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+ [5]

原研机构

Repros Therapeutics, Inc.

在研机构

Repros Therapeutics, Inc.

非在研机构

Renable Pharma Ltd.Ferring BV

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

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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96

项与恩氯米芬相关的文献（医药）

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 ; Khera, Mohit ; Lipshultz, Larry I ; Saffati, Gal ; 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.

2023-09-01·Andrology

Selective modulation of estrogen receptor in obese men with androgen deficiency: A systematic review and meta‐analysis

Review

作者: Tienforti, Daniele ; Muselli, Mario ; Totaro, Maria ; Dalmazio, Gilda ; Di Giulio, Francesca ; Corona, Giovanni ; Baroni, Marco Giorgio ; Castellini, Chiara ; Spagnolo, Luca ; Barbonetti, Arcangelo

AbstractBackgroundAlthough selective estrogen receptor modulators have been proposed as a treatment for men with central functional hypogonadism, only a few data have been produced in men with obesity‐related functional androgen deficiency.ObjectiveTo determine whether and to what extent selective estrogen receptor modulators are an effective and safe therapy in men with obesity‐related functional androgen deficiency.Materials and methodsA thorough search of PubMed, Web of Science, Scopus, and Cochrane Library databases was performed to identify studies comparing testosterone levels before and after treatment. Mean differences with 95% coefficient intervals were combined using random effects models. Funnel plot, Egger's test, and trim‐and‐fill analysis were used to assess publication bias.ResultsSeven studies met the inclusion criteria providing information on 292 men with obesity‐related functional androgen deficiency treated with clomiphene citrate (12.5–50 mg daily) or enclomiphene citrate (12.5–25 mg daily) for 1.5–4 months. The pooled estimates indicated a significant increase in testosterone levels both with clomiphene (mean difference: 11.56 nmol/L; 95% coefficient interval: 9.68, 13.43; I2 = 69%, pfor heterogeneity = 0.01) and enclomiphene citrate (mean difference: 7.50 nmol/L; 95% coefficient interval: 6.52, 8.48; I2 = 4%, pfor heterogeneity = 0.37). After the exclusion of one study on severely obese men, who exhibited the highest response rate to clomiphene citrate, the heterogeneity disappeared (mean difference: 10.27 nmol/L; 95% coefficient interval: 9.39, 11.16; I2 = 0%, pfor heterogeneity = 0.66). No publication bias was revealed by Egger's test and trim‐and‐fill analysis. No treatment‐related unexpected findings regarding safety profile were registered.Discussion and conclusionTreatment with clomiphene citrate and enclomiphene citrate may be an effective and safe alternative to testosterone replacement therapy in men with obesity‐related functional androgen deficiency. Further long‐term studies are warranted to define clinical reflections of the selective estrogen receptor modulators‐induced increase in testosterone levels and to better clarify the safety profile.

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.	-
肥胖	临床前	美国	Repros Therapeutics, Inc.	2016-01-11
特发性低促性腺素性功能减退症	临床前	美国	Repros Therapeutics, Inc.	2014-01-01
代谢性骨病	临床前	美国	Repros Therapeutics, Inc.	2012-09-01
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	齋廠選遞襯繭獵構夢築(積遞壓觸醖蓋淵蓋鏇顧) = p=0.001 積鏇壓艱積鏇窪鹹壓餘 (顧艱觸窪製鏇鑰壓窪蓋 ) 更多	积极	2024-05-01
				Clomiphene
AUA2023	N/A	低睾酮水平	-	Clomiphene	蓋艱艱窪獵廠餘顧窪衊(鏇糧範遞網衊夢齋鹹憲) = 鏇築築範網範艱廠壓憲鹽夢艱積鑰夢窪鏇廠齋 (獵製壓餘蓋餘願廠鬱顧 ) 更多	-	2023-04-01
				Enclomiphene	蓋艱艱窪獵廠餘顧窪衊(鏇糧範遞網衊夢齋鹹憲) = 襯遞糧窪醖鹽淵憲衊鹹鹽夢艱積鑰夢窪鏇廠齋 (獵製壓餘蓋餘願廠鬱顧 ) 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)	網製膚繭顧蓋鑰觸築鑰(艱遞齋蓋鹽衊鹽選顧淵) = 餘網簾網壓夢壓網鹽製衊範壓製簾憲願憲艱製 (築獵鏇蓋簾餘願窪築鑰, 觸簾窪鏇觸鏇壓淵鹽網 ~ 艱糧觸襯衊顧獵夢範選) 更多	-	2019-06-14
				Enclomiphene (Enclomiphene 25 mg)	網製膚繭顧蓋鑰觸築鑰(艱遞齋蓋鹽衊鹽選顧淵) = 範廠廠鹽獵觸醖簾製廠衊範壓製簾憲願憲艱製 (築獵鏇蓋簾餘願窪築鑰, 糧製製簾獵鬱積遞製壓 ~ 夢簾觸鬱積遞鹹選繭蓋) 更多
MP76-07 (AUA2016)	N/A	-	-	Oral Enclomiphene Citrate	廠選衊範餘鏇簾壓蓋憲(艱選壓齋築鹽艱積鹽鑰) = 齋網壓範觸齋窪觸願築醖壓醖廠構繭簾餘遞壓 (膚觸鏇憲淵壓顧餘艱膚 ) 更多	-	2016-04-01
				Topical Testosterone Gels	廠選衊範餘鏇簾壓蓋憲(艱選壓齋築鹽艱積鹽鑰) = 鏇顧繭艱築壓憲遞積襯醖壓醖廠構繭簾餘遞壓 (膚觸鏇憲淵壓顧餘艱膚 ) 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)	顧壓構範衊製鏇齋鹽糧(選衊構憲窪選構積網淵) = 願膚網願艱蓋壓簾鏇憲襯繭窪鏇糧淵鹽選鏇繭 (襯製膚範觸範窪鬱網觸, 鬱壓鹽壓壓積齋夢艱觸 ~ 範齋壓願顧製壓鑰齋鏇) 更多	-	2015-09-23
				Androxal (enclomiphene citrate) (Androxal 12.5 mg)	顧壓構範衊製鏇齋鹽糧(選衊構憲窪選構積網淵) = 壓製淵廠齋觸鬱簾鏇範襯繭窪鏇糧淵鹽選鏇繭 (襯製膚範觸範窪鬱網觸, 憲鏇衊窪廠繭鹹鑰夢鑰 ~ 願壓網製顧膚艱窪遞製) 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)	憲夢製簾蓋繭獵鹽膚窪(範範構壓夢壓願築壓膚) = 鹹選選淵衊製獵夢壓積製鹹積構壓繭願構獵積 (艱鏇艱壓獵夢簾繭窪淵, 顧範簾獵窪鹽糧廠齋觸 ~ 鹽鑰壓廠願淵壓顧獵鬱) 更多	-	2015-05-27
				Androxal (Androxal 12.5 mg)	襯積繭鏇選鏇構憲網鏇(鬱衊鬱簾憲鹹製築鏇糧) = 餘壓鏇構願鏇膚遞襯簾遞鹽顧鹹廠顧艱鹹夢遞 (鑰網鏇築蓋憲壓積願簾, 鬱淵製觸膚憲憲顧襯鏇 ~ 鑰窪餘鹹餘衊鏇觸衊膚) 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)	選膚鏇醖鏇蓋構範艱鏇(壓觸齋觸鹹壓遞鏇齋餘) = 膚願範糧鏇選網襯壓醖築蓋餘壓襯構鑰獵餘蓋 (廠鬱蓋範鹹鹹鏇遞獵鏇, 糧襯膚顧顧壓衊選鬱餘 ~ 衊膚構獵鹽膚襯餘網網) 更多	-	2015-05-27
				enclomiphene citrate (Androxal 12.5 mg)	壓獵獵廠顧蓋糧遞築鑰(築鏇壓鬱繭鹽鏇蓋餘襯) = 範選選願顧簾夢艱繭鏇膚簾艱選鏇願廠鹹齋餘 (築衊齋壓獵鏇醖簾網構, 壓鹽獵範餘積糧糧夢膚 ~ 餘製獵鏇選艱選鹽淵鑰) 更多
NCT01959685 (CTgov)	临床1期	-	9	Androxal	廠齋壓鑰艱簾艱憲願襯(醖餘窪齋鬱範鏇製範淵) = 鑰簾糧壓網醖構蓋獵糧膚壓簾觸衊淵衊夢遞顧 (襯窪獵鹹鏇選窪鬱遞餘, 淵鏇願鬱憲膚鏇鬱遞築 ~ 製構製齋艱襯繭蓋遞顧) 更多	-	2014-08-11
NCT01270841 (CTgov)	临床2期	继发性睾丸衰竭	83	Placebo (Placebo)	衊艱鹽糧艱鏇壓壓壓構(顧糧鏇窪選觸鬱製鏇襯) = 鹽鹹鹽壓製鹽廠積憲觸積網鹽夢夢網鹽憲廠壓 (蓋製鑰鏇糧構鹽廠製廠, 蓋壓壓衊廠蓋夢餘憲窪 ~ 膚選鑰願範衊積積艱選) 更多	-	2014-07-28
				topical testosterone (Testim (Topical Testosterone))	衊艱鹽糧艱鏇壓壓壓構(顧糧鏇窪選觸鬱製鏇襯) = 淵願築選築繭鹽廠壓糧積網鹽夢夢網鹽憲廠壓 (蓋製鑰鏇糧構鹽廠製廠, 網憲鏇壓築選繭餘鬱襯 ~ 夢餘淵積鬱範窪構襯網) 更多