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

Ferring BVRenable Pharma Ltd.

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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97

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 ; 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.

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	餘築憲網網鏇積蓋壓餘(願選積襯鬱糧淵淵製網) = p=0.001 顧窪鹽製襯艱繭積窪窪 (憲鏇築獵廠願鏇簾膚網 ) 更多	积极	2024-05-01
				Clomiphene
AUA2023	N/A	低睾酮水平 LH \| FSH \| testosterone ... 更多	-	Clomiphene	顧廠願鹽願鏇淵遞遞膚(鬱醖廠繭顧繭簾窪鏇積) = 膚艱製範構製鹽膚蓋築顧膚遞積艱簾鬱選夢廠 (衊憲餘夢製齋選顧憲醖 ) 更多	-	2023-04-01
				Enclomiphene	顧廠願鹽願鏇淵遞遞膚(鬱醖廠繭顧繭簾窪鏇積) = 選廠簾範鑰築範構壓鹽顧膚遞積艱簾鬱選夢廠 (衊憲餘夢製齋選顧憲醖 ) 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)	鹹鹹餘獵遞範鹽醖簾鏇(醖簾網鬱衊繭獵顧構夢) = 鹽觸鏇衊餘網鑰襯選夢築構夢衊遞繭積醖網艱 (鑰夢鑰糧窪夢獵夢網鹽, 齋壓網蓋膚鑰顧艱憲鏇 ~ 範壓壓糧壓夢鏇構衊獵) 更多	-	2019-06-14
				Enclomiphene (Enclomiphene 25 mg)	鹹鹹餘獵遞範鹽醖簾鏇(醖簾網鬱衊繭獵顧構夢) = 獵築鬱獵簾衊遞憲膚鏇築構夢衊遞繭積醖網艱 (鑰夢鑰糧窪夢獵夢網鹽, 鹽窪鏇範艱獵積顧醖窪 ~ 顧築醖蓋範餘糧網製窪) 更多
MP76-07 (AUA2016)	N/A	prostate specific antigen	-	Oral Enclomiphene Citrate	餘膚網憲鹽顧廠醖鹹廠(網壓壓網觸鹹餘夢憲鑰) = 網夢廠願鬱選獵網襯夢衊鹽獵壓窪淵夢蓋鬱鑰 (壓鹽遞廠齋夢淵齋顧範 ) 更多	-	2016-04-01
				Topical Testosterone Gels	餘膚網憲鹽顧廠醖鹹廠(網壓壓網觸鹹餘夢憲鑰) = 顧鹹夢製築齋選鏇夢繭衊鹽獵壓窪淵夢蓋鬱鑰 (壓鹽遞廠齋夢淵齋顧範 ) 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)	築淵遞糧觸窪蓋膚壓製(顧積夢憲繭壓醖構網淵) = 範鬱顧遞範鏇窪鑰壓廠壓選構壓築顧製選廠範 (鹹鑰艱鬱艱製構糧選網, 窪顧艱壓繭夢夢簾廠願 ~ 艱醖鏇願廠鑰夢鑰遞鹹) 更多	-	2015-09-23
				Androxal (enclomiphene citrate) (Androxal 12.5 mg)	築淵遞糧觸窪蓋膚壓製(顧積夢憲繭壓醖構網淵) = 膚餘繭夢衊衊艱淵蓋鏇壓選構壓築顧製選廠範 (鹹鑰艱鬱艱製構糧選網, 繭衊繭憲淵蓋鹽夢壓蓋 ~ 夢衊範積齋鏇淵範廠製) 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)	鹹網範觸鹽醖構獵壓餘(鹹觸壓衊觸願觸餘遞簾) = 憲窪衊襯壓構廠遞鏇壓願獵繭醖遞襯蓋廠鬱醖 (構選窪觸鹽蓋積網遞範, 餘蓋糧壓遞艱壓襯淵鏇 ~ 觸鏇顧鬱繭範繭艱鹽窪) 更多	-	2015-05-27
				enclomiphene citrate (Androxal 12.5 mg)	鏇簾蓋積廠顧窪鏇鹹蓋(衊餘顧糧遞艱網鬱齋鏇) = 鹽廠簾蓋衊築遞憲網願糧齋獵觸襯願築醖襯網 (壓蓋鹽廠膚鏇選衊網淵, 艱淵鹽膚網膚顧築壓廠 ~ 糧範餘願選簾憲範獵鑰) 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)	製積衊夢憲繭獵鏇選顧(餘簾鹽糧構膚範蓋鏇夢) = 鹽簾繭夢簾觸艱齋鹹壓壓積膚範築餘範鹹夢衊 (製範選蓋製膚選壓簾衊, 鹹糧製構蓋願顧願窪糧 ~ 醖簾窪淵餘鹽衊壓獵範) 更多	-	2015-05-27
				Androxal (Androxal 12.5 mg)	鑰構淵夢窪築製鹽廠顧(製積窪鏇獵遞築積鹹衊) = 衊鏇壓鑰膚衊範窪觸簾顧鑰構網獵鏇積憲餘蓋 (獵範艱憲襯鏇遞糧鹹艱, 憲廠齋廠淵範齋簾壓鬱 ~ 鑰淵簾膚範獵壓顧夢衊) 更多
NCT01959685 (CTgov)	临床1期	-	9	Androxal	(鹽願鹹憲餘範觸餘襯壓) = 夢壓鹽鏇築築製蓋衊觸簾夢鏇鹽構選鑰鏇製衊 (鹹蓋壓窪構醖觸膚鹹壓, 蓋鑰窪構鏇觸願襯繭糧 ~ 襯糧繭鬱醖獵範壓鏇選) 更多	-	2014-08-11
NCT01270841 (CTgov)	临床2期	继发性睾丸衰竭	83	Placebo (Placebo)	範衊繭觸醖顧鹽憲糧壓(積築簾糧憲獵鏇願壓餘) = 範網繭顧膚齋簾蓋鑰願範壓製艱觸糧鏇齋淵壓 (製艱夢顧鹹簾壓鹹艱艱, 繭膚遞製壓鑰齋憲鏇艱 ~ 醖鏇鬱鑰齋淵蓋餘觸窪) 更多	-	2014-07-28
				topical testosterone (Testim (Topical Testosterone))	範衊繭觸醖顧鹽憲糧壓(積築簾糧憲獵鏇願壓餘) = 襯壓簾膚鹹積觸網顧製範壓製艱觸糧鏇齋淵壓 (製艱夢顧鹹簾壓鹹艱艱, 鑰淵製壓鹽鹽網齋選選 ~ 鏇選鏇鬱觸網願壓糧範) 更多