炔诺酮/乙炔雌二醇(Norethisterone/Ethinyl estradiol) - 药物靶点：ER x PR_在研适应症：痛经，避孕_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Norethisterone/Ethinylestradiol

+ [5]

靶点

ER x PR

作用机制

ERs激动剂(雌激素受体家族激动剂)、PR激动剂(孕激素受体激动剂)

治疗领域

神经系统疾病其他疾病

在研适应症

痛经避孕

非在研适应症

子宫内膜异位症

原研机构

Daiichi Seiyaku Co., Ltd.Syntex Corp.

在研机构

Nobelpharma Co., Ltd.

Kaken Pharmaceutical Co., Ltd.

非在研机构-

最高研发阶段批准上市

首次获批日期

日本 (1999-06-16),

避孕

最高研发阶段(中国)-

特殊审评-

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结构

分子式C40H50O4

InChIKeyNAPPWIFDUAHTRY-XYDRQXHOSA-N

CAS号37270-71-6

关联

12

项与炔诺酮/乙炔雌二醇相关的临床试验

NCT02103569 / Completed临床1期

Effect of a Combination of Daclatasvir, Asunaprevir, and BMS-791325 on the Pharmacokinetics of a Combined Oral Contraceptive Containing Ethinyl Estradiol and Norethindrone Acetate in Healthy Female Subjects

The purpose of this study is to assess the effect of DCV/ASV/BMS-791325 fixed dose combination (FDC) + 75mg BMS-791325 on the Pharmacokinetics (PK) of the oral contraceptive agent.

开始日期2014-04-01

申办/合作机构

Bristol Myers Squibb Co.

NCT01253824 / Completed临床3期

Pharmacodynamics of NPC-01( 1mg Norethisterone and 0.02mg Ethinyl Estradiol) and IKH-01( 1mg Norethisterone and 0.035mg Ethinyl Estradiol); Effect of NPC-01 and IKH-01 on Serum Concentrations of Estradiol, Progesterone, FSH and LH.

The purpose of this study is to compare the serum levels of estradiol, progesterone, FSH and LH in NPC-01 or IKH-01 one treatment cycle with those in before and after administration cycle.

开始日期2011-01-01

申办/合作机构

Nobelpharma Co., Ltd.

NCT01246791 / Completed临床3期

A Single Dose Pharmacokinetics Study of NPC-01 (1mg Norethisterone and 0.02mg Ethynyl Estradiol) in Healthy Female Volunteers

The purpose of this study is to assess the pharmacokinetic profiles of norethisterone and ethinyl estradiol after single oral administration of NPC-01 in healthy female volunteers.
Pharmacokinetics of norethisterone and ethinyl estradiol will be evaluated on the basis of AUC, Cmax, tmax, t1/2, MRT, kel and AUC∞.

开始日期2010-11-01

申办/合作机构

Nobelpharma Co., Ltd.

100 项与炔诺酮/乙炔雌二醇相关的临床结果

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100 项与炔诺酮/乙炔雌二醇相关的转化医学

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100 项与炔诺酮/乙炔雌二醇相关的专利（医药）

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3

项与炔诺酮/乙炔雌二醇相关的文献（医药）

2018-06-01·Xi bao yu fen zi mian yi xue za zhi = Chinese journal of cellular and molecular immunology

[NSD3 suppresses LPS-triggered TNF-α production via promoting the dimethylation of histone H3K36 in macrophages].

Article

作者: Liu, Zhaolong ; Sun, Yanxiang ; Yang, Le ; Cheng, Qijiang

Objective To investigate the role of nuclear receptor-binding SET domain protein 3 (NSD3) in lipopolysaccharide (LPS)-triggered tumor necrosis factor α (TNF-α) production in macrophages and the underlying epigenetic mechanism. Methods The experiment used murine peritoneal macrophages and RAW264.7 cells as cell models. The mRNA and protein level of NSD3 were detected by real-time quantitative PCR and Western blot analysis in mouse peritoneal macrophages stimulated with LPS (100 ng/mL). ELISA was used to detect the production of TNF-α in NSD3-overexpressing RAW264.7 cells or NSD3-silencing peritoneal macrophages. Western blot analysis was performed to test the activation of LPS-triggered NF-κBp65 in NSD3-silencing macrophages. Luciferase assay was used to assess NF-κBp65-mediated transcriptional activation of TNF-α gene. ChIP assay was used to detect the recruitment of H3K36 methylation to TNF-α gene promoter. Results LPS inhibited the expression of NSD3 in the macrophages. Over-expression of NSD3 suppressed LPS-triggered TNF-α production, and silencing NSD3 promoted LPS-triggered TNF-α production. However, NSD3 had no effect on the activation of LPS-triggered NF-κBp65. NSD3 enhanced NF-κBp65-mediated transcriptional activation of TNF-α gene. NSD3 enhanced the dimethylation of H3K36 of TNF-α gene promoter. Conclusion NSD3 can promote the dimethylation of H3K36 of TNF-α gene promoter and suppress TNF-α transcription and production.

2016-12-01·Fertility and Sterility2区 · 医学

Evaluation of an ultra-low-dose oral contraceptive for dysmenorrhea: a placebo-controlled, double-blind, randomized trial

2区 · 医学

Article

作者: Momoeda, Mikio ; Harada, Tasuku

OBJECTIVETo evaluate the efficacy and safety of an ultra-low-dose oral contraceptive (NPC-01; 0.02 mg ethinyl estradiol and 1 mg norethisterone) in subjects with dysmenorrhea.DESIGNPlacebo-controlled, double-blind, randomized trial.SETTINGClinical trial sites.PATIENT(S)Two hundred fifteen subjects with dysmenorrhea.INTERVENTION(S)Subjects were randomly assigned to receive NPC-01, placebo, or IKH-01 (0.035 mg ethinyl estradiol and 1 mg norethisterone) for four cycles.MAIN OUTCOME MEASURE(S)Total dysmenorrhea score (verbal rating scale) assessing pain on the basis of limited ability to work and need for analgesics.RESULT(S)The reductions of total dysmenorrhea score and visual analog scale score after the treatment were significantly higher in the NPC-01 group than in the placebo group. Furthermore, the efficacy of NPC-01 was comparable to that of IKH-01. The overall incidence of side effects was significantly higher in the NPC-01 group than in the placebo group. All side effects that occurred in the NPC-01 group were previously reported in patients receiving IKH-01. No serious side effects occurred.CONCLUSION(S)The ultra-low-dose contraceptive NPC-01 relieved dysmenorrhea as effectively as IKH-01. Thus, NPC-01 could represent a new option for long-term treatment of dysmenorrhea.CLINICAL TRIAL IDENTIFICATION NUMBERNCT01129102.

2011-05-01·Fertility and Sterility2区 · 医学

Evaluation of a low-dose oral contraceptive pill for primary dysmenorrhea: a placebo-controlled, double-blind, randomized trial

2区 · 医学

Article

作者: Yuji Taketani ; Tasuku Harada ; Naoki Terakawa ; Mikio Momoeda ; Hiroshi Hoshiai

OBJECTIVETo evaluate the efficacy and safety of low-dose oral contraceptives (IKH-01; 0.035 mg ethinyl estradiol and 1 mg norethisterone) for patients with primary dysmenorrhea.DESIGNPlacebo-controlled, double-blind, randomized trial.SETTINGClinical trial sites in Japan.PATIENT(S)One hundred fifteen patients with primary dysmenorrhea.INTERVENTION(S)Patients randomly assigned to receive IKH-01 or placebo for four cycles.MAIN OUTCOME MEASURE(S)Total dysmenorrhea score, verbal rating scale defining pain according to limited ability to work and need for analgesics, and visual analog scale (VAS).RESULT(S)Reduction in total dysmenorrhea score and VAS before and after treatment was significantly higher in the IKH-01 group than in the placebo group. Total dysmenorrhea score and VAS in the IKH-01 group significantly decreased from cycles 2 to 5. Overall incidence of adverse events was significantly higher in the IKH-01 group. Incidence decreased over time in the IKH-01 group; it was invariable in the placebo group. No serious adverse events occurred.CONCLUSION(S)IKH-01 could be used as a single agent or in combination with analgesics for treatment of primary dysmenorrhea.

100 项与炔诺酮/乙炔雌二醇相关的药物交易

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研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
痛经	日本	Nobelpharma Co., Ltd.	2008-04-16
避孕	日本	Kaken Pharmaceutical Co., Ltd.	1999-06-16

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
痛经	药物发现	-	Nobelpharma Co., Ltd.	2009-05-01
子宫内膜异位症	药物发现	-	Nobelpharma Co., Ltd.	2009-05-01

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT01246791 (CTgov)	临床3期	-	12	NPC-01	願醖憲窪繭壓餘餘鬱網(餘糧夢窪襯窪膚鹽鬱膚) = 鏇簾餘艱夢鏇蓋窪齋鹽鏇構願願範願鏇選醖觸 (願壓艱鬱鏇襯襯觸簾簾, 蓋壓鏇築夢襯窪範壓襯 ~ 夢鑰淵壓鏇製醖淵鹽淵) 更多	-	2014-06-17
NCT01129102 (CTgov)	临床3期	痛经	215	NPC-01 (NPC-01)	顧鹽蓋顧選積糧蓋衊築(餘遞壓齋膚願願網範構) = 憲鏇網獵廠網鹽鹽襯蓋餘繭觸窪構鑰願廠醖積 (顧鏇壓構廠壓夢積繭淵, 廠簾網顧襯廠淵襯膚壓 ~ 鑰範廠艱憲遞衊窪衊願) 更多	-	2014-06-17
				Placebo (Placebo)	顧鹽蓋顧選積糧蓋衊築(餘遞壓齋膚願願網範構) = 鏇齋糧鏇鹹鹹繭夢蓋範餘繭觸窪構鑰願廠醖積 (顧鏇壓構廠壓夢積繭淵, 淵醖齋選觸廠糧鹹鏇鹹 ~ 鹽淵範繭壓夢網餘醖壓) 更多
NCT01253824 (CTgov)	临床3期	-	14	NPC-01 (NPC-01)	齋獵範繭鹹淵構衊獵鏇(壓糧願膚鹽顧網選膚鏇) = 獵繭窪積夢窪選範艱淵製餘築憲獵廠夢鹽襯餘 (願醖積餘遞範鏇齋艱艱, 範憲簾簾醖觸壓願齋鹹 ~ 築廠鬱鑰廠衊齋淵醖願) 更多	-	2014-06-17
				IKH-01 (IKH-01)	齋獵範繭鹹淵構衊獵鏇(壓糧願膚鹽顧網選膚鏇) = 遞餘願製襯獵憲醖襯窪製餘築憲獵廠夢鹽襯餘 (願醖積餘遞範鏇齋艱艱, 衊鹹獵蓋範網艱鹹積廠 ~ 鏇廠鏇壓窪築夢範網淵) 更多
NCT00902746 (CTgov)	临床3期	子宫内膜异位症 \| 痛经	149	NPC-01	繭膚鏇選製醖鹹襯觸構(繭鑰壓襯鬱襯繭鏇獵齋) = 窪襯艱積淵齋膚餘鹽鏇鏇膚獵膚鏇廠構衊選願 (餘膚壓網構襯廠積壓壓, 選觸觸糧餘選衊齋淵遞 ~ 製淵積壓廠齋製鹽衊衊) 更多	-	2014-06-13
NCT00746096 (CTgov)	临床3期	原发性痛经	115	IKH-01 (IKH-01)	鬱膚鬱簾憲糧憲鏇夢艱(構顧襯構築衊鹹鹹構鹽) = 網餘構鹽壓鹹齋憲範淵蓋製膚鹽鑰遞獵繭獵製 (簾壓淵襯廠夢積夢範襯, 齋鑰築遞鬱餘選繭構鹹 ~ 鹹齋醖淵艱製餘齋觸觸) 更多	-	2014-06-13
				Placebo (Placebo)	鬱膚鬱簾憲糧憲鏇夢艱(構顧襯構築衊鹹鹹構鹽) = 襯築淵鏇鬱願齋鹹選築蓋製膚鹽鑰遞獵繭獵製 (簾壓淵襯廠夢積夢範襯, 夢選選淵簾窪築鏇鬱遞 ~ 憲鹽積憲艱獵鹹壓遞糧) 更多