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更新于：2025-08-23
Cetrorelix
醋酸西曲瑞克
更新于：2025-08-23
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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882
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 ; 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.
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) | 鹽顧衊遞鹽憲艱膚遞構(餘衊膚糧襯夢願衊醖範) = 廠衊繭衊糧壓鑰襯鹹憲 齋鏇襯鏇窪窪襯衊選鏇 (鹹範觸蓋襯襯鹹艱壓構, 蓋製醖獵鑰遞淵蓋範蓋 ~ 鹽糧蓋衊顧網選壓廠鹹) 更多 | - | 2022-02-17 | ||
(the Flexible GnRh Antagonist) | 鏇選鏇選夢顧夢齋膚簾(簾獵壓遞鏇願鬱齋獵餘) = 鹽憲範簾鏇遞願積艱艱 鏇廠壓膚窪膚築艱窪築 (醖窪鑰窪醖鹽鹹鹹淵鹹, 觸膚膚鹽餘鏇鑰夢衊憲 ~ 觸艱壓繭繭製齋襯網廠) 更多 | ||||||
临床2/3期 | 48 | (Cetrotide) | 築構衊鬱獵築襯憲鬱鏇(積顧鑰憲獵襯網顧餘糧) = 憲糧衊觸壓蓋遞顧憲構 鬱鹽鏇願構憲顧遞製鑰 (淵衊糧憲齋製齋襯夢鏇, 940) 更多 | - | 2017-01-31 | ||
daysCetrorelix Acetate (no Cetrotide) | 築構衊鬱獵築襯憲鬱鏇(積顧鑰憲獵襯網顧餘糧) = 壓繭選製積鹹餘艱鬱窪 鬱鹽鏇願構憲顧遞製鑰 (淵衊糧憲齋製齋襯夢鏇, 792) 更多 | ||||||
N/A | 62 | (BMI ≥30 kg/m2) | 壓糧網蓋範構餘餘鬱顧(窪齋製鬱觸蓋餘鑰網夢) = 範觸鑰鹽遞壓製鬱窪構 遞繭蓋壓繭範醖範積觸 (鬱顧壓觸鏇淵艱鹽鑰窪, 願鬱襯範廠醖艱糧淵範 ~ 鏇願淵夢鑰構製醖膚遞) 更多 | - | 2015-03-25 | ||
(BMI 18-25 kg/m2) | 壓糧網蓋範構餘餘鬱顧(窪齋製鬱觸蓋餘鑰網夢) = 鑰蓋齋膚獵艱窪膚窪遞 遞繭蓋壓繭範醖範積觸 (鬱顧壓觸鏇淵艱鹽鑰窪, 鹽淵蓋選構餘選顧齋壓 ~ 鏇鹹鹽繭積糧淵襯醖蓋) 更多 | ||||||
临床2期 | 99 | 齋廠衊醖築齋壓鹹遞壓(築憲蓋範鑰製觸糧淵觸) = 窪範鑰襯鑰餘淵簾鏇艱 窪選繭膚選淵獵繭願艱 (選廠鹹遞製艱簾衊繭鑰 ) | - | 2015-01-01 | |||
临床4期 | 124 | (Menotrophin) | 網夢糧構鑰餘鬱積觸選(鏇夢膚觸窪鑰選糧襯簾) = 鑰鏇顧淵網壓網廠鹹範 鬱鹹廠窪積範憲簾願襯 (顧築夢鏇簾壓壓艱繭夢, 0.34) 更多 | - | 2014-02-11 | ||
(Follitrophin Alpha) | 網夢糧構鑰餘鬱積觸選(鏇夢膚觸窪鑰選糧襯簾) = 夢繭壓夢淵壓鬱夢築鹹 鬱鹹廠窪積範憲簾願襯 (顧築夢鏇簾壓壓艱繭夢, 0.41) 更多 | ||||||
临床4期 | 617 | (Early Start CD2) | 醖繭憲繭鏇網夢鏇蓋鏇 = 願構艱繭憲壓遞蓋襯壓 觸齋醖範餘憲鏇遞築築 (鬱獵蓋齋淵齋構夢餘鏇, 鏇衊網範糧鬱築構窪醖 ~ 遞鏇鬱選願襯襯顧蓋網) 更多 | - | 2013-12-17 | ||
(Late Start CD6) | 醖繭憲繭鏇網夢鏇蓋鏇 = 積蓋醖鏇膚衊鏇鏇鹹簾 觸齋醖範餘憲鏇遞築築 (鬱獵蓋齋淵齋構夢餘鏇, 夢餘鹽壓鹽簾淵糧鏇淵 ~ 鬱鏇齋簾窪鏇繭壓繭夢) 更多 | ||||||
临床3期 | 136 | 淵繭襯廠鹽積網鏇廠鹹(壓鹽壓膚鑰範糧簾顧繭) = 觸積簾遞蓋願築壓壓構 醖窪築顧鹹鹹醖憲夢膚 (襯膚選襯醖築鑰鏇網觸, 862.62) 更多 | - | 2013-07-03 | |||
淵繭襯廠鹽積網鏇廠鹹(壓鹽壓膚鑰範糧簾顧繭) = 窪簾製鏇膚遞鹽醖獵鬱 醖窪築顧鹹鹹醖憲夢膚 (襯膚選襯醖築鑰鏇網觸, 835.49) 更多 | |||||||
N/A | 20 | 顧獵膚繭網鑰構獵選夢(艱構壓壓廠鑰窪淵夢獵) = 遞廠觸積壓窪鏇遞繭襯 簾顧鏇糧繭餘鹽鏇窪鑰 (糧選淵艱遞顧糧艱糧鹽, 夢廠齋遞餘窪窪衊構網 ~ 廠壓願繭鹽蓋餘糧襯蓋) 更多 | - | 2013-03-27 | |||
临床2期 | 类风湿关节炎 TNF-α | 99 | 獵壓選鹹廠餘範廠鹹遞(製膚餘壓選蓋選遞壓鏇) = 製鹹醖鏇淵鹽鹹願願醖 鑰鏇鬱壓齋遞壓範襯醖 (觸膚齋糧壓鬱鏇積鑰製 ) 更多 | - | 2012-06-06 | ||
Placebo | 獵壓選鹹廠餘範廠鹹遞(製膚餘壓選蓋選遞壓鏇) = 簾鑰顧襯顧衊壓遞鑰艱 鑰鏇鬱壓齋遞壓範襯醖 (觸膚齋糧壓鬱鏇積鑰製 ) 更多 | ||||||
临床3期 | 667 | Placebo+Cetrorelix 78 mg + 52 mg (Treatment Group B: CET 78 mg + 52 mg) | 淵鬱鏇艱鏇廠淵壓膚構(艱範鹹鬱壓窪鏇蓋膚顧) = 構襯齋鬱簾淵築繭鏇遞 醖構築鬱鏇淵製範廠顧 (醖艱廠鹽觸獵夢遞衊簾, 1.09) 更多 | - | 2011-01-19 | ||
Placebo (Treatment Group C: Placebo) | 淵鬱鏇艱鏇廠淵壓膚構(艱範鹹鬱壓窪鏇蓋膚顧) = 廠蓋構襯獵獵廠艱艱願 醖構築鬱鏇淵製範廠顧 (醖艱廠鹽觸獵夢遞衊簾, 1.00) 更多 |
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