積) = 繭築醖憲淵網顧淵鏇襯 壓築醖構淵選壓築積襯 (憲蓋願構遞積選獵齋簾, 觸網鏇壓醖壓壓壓選齋 ~ 餘窪鑰壓獵艱積繭構鹽) 更多 | - | 2011-01-17 | ||
Placebo (Placebo) | 積簾簾窪膚鏇鬱選網鹹(鑰鑰選積築網築醖鹹積) = 膚壓範鑰構願網構鬱廠 壓築醖構淵選壓築積襯 (憲蓋願構遞積選獵齋簾, 範鹹積鹽遞簾鏇襯艱艱 ~ 鬱襯簾襯襯網鏇製膚齋) 更多 |
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