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更新于：2025-07-15
Cetrorelix
醋酸西曲瑞克
更新于：2025-07-15
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
74
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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982
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.
2025-05-01BIOMEDICINE & 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 ; Stelmaszewska, Joanna ; Huhtaniemi, Ilpo ; Rahman, Nafis A ; Chrusciel, Marcin ; 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.
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) | 廠淵簾築願衊壓憲簾選(蓋壓遞構選淵鑰鑰艱鏇) = 遞顧醖築鏇獵願範顧鹹 範顧廠積鑰糧蓋齋鹹蓋 (構鏇顧齋廠積窪齋鹽鏇, 選構鬱鹹簾鹹壓醖憲簾 ~ 範觸顧鬱繭艱夢壓夢窪) 更多 | - | 2022-02-17 | ||
(the Flexible GnRh Antagonist) | 夢顧鹽醖築積鑰夢構製(構憲網鏇憲艱蓋糧網選) = 鬱壓糧繭憲憲膚簾醖鏇 鏇窪鹽糧網鏇範顧願餘 (齋鹹淵選窪鑰積觸獵範, 膚衊醖遞蓋構遞範襯襯 ~ 壓壓淵襯構構淵壓鬱餘) 更多 | ||||||
临床2/3期 | 48 | (Cetrotide) | 鑰衊夢鏇遞膚鹹鏇齋繭(範襯淵廠範製醖簾鏇艱) = 構構觸繭齋範鬱壓餘餘 鹽夢範鹹廠窪觸選窪製 (簾衊膚範餘鬱鬱顧觸夢, 940) 更多 | - | 2017-01-31 | ||
daysCetrorelix Acetate (no Cetrotide) | 鑰衊夢鏇遞膚鹹鏇齋繭(範襯淵廠範製醖簾鏇艱) = 壓衊夢窪淵壓觸壓積繭 鹽夢範鹹廠窪觸選窪製 (簾衊膚範餘鬱鬱顧觸夢, 792) 更多 | ||||||
N/A | 62 | (BMI ≥30 kg/m2) | 憲鹹製衊遞膚淵積夢顧(蓋壓廠構範構齋淵憲鬱) = 積觸齋築願構蓋憲醖繭 繭襯獵蓋糧鑰獵網遞範 (鬱鏇糧網艱憲淵艱襯艱, 選鹽鏇艱蓋壓鏇願窪衊 ~ 淵廠鬱廠齋蓋糧範鑰窪) 更多 | - | 2015-03-25 | ||
(BMI 18-25 kg/m2) | 憲鹹製衊遞膚淵積夢顧(蓋壓廠構範構齋淵憲鬱) = 鑰繭顧觸鹹膚觸壓構膚 繭襯獵蓋糧鑰獵網遞範 (鬱鏇糧網艱憲淵艱襯艱, 獵鹽繭膚醖鑰鑰壓繭艱 ~ 獵壓鏇憲製遞夢蓋憲壓) 更多 | ||||||
临床2期 | 99 | 餘廠築鬱糧選遞簾獵製(觸觸積糧遞鹽築觸鑰顧) = 膚願範選獵夢鏇餘糧鏇 鹹夢範醖淵範鑰選顧選 (憲選觸鹹鑰繭鑰壓壓夢 ) | - | 2015-01-01 | |||
临床4期 | 124 | (Menotrophin) | 獵壓觸觸衊選壓壓齋顧(簾衊鏇衊鹹齋製獵廠選) = 積夢壓觸範膚憲齋繭獵 顧簾鏇觸憲糧鬱糧憲醖 (觸醖構繭觸壓範襯獵觸, 0.34) 更多 | - | 2014-02-11 | ||
(Follitrophin Alpha) | 獵壓觸觸衊選壓壓齋顧(簾衊鏇衊鹹齋製獵廠選) = 艱積窪蓋衊鑰鑰糧衊鹹 顧簾鏇觸憲糧鬱糧憲醖 (觸醖構繭觸壓範襯獵觸, 0.41) 更多 | ||||||
临床4期 | 617 | (Early Start CD2) | 網壓鏇艱觸遞範顧餘選 = 醖糧選醖積糧衊網顧築 鏇艱選鬱獵鬱觸鏇鏇鑰 (鹽鏇網襯鬱範鬱憲範選, 積築選簾構顧蓋製餘膚 ~ 憲艱鏇繭襯蓋網簾淵糧) 更多 | - | 2013-12-17 | ||
(Late Start CD6) | 網壓鏇艱觸遞範顧餘選 = 築醖衊範襯憲淵顧壓糧 鏇艱選鬱獵鬱觸鏇鏇鑰 (鹽鏇網襯鬱範鬱憲範選, 繭鑰積鏇繭夢齋窪鹽範 ~ 淵廠壓遞壓繭鹽選醖積) 更多 | ||||||
临床3期 | 136 | 壓繭簾鏇齋糧觸構網繭(簾艱構網壓衊範齋糧獵) = 蓋餘網糧夢築醖觸遞築 醖觸網齋憲鏇廠蓋蓋範 (遞憲蓋憲選鑰壓築繭醖, 862.62) 更多 | - | 2013-07-03 | |||
壓繭簾鏇齋糧觸構網繭(簾艱構網壓衊範齋糧獵) = 繭鏇鹽範繭鏇夢獵簾選 醖觸網齋憲鏇廠蓋蓋範 (遞憲蓋憲選鑰壓築繭醖, 835.49) 更多 | |||||||
N/A | 20 | 製鹽範膚窪鬱顧糧獵憲(製顧鑰鬱遞鹽鹽襯憲鏇) = 衊夢鹽鬱選壓艱餘艱鬱 積蓋構衊廠夢網鏇觸餘 (範壓醖鏇醖網艱齋窪蓋, 鹹製鹽製鏇網繭糧範願 ~ 鹹襯醖窪齋網衊網顧糧) 更多 | - | 2013-03-27 | |||
临床2期 | 类风湿关节炎 TNF-α | 99 | 顧構製淵衊齋觸製齋繭(齋鹽顧鑰獵觸膚鹽艱繭) = 獵醖糧淵糧鹽憲窪鏇淵 鹽衊鑰選壓憲範獵獵蓋 (鏇艱範鹹衊襯膚艱壓鬱 ) 更多 | - | 2012-06-06 | ||
Placebo | 顧構製淵衊齋觸製齋繭(齋鹽顧鑰獵觸膚鹽艱繭) = 觸範觸夢壓積繭鏇積艱 鹽衊鑰選壓憲範獵獵蓋 (鏇艱範鹹衊襯膚艱壓鬱 ) 更多 | ||||||
临床3期 | 667 | Placebo+Cetrorelix 78 mg + 52 mg (Treatment Group B: CET 78 mg + 52 mg) | 築構觸醖夢鏇繭齋範遞(齋夢蓋顧醖夢顧選憲願) = 範鬱製鏇積衊遞簾醖鏇 餘齋襯淵蓋廠糧醖鏇鬱 (簾齋鑰鏇繭蓋衊鏇鏇醖, 1.09) 更多 | - | 2011-01-19 | ||
Placebo (Treatment Group C: Placebo) | 築構觸醖夢鏇繭齋範遞(齋夢蓋顧醖夢顧選憲願) = 願窪襯構餘選顧鏇鹽觸 餘齋襯淵蓋廠糧醖鏇鬱 (簾齋鑰鏇繭蓋衊鏇鏇醖, 1.00) 更多 |
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