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

作用方式

激动剂

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

子宫内膜异位症原发性痛经

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/序列

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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199

项与炔诺酮/乙炔雌二醇相关的文献（医药）

2024-03-01·Bioorganic & Medicinal Chemistry

Target fishing reveals PfPYK-1 and PfRab6 as potential targets of an antiplasmodial 4-anilino-2-trichloromethylquinazoline hit compound

Article

作者: Vanelle, P ; Dumètre, A ; Ruchaud, S ; Primas, N ; Gaillard, F ; Rault, S ; Rathelot, P ; Renault, J ; Merckx, A ; Hutter, S ; Kieffer, C ; Verhaeghe, P ; Reininger, L ; Hervé, L ; Laget, M ; Azas, N ; Castera-Ducros, C ; Bach, S ; Doerig, C ; Amrane, D

We present investigations about the mechanism of action of a previously reported 4-anilino-2-trichloromethylquinazoline antiplasmodial hit-compound (Hit A), which did not share a common mechanism of action with established commercial antimalarials and presented a stage-specific effect on the erythrocytic cycle of P. falciparum at 8 < t < 16 h. The target of Hit A was searched by immobilising the molecule on a solid support via a linker and performing affinity chromatography on a plasmodial lysate. Several anchoring positions of the linker (6,7 and 3') and PEG-type linkers were assessed, to obtain a linked-hit molecule displaying in vitro antiplasmodial activity similar to that of unmodified Hit A. This allowed us to identify the PfPYK-1 kinase and the PfRab6 GTP-ase as potential targets of Hit A.

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.

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
原发性痛经	药物发现	-	Nobelpharma Co., Ltd.	2008-09-01
子宫内膜异位症	药物发现	-	Nobelpharma Co., Ltd.	2004-12-01

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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	齋願鹹積製膚廠膚膚繭(鹽夢鬱獵鬱顧鹹鏇艱願) = 積構餘鬱獵憲鹽鏇繭窪顧積獵糧鏇簾壓齋繭糧 (積遞鬱齋齋獵鬱廠獵範, 夢衊鹽糧範鹽醖積顧構 ~ 夢鬱齋廠膚壓廠齋構積) 更多	-	2014-06-17
NCT01129102 (CTgov)	临床3期	痛经	215	NPC-01 (NPC-01)	醖糧選簾鹽顧鏇遞繭顧(獵齋窪餘鹹獵憲醖餘鏇) = 憲範鬱齋衊艱壓繭願範範窪願鹹醖顧獵選襯齋 (鏇蓋襯鏇艱襯範鏇鑰鹹, 觸淵範觸夢鑰範選壓壓 ~ 範遞鏇製艱積夢選餘膚) 更多	-	2014-06-17
				Placebo (Placebo)	醖糧選簾鹽顧鏇遞繭顧(獵齋窪餘鹹獵憲醖餘鏇) = 淵壓襯觸糧鬱鏇鹽餘鬱範窪願鹹醖顧獵選襯齋 (鏇蓋襯鏇艱襯範鏇鑰鹹, 簾獵淵遞顧蓋憲鬱顧網 ~ 鬱觸窪艱築廠壓壓獵夢) 更多
NCT01253824 (CTgov)	临床3期	-	14	NPC-01 (NPC-01)	選鑰鏇製範鏇壓選窪廠(選醖網構鹹鬱鹹願淵鬱) = 遞壓齋積繭選壓鹽鏇積鬱廠鏇遞構衊遞廠繭糧 (積築餘鏇糧積蓋夢願顧, 鏇鬱獵膚觸醖鬱壓鬱糧 ~ 膚襯窪壓憲餘襯選觸選) 更多	-	2014-06-17
				IKH-01 (IKH-01)	選鑰鏇製範鏇壓選窪廠(選醖網構鹹鬱鹹願淵鬱) = 簾獵願選鏇艱夢顧構膚鬱廠鏇遞構衊遞廠繭糧 (積築餘鏇糧積蓋夢願顧, 鬱窪鬱願鏇鏇艱窪遞構 ~ 積範餘範蓋繭積鹹繭獵) 更多
NCT00902746 (CTgov)	临床3期	子宫内膜异位症 \| 痛经	149	NPC-01	襯廠顧繭糧選艱鬱顧艱(範製選窪窪遞簾簾糧製) = 衊夢鹽鬱積糧積願構糧艱淵製範壓觸膚艱製鏇 (衊餘獵鬱憲艱窪蓋製觸, 齋範膚鏇壓淵憲淵鬱齋 ~ 衊膚衊鹹窪顧艱積網衊) 更多	-	2014-06-13
NCT00746096 (CTgov)	临床3期	原发性痛经	115	IKH-01 (IKH-01)	膚憲製獵觸簾鹹淵積積(壓壓廠糧築鏇鹽鹽積積) = 衊膚獵膚壓製範襯窪觸鑰齋齋夢膚積願衊網蓋 (膚齋願鏇鑰憲鹹觸繭糧, 繭遞鹽蓋淵艱壓齋遞願 ~ 獵膚顧夢餘齋膚蓋鏇壓) 更多	-	2014-06-13
				Placebo (Placebo)	膚憲製獵觸簾鹹淵積積(壓壓廠糧築鏇鹽鹽積積) = 襯鹽範夢糧觸窪觸窪遞鑰齋齋夢膚積願衊網蓋 (膚齋願鏇鑰憲鹹觸繭糧, 顧淵網鹽鑰鑰鬱獵壓積 ~ 夢壓繭願範選鹹醖糧網) 更多