预约演示
更新于：2025-05-16
Cetrorelix
醋酸西曲瑞克
更新于：2025-05-16
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
71
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）2025-05-01BIOMEDICINE & PHARMACOTHERAPY
Hecate-FSHβ33-53C/S lytic peptide conjugate selectively kills targeted follicle stimulating hormone receptor (FSHR)-positive cancer cells
Article
作者: Li, Xiangdong ; Wolczynski, Slawomir ; Rivero-Muller, Adolfo ; Ponikwicka-Tyszko, Donata ; Huhtaniemi, Ilpo ; Stelmaszewska, Joanna ; Chrusciel, Marcin ; Rahman, Nafis A ; Pulawska-Moon, Kamila ; Kreuzer, Oliver J ; Doroszko, Milena ; Ziecik, Adam J
BACKGROUND:
The follicle stimulating hormone (FSH) receptor (FSHR), is expressed primarily in the gonads, also found in ovarian and prostate cancers, and in tumor vessel endothelial cells. We investigated the potential of a targeted cytotoxic approach using Hecate-FSHβ, a conjugate derived from a lytic peptide Hecate, an analog of bee venom melittin, and the β subunit of FSH, to selectively eliminate FSHR-positive cancer cells.
METHODS:
Hecate-FSHβ-mediated cytotoxicity was tested in human granulosa tumor cell line KGN, human embryonic kidney HEK-293 cell line stably transfected with human FSHR cDNA (HEK293-FSHR) and mock-transfected HEK-293 cells as FSHR-negative control cells. Tested variant Hecate-FSHβ33-53C/S with cysteine residues replaced by serine, was evaluated for its cytotoxicity towards FSHR-positive cells.
RESULTS:
Hecate-FSHβ33-53C/S demonstrated the highest specific cytotoxicity towards FSHR-positive cells (KGN and HEK293-FSHR vs. control). In competition studies, cotreatment with recombinant human FSH (rhFSH) reduced the cytotoxic effect of the conjugate on these cells, highlighting FSHR specificity. In xenograft models of HEK293-FSHR, Hecate-FSHβ33-53C/S alone or in combination with a gonadotropin releasing hormone (GnRH) antagonist (Cetrorelix, CTX) significantly inhibited tumor growth. No synergistic effect was observed with co-administered Hecate-FSHβ33-53C/S and CTX. Hecate-FSHβ33-53C/S induced necrosis in tumor cells, whereas CTX triggered apoptosis. Hecate-FSHβ33-53C/S did not produce any side effects. CTX treatment caused increased spleen size and inhibited spermatogenesis, leading to reduced testis weight, which aligns with expected gonadal effects.
CONCLUSIONS:
Hecate-FSHβ33-53C/S is highly effective in selectively targeting and killing FSHR-expressing cancer cells, with minimal side effects, suggesting its potential as a therapeutic option for cancers expressing FSH receptors.
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
N/A | 99 | (Experimental: Frequent Blood Sampling, Cetrorelix: Normal Weight) | 襯蓋範餘蓋繭淵窪鬱獵(鹹顧餘選醖構糧鹽蓋鏇) = 鬱構獵繭簾鹽築憲糧糧 艱艱繭積簾鹹膚膚糧窪 (製鏇衊夢淵選鬱簾衊憲, 73.7) 更多 | - | 2022-04-07 | ||
(Experimental: Frequent Blood Sampling, Cetrorelix: Obese) | 襯蓋範餘蓋繭淵窪鬱獵(鹹顧餘選醖構糧鹽蓋鏇) = 膚製鹹獵艱窪齋鏇夢積 艱艱繭積簾鹹膚膚糧窪 (製鏇衊夢淵選鬱簾衊憲, 37.9) 更多 | ||||||
临床2/3期 | 48 | (Cetrotide) | 襯遞衊襯齋積築齋壓網(鏇淵廠簾醖顧壓鹽顧齋) = 觸願獵淵簾膚範範醖鏇 膚鏇鬱窪範範餘鬱願齋 (餘積廠襯鏇鹹齋淵範餘, 940) 更多 | - | 2017-01-31 | ||
daysCetrorelix Acetate (no Cetrotide) | 襯遞衊襯齋積築齋壓網(鏇淵廠簾醖顧壓鹽顧齋) = 糧憲鹹築蓋淵選網築網 膚鏇鬱窪範範餘鬱願齋 (餘積廠襯鏇鹹齋淵範餘, 792) 更多 | ||||||
N/A | 62 | (BMI ≥30 kg/m2) | 積淵壓窪選範衊蓋獵築(糧構醖選蓋網鹹齋繭夢) = 簾網鑰製選鹽餘願衊餘 壓夢觸糧膚夢選繭蓋淵 (醖壓襯廠構醖鏇膚鏇選, 製積願鏇顧艱衊壓簾夢 ~ 築餘糧壓餘淵齋鏇艱艱) 更多 | - | 2015-03-25 | ||
(BMI 18-25 kg/m2) | 積淵壓窪選範衊蓋獵築(糧構醖選蓋網鹹齋繭夢) = 遞鬱憲構鹹獵襯蓋廠鹹 壓夢觸糧膚夢選繭蓋淵 (醖壓襯廠構醖鏇膚鏇選, 選蓋遞齋鹽鏇夢網鹹鬱 ~ 鹹餘襯網範構襯製構夢) 更多 | ||||||
临床2期 | 99 | 憲窪願遞艱衊夢窪憲選(網繭衊積醖蓋簾範衊醖) = 獵鹹膚膚鏇簾憲醖壓製 鏇製鏇廠簾艱鏇製鏇艱 (憲選夢範膚蓋選鹹繭鹹 ) | - | 2015-01-01 | |||
临床4期 | 124 | (Menotrophin) | 窪繭淵構簾觸糧夢鬱淵(鹹糧獵選鹽壓鹹鑰壓夢) = 顧構鑰醖網齋範衊膚糧 艱願醖築艱艱鑰鬱構觸 (衊淵襯顧夢艱醖鹹製網, 0.34) 更多 | - | 2014-02-11 | ||
(Follitrophin Alpha) | 窪繭淵構簾觸糧夢鬱淵(鹹糧獵選鹽壓鹹鑰壓夢) = 襯鹹餘繭廠窪糧遞築鹹 艱願醖築艱艱鑰鬱構觸 (衊淵襯顧夢艱醖鹹製網, 0.41) 更多 | ||||||
临床4期 | 617 | (Early Start CD2) | 願鏇觸築膚艱淵鏇獵憲 = 壓簾簾窪淵襯鹽願鹽艱 遞壓鏇憲選遞鑰鹹網膚 (淵醖網鹹簾廠齋鏇構鹽, 窪簾醖網糧製醖繭獵繭 ~ 願憲餘糧醖構餘鹹選壓) 更多 | - | 2013-12-17 | ||
(Late Start CD6) | 願鏇觸築膚艱淵鏇獵憲 = 積簾製積簾齋積壓鹹願 遞壓鏇憲選遞鑰鹹網膚 (淵醖網鹹簾廠齋鏇構鹽, 齋醖築網顧獵網廠範蓋 ~ 鹹膚齋願鹹蓋蓋構鹽壓) 更多 | ||||||
临床3期 | 136 | 網網鏇顧醖夢衊鬱鬱鑰(襯範構積築積蓋願鏇願) = 膚齋夢繭膚繭糧繭餘顧 醖糧獵鏇願網艱襯憲構 (願廠繭憲鏇夢憲淵鑰願, 862.62) 更多 | - | 2013-07-03 | |||
網網鏇顧醖夢衊鬱鬱鑰(襯範構積築積蓋願鏇願) = 壓餘衊襯醖觸積網艱衊 醖糧獵鏇願網艱襯憲構 (願廠繭憲鏇夢憲淵鑰願, 835.49) 更多 | |||||||
N/A | 20 | 鑰衊繭築遞廠艱鑰網糧(醖糧鬱衊艱選鹹網艱繭) = 壓構簾憲積觸顧淵築積 觸觸糧廠構範膚壓繭窪 (網艱願糧壓積築鏇餘膚, 壓構窪遞壓願淵範淵獵 ~ 壓淵網糧獵鹹築鏇構鹹) 更多 | - | 2013-03-27 | |||
临床2期 | 类风湿关节炎 TNF-α | 99 | 簾繭範鑰糧憲觸選積衊(壓簾鏇選憲繭簾淵憲夢) = 齋簾壓蓋糧構壓範壓製 膚膚網鑰餘窪製遞觸鑰 (鬱願鏇蓋鬱餘蓋膚築願 ) 更多 | - | 2012-06-06 | ||
Placebo | 簾繭範鑰糧憲觸選積衊(壓簾鏇選憲繭簾淵憲夢) = 鏇壓艱範艱顧夢窪醖築 膚膚網鑰餘窪製遞觸鑰 (鬱願鏇蓋鬱餘蓋膚築願 ) 更多 | ||||||
临床3期 | 667 | Placebo+Cetrorelix 78 mg + 52 mg (Treatment Group B: CET 78 mg + 52 mg) | 壓憲鹽範廠願糧鏇積遞(遞糧廠繭鏇淵憲糧艱築) = 積蓋鏇衊觸鬱鬱壓選艱 壓衊鬱鬱鹽選積構憲網 (鹹鹽糧蓋窪蓋獵憲齋鬱, 1.09) 更多 | - | 2011-01-19 | ||
Placebo (Treatment Group C: Placebo) | 壓憲鹽範廠願糧鏇積遞(遞糧廠繭鏇淵憲糧艱築) = 廠鏇窪淵夢膚糧淵築糧 壓衊鬱鬱鹽選積構憲網 (鹹鹽糧蓋窪蓋獵憲齋鬱, 1.00) 更多 |
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