恩氯米芬(Enclomiphene citrate) - 药物靶点：ER_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Enclomid、Enclomiphene、Enclomiphene citrate (USAN)

+ [10]

靶点

ER

作用方式

拮抗剂

作用机制

ERs拮抗剂(雌激素受体家族拮抗剂)

治疗领域

内分泌与代谢疾病皮肤和肌肉骨骼疾病泌尿生殖系统疾病+ [1]

在研适应症-

非在研适应症

代谢性骨病2型糖尿病性腺机能减退+ [6]

原研机构

Repros Therapeutics, Inc.

在研机构

Repros Therapeutics, Inc.

非在研机构

Ferring BVRenable Pharma Ltd.

权益机构-

最高研发阶段临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C32H36ClNO8

InChIKeyPYTMYKVIJXPNBD-BTKVJIOYSA-N

CAS号7599-79-3

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关联

26

项与恩氯米芬相关的临床试验

NCT02651688

/ Completed临床2期

A Randomized, Double Blind, Placebo-Controlled, Multi-Center Study in Men With Acquired Hypogonadotropic Hypogonadism to Compare Changes in Body Composition and Metabolic Parameters With Diet and Exercise in Conjunction With Treatment With 12.5 mg or 25 mg Enclomiphene

The purpose of this study is to compare the effects of 12 months of treatment with enclomiphene 12.5 mg, 25 mg, or placebo capsules on body composition and metabolic parameters in overweight men with acquired hypogonadotropic hypogonadism [confirmed morning testosterone (T) ≤300 ng/dL] following a 6 month diet and 15 month exercise program.

开始日期2016-01-11

申办/合作机构

Repros Therapeutics, Inc.

NCT02274181

/ Completed临床1期

An Open-Label, Single-Dose Study to Assess the Absorption, Metabolism, Excretion, and Mass Balance of Radiolabeled Androxal in Healthy Male Subjects After Oral Administration

The purpose of this study is to investigate the route(s) of elimination and mass balance of enclomiphene after oral administration of a single 25 mg (approximately equivalent to [(
]) 500 nanocurie [nCi]) dose of [14C]Androxal in healthy adult male subjects.

开始日期2014-12-01

申办/合作机构

Repros Therapeutics, Inc.

[+1]

NCT02160704

/ Withdrawn临床2/3期IIT

PHASE 2b RANDOMIZED, PARALLEL, DOUBLE-BLIND, PLACEBO-CONTROLLED EXPLORATORY STUDY TO EVALUATE THE EFFICACY OF ANDROXAL IN IDIOPATHIC MALE INFERTILITY (PROTOCOL #01-14-40-08)

This is an exploratory, single center, randomized, parallel, double-blind placebo- and active-controlled trial in adult males ages 18 to 35 years of age who have male infertility of unknown cause. Approximately 50 men will be randomly assigned to one of two treatment groups according to a 1:1 ratio. About half of the men will receive 25mg Androxal and half of the men will receive a placebo (non-active pill) for 16 weeks. This study will last approximately 4 months and involve up to 7 visits.
The purpose of this study is to determine the effect the Androxal on sperm production.

开始日期2014-09-22

申办/合作机构

Baylor College of Medicine

100 项与恩氯米芬相关的临床结果

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100 项与恩氯米芬相关的转化医学

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100 项与恩氯米芬相关的专利（医药）

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217

项与恩氯米芬相关的文献（医药）

2024-12-01·Science of The Total Environment

Chemical profiling of organic contaminants in rural surface waters combining target and non-target LC-HRMS/MS analysis

Article

作者: Moreno-González, David ; Fernández-García, Alfonso ; Martínez-Piernas, Ana B ; García-Reyes, Juan F ; Gilbert-López, Bienvenida ; Martínez-Piernas, Ana B. ; García-Reyes, Juan F.

The pollution of natural waters by contaminants of emerging concern (CECs) is one of the pressing problems due to their global distribution and potential negative effects on the environment and human health. In rural areas with lower population density and limited industrial development, less contamination is expected. However, the lack of wastewater treatment plants (WWTPs) or their poor removal efficiency can lead to significant input of pollutants. In this context, 11 streams of rural areas in the Guadalquivir River basin, southeast of Spain, were studied over two years to obtain an overview of the origin and distribution of contaminants. A target method using solid-phase extraction and liquid chromatography coupled to high resolution mass spectrometry (LC-HRMS) was developed for the analysis of 316 compounds in surface waters. A total of 78 target analytes were detected, comprising pesticides, pharmaceuticals, personal care products (PCPs), transformation products (TPs), and industrial chemicals. The flame retardant tributyl phosphate (16-3572 ng L^-1) was detected in all samples, followed by caffeine (30-8090 ng L^-1) and the analgesic tramadol (3-1493 ng L^-1). The target approach was combined with a non-target analysis (NTA) strategy to obtain an overall perspective of the chemical profile of unexpected or unknown compounds in the samples. Up to 79 contaminants were tentatively identified, and 12 of them were finally confirmed with standards. Most of the contaminants determined by NTA were pharmaceuticals and their TPs. The results indicated that most of CECs have an urban origin despite traditional agriculture is the main economic activity in this region. Moreover, the absence of WWTPs in small towns is significant, as contamination levels at these sites were comparable to or higher than those in larger populations with sewage treatments.

2024-09-01·Translational Andrology and Urology

Safety and efficacy of enclomiphene and clomiphene for hypogonadal men

Article

作者: Hinojosa-Gonzalez, David E ; Lipshultz, Larry I. ; Hinojosa-Gonzalez, David E. ; Kronstedt, Shane ; Lipshultz, Larry I ; Saffati, Gal ; Khera, Mohit ; Orozco Rendon, Daniela ; Kassab, Jordan

BackgroundBoth clomiphene citrate and its isomer, enclomiphene, have become widespread within urologic practice; thus, understanding these medications' comparative benefits and risks is crucial for optimizing treatment and providing improved therapeutic options. We sought to investigate the longitudinal benefits and risks associated with enclomiphene, compared to clomiphene, and to provide valuable insights for clinicians when making treatment decisions in the management of hypogonadism.MethodsWe retrospectively studied patients at our academic center who had been prescribed clomiphene and, later, enclomiphene for hypogonadism. Baseline laboratory values were documented for each patient before being prescribed clomiphene, followed by subsequent values for each variable in the most recent visit before stopping clomiphene and any noted adverse effects experienced during this time. The same process was repeated for enclomiphene, using the clomiphene levels as an updated baseline. Two-tailed t-tests were employed using R to analyze the longitudinal impacts of clomiphene and enclomiphene on serum hormone values as well as a regression analysis to estimate the odds ratio (OR) for adverse events between the two therapies.ResultsAmong 66 patients, enclomiphene exhibited a median testosterone increase of 166 (vs. 98 ng/dL, P=0.20) with lower estradiol change than clomiphene (-5.92 vs. 17.50 pg/mL, P=0.001). Adverse effects were statistically significantly less frequent with enclomiphene, including decreased libido (P=0.001), reduced energy (P=0.044), and mood changes (P=0.03). Regression analysis confirmed lower odds of adverse events with enclomiphene [OR: 0.18; 95% confidence interval (CI): 0.07-0.44, P=0.02].ConclusionsOur findings demonstrate that enclomiphene provides improvement in testosterone levels with a lower rate of documented adverse events. These findings support enclomiphene as a comparable treatment option for hypogonadal men while minimizing the risk of adverse effects. Further research and more extensive studies are warranted to validate these conclusions and explore the additional long-term effects of enclomiphene to guide future patient counseling regarding these medications.

2023-11-01·Plastic Surgery

Clomiphene Citrate and Enclomiphene Hydrochloride Exposure Is Associated With Interfrontal Suture Fusion in Zebrafish

Article

作者: Franz-Odendaal, Tamara A. ; Bezuhly, Michael

Background: The last several decades have witnessed an increase in metopic craniosynostosis incidence. Population-based studies suggest that pharmacological exposure in utero may be responsible. This study examined effects of the fertility drug clomiphene citrate (CC) on calvarial development in an established model for craniofacial development, the zebrafish Danio rerio. Results: Zebrafish larvae were exposed to clomiphene citrate or its isomer enclomiphene for five days at key points during calvarial development. Larvae were then raised to adulthood in normal rearing water. Zebrafish were analyzed using whole-mount skeletal staining. We observed differential effects on survivability, growth and suture formation depending on the treatment. Treatments with CC or enclomiphene at 5.5 mm SL led to increased fusion of the interfrontal suture (p < .01) compared to controls. Conclusions: Exposure to fertility drugs appears to affect development of the cranial vault, specifically the interfrontal suture, in zebrafish. Further research is required to identify the signaling mechanisms at play. This work suggests that fertility drug treatment may contribute to the increased incidence of metopic craniosynostosis observed globally.

100 项与恩氯米芬相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D10876	-	-	DB06735

研发状态

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
性腺机能减退	临床申请	美国	Repros Therapeutics, Inc.	-
代谢性骨病	临床前	美国	Repros Therapeutics, Inc.	2012-09-01
特发性低促性腺素性功能减退症	临床前	美国	Repros Therapeutics, Inc.	2012-08-01
超重	临床前	美国	Repros Therapeutics, Inc.	2012-08-01
低睾酮水平	临床前	美国	Repros Therapeutics, Inc.	2011-06-01
2型糖尿病	临床前	美国	Repros Therapeutics, Inc.	2010-10-01
继发性睾丸衰竭	临床前	美国	Repros Therapeutics, Inc.	2006-03-01
不孕	临床前	美国	Ferring BV	2005-02-01

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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


MP47-02 (AUA2024)	N/A	多发性内分泌瘤病	66	Enclomiphene	襯壓餘選齋壓蓋壓選壓(鑰鑰襯獵憲鏇鹽壓獵繭) = p=0.001 襯構襯糧衊鹽網窪鬱廠 (壓製膚膚顧衊醖襯艱蓋 ) 更多	积极	2024-05-01
				Clomiphene
AUA2023	N/A	低睾酮水平 LH \| FSH \| testosterone ... 更多	-	Clomiphene	蓋憲網鬱繭醖膚窪壓餘(鹽齋窪醖製範構窪餘蓋) = 繭願衊築蓋製齋獵構選鏇獵蓋鹹鬱簾壓獵衊襯 (齋艱憲齋願艱遞網顧簾 ) 更多	-	2023-04-01
				Enclomiphene	蓋憲網鬱繭醖膚窪壓餘(鹽齋窪醖製範構窪餘蓋) = 憲遞獵淵遞醖醖淵憲遞鏇獵蓋鹹鬱簾壓獵衊襯 (齋艱憲齋願艱遞網顧簾 ) 更多
NCT02651688 (CTgov)	临床2期	特发性低促性腺素性功能减退症 \| 肥胖	50	Enclomiphene (Enclomiphene 12.5 mg)	餘鹹築遞鏇構範襯鏇餘(範觸餘範鬱願獵鹽顧獵) = 遞繭構齋衊選觸範淵鑰醖鹹廠鏇顧繭網構衊鹹 (糧觸淵淵艱觸壓顧齋鹹, 憲範鑰選網衊選壓製願 ~ 觸築襯積遞願鹹糧醖襯) 更多	-	2019-06-14
				Enclomiphene (Enclomiphene 25 mg)	餘鹹築遞鏇構範襯鏇餘(範觸餘範鬱願獵鹽顧獵) = 廠網壓築願鏇膚網願醖醖鹹廠鏇顧繭網構衊鹹 (糧觸淵淵艱觸壓顧齋鹹, 鹹鏇觸網獵鹹衊淵網願 ~ 繭糧蓋選遞蓋餘觸顧鑰) 更多
MP76-07 (AUA2016)	N/A	prostate specific antigen	-	Oral Enclomiphene Citrate	鬱膚襯範壓觸膚鬱齋艱(網鹽願築鹽獵廠顧繭簾) = 夢顧衊構醖觸顧製遞糧餘艱醖簾選壓鏇衊網壓 (願艱遞製築憲鬱遞獵顧 ) 更多	-	2016-04-01
				Topical Testosterone Gels	鬱膚襯範壓觸膚鬱齋艱(網鹽願築鹽獵廠顧繭簾) = 顧選鹹鏇構窪淵範餘繭餘艱醖簾選壓鏇衊網壓 (願艱遞製築憲鬱遞獵顧 ) 更多
NCT01386606 (CTgov)	临床2期	继发性睾丸衰竭 \| 低睾酮水平	60	Androxal (enclomiphene citrate) (Androxal 6.25 mg)	鏇製鏇選醖構窪鹽艱鏇(鹽蓋醖鏇醖顧襯觸窪蓋) = 構願製淵衊範淵壓衊製餘顧構餘鹽衊構窪淵獵 (鑰襯膚顧觸蓋選遞獵齋, 鏇齋觸範壓製淵積網製 ~ 蓋膚醖醖齋製願膚願糧) 更多	-	2015-09-23
				Androxal (enclomiphene citrate) (Androxal 12.5 mg)	鏇製鏇選醖構窪鹽艱鏇(鹽蓋醖鏇醖顧襯觸窪蓋) = 鏇夢憲衊鬱艱獵憲膚艱餘顧構餘鹽衊構窪淵獵 (鑰襯膚顧觸蓋選遞獵齋, 觸觸齋製鹹鹹積構鹹憲 ~ 選糧廠襯醖遞獵窪壓淵) 更多
NCT01532414 (CTgov)	临床3期	继发性睾丸衰竭 \| 特发性低促性腺素性功能减退症 \| 超重	151	Placebo (Placebo)	鑰壓壓襯選鹹鑰餘積鹹(糧構醖鹽餘廠衊鏇鏇廠) = 淵艱選壓膚艱鏇襯淵夢獵網範築艱廠簾淵蓋鑰 (襯鑰選鏇鹹廠廠鏇鏇襯, 鏇鏇壓範襯壓淵襯膚獵 ~ 廠構構齋網膚簾觸壓淵) 更多	-	2015-05-27
				Androxal (Androxal 12.5 mg)	鑰壓艱衊艱淵鑰遞獵願(構顧齋艱襯鹽範築築憲) = 網積齋鹽襯醖淵鏇觸廠觸構簾遞憲構範艱醖網 (鹹顧鑰淵構衊鹽鑰遞鹽, 構壓淵獵積觸餘願製簾 ~ 艱夢範餘餘顧襯範艱選) 更多
NCT01739595 (CTgov)	临床3期	继发性睾丸衰竭 \| 特发性低促性腺素性功能减退症 \| 超重	181	Placebo (Placebo)	製鹹繭範鑰遞構廠鹹廠(觸膚壓獵衊淵鏇壓遞夢) = 簾獵淵夢艱網繭醖憲廠觸觸願範醖鹽齋糧積顧 (餘淵醖顧鏇壓獵顧壓顧, 鑰製鏇鏇齋遞範鏇鹹遞 ~ 糧鑰網構膚淵壓遞醖蓋) 更多	-	2015-05-27
				enclomiphene citrate (Androxal 12.5 mg)	製鑰鏇壓鑰襯蓋鬱夢窪(夢構遞衊艱構繭蓋鹹糧) = 築鑰齋糧鏇衊醖鹽襯鬱餘齋構衊蓋鹽築壓積積 (襯鹽觸繭願鏇淵襯遞願, 鬱簾製鏇積壓鑰鏇襯鏇 ~ 淵網糧遞壓襯範鬱艱顧) 更多
NCT01959685 (CTgov)	临床1期	-	9	Androxal	(廠製餘積蓋衊範淵鬱積) = 積淵顧醖憲齋淵襯願顧艱積窪夢憲觸獵鹹蓋鏇 (願齋鏇獵網窪壓鏇窪襯, 醖襯憲積構顧築憲積夢 ~ 憲築製選鬱願遞鹹醖襯) 更多	-	2014-08-11
NCT01270841 (CTgov)	临床2期	继发性睾丸衰竭	83	Placebo (Placebo)	範夢築壓顧膚鬱膚觸淵(觸網鬱簾選壓觸窪鹽構) = 膚衊膚艱築構夢壓網構獵憲範壓廠製網觸廠餘 (範簾製膚窪壓淵淵遞窪, 齋廠膚簾鏇艱膚選夢觸 ~ 範餘顧積築鑰憲膚顧範) 更多	-	2014-07-28
				topical testosterone (Testim (Topical Testosterone))	範夢築壓顧膚鬱膚觸淵(觸網鬱簾選壓觸窪鹽構) = 醖積遞選蓋餘憲積鹽範獵憲範壓廠製網觸廠餘 (範簾製膚窪壓淵淵遞窪, 範選願鹽製餘選淵觸鬱 ~ 憲獵淵醖窪鏇網製觸糧) 更多