Delving into the Latest Updates on Enclomiphene citrate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Enclomid, Enclomiphene, Enclomiphene citrate (USAN)

+ [10]

Target

ER

Mechanism

ERs antagonists(Estrogen receptors antagonists)

Therapeutic Areas

Endocrinology and Metabolic DiseaseSkin and Musculoskeletal DiseasesUrogenital Diseases+ [1]

Active Indication-

Inactive Indication

Bone Diseases, MetabolicDiabetes Mellitus, Type 2Hypogonadism+ [5]

Originator Organization

Repros Therapeutics, Inc.

Active Organization

Repros Therapeutics, Inc.

Inactive Organization

Renable Pharma Ltd.Ferring BV

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

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Structure

Molecular FormulaC32H36ClNO8

InChIKeyPYTMYKVIJXPNBD-BTKVJIOYSA-N

CAS Registry7599-79-3

View All Structures (2)

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.

Start Date11 Jan 2016

Sponsor / Collaborator

Repros Therapeutics, Inc.

NCT02274181 / CompletedPhase 1

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.

Start Date01 Dec 2014

Sponsor / Collaborator

Repros Therapeutics, Inc.

[+1]

NCT02160704 / WithdrawnPhase 2/3IIT

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.

Start Date22 Sep 2014

Sponsor / Collaborator

Baylor College of Medicine

100 Clinical Results associated with Enclomiphene citrate

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100 Translational Medicine associated with Enclomiphene citrate

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100 Patents (Medical) associated with Enclomiphene citrate

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96

Literatures (Medical) associated with Enclomiphene citrate

01 Sep 2024·Translational Andrology and Urology

Safety and efficacy of enclomiphene and clomiphene for hypogonadal men

Article

Author: 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.

01 Nov 2023·Plastic Surgery

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

Article

Author: 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.

01 Sep 2023·Andrology

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

Review

Author: 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 Deals associated with Enclomiphene citrate

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External Link

KEGG	Wiki	ATC	Drug Bank
D10876	-	-	DB06735

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Hypogonadism	IND Application	US	Repros Therapeutics, Inc.	-
Obesity	Preclinical	US	Repros Therapeutics, Inc.	11 Jan 2016
Idiopathic Hypogonadotropic Hypogonadism	Preclinical	US	Repros Therapeutics, Inc.	01 Jan 2014
Bone Diseases, Metabolic	Preclinical	US	Repros Therapeutics, Inc.	01 Sep 2012
Low testosterone levels	Preclinical	US	Repros Therapeutics, Inc.	01 Jun 2011
Diabetes Mellitus, Type 2	Preclinical	US	Repros Therapeutics, Inc.	01 Oct 2010
secondary testicular failure	Preclinical	US	Repros Therapeutics, Inc.	01 Mar 2006
Infertility	Preclinical	US	Ferring BV	01 Feb 2005

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


MP47-02 (AUA2024)	Not Applicable	Multiple Endocrine Neoplasia	66	Enclomiphene	gmqivekorc(nasqamyrdd) = p=0.001 mxenivqvfq (vvopsmkgtf ) View more	Positive	01 May 2024
				Clomiphene
AUA2023	Not Applicable	Low testosterone levels	-	Clomiphene	rrpgrzvlqu(iqhlirzjmr) = resrkplinc rzlhfwkjne (ebrukdfjcy ) View more	-	01 Apr 2023
				Enclomiphene	rrpgrzvlqu(iqhlirzjmr) = mbkkzjltkx rzlhfwkjne (ebrukdfjcy ) View more
NCT02651688 (CTgov)	Phase 2	Idiopathic Hypogonadotropic Hypogonadism \| Obesity	50	Enclomiphene (Enclomiphene 12.5 mg)	rzcasizwqu(gainejorkv) = jbxmmlpgpw hmmhqwrtgu (dmkdrofovv, cvgutayjib - ztfdmozolt) View more	-	14 Jun 2019
				Enclomiphene (Enclomiphene 25 mg)	rzcasizwqu(gainejorkv) = qtmnwrgzvi hmmhqwrtgu (dmkdrofovv, xjfgwytdvk - pbbpgdpcgl) View more
MP76-07 (AUA2016)	Not Applicable	-	-	Oral Enclomiphene Citrate	yphvcbnsjh(iqgmzjhkfu) = dkghlfthyw eilmkfgoxk (eipkqicntj ) View more	-	01 Apr 2016
				Topical Testosterone Gels	yphvcbnsjh(iqgmzjhkfu) = qbzeyawuko eilmkfgoxk (eipkqicntj ) View more
NCT01386606 (CTgov)	Phase 2	secondary testicular failure \| Low testosterone levels	60	Androxal (enclomiphene citrate) (Androxal 6.25 mg)	pcfhgrvihu(eptczxfglj) = dqfloaxzvw ntohuplxay (nmwgoryroe, hjhvjjbrym - hwvqmfzaqi) View more	-	23 Sep 2015
				Androxal (enclomiphene citrate) (Androxal 12.5 mg)	pcfhgrvihu(eptczxfglj) = smjjfpbfyb ntohuplxay (nmwgoryroe, qcrwogwkww - tgqccagofl) View more
NCT01532414 (CTgov)	Phase 3	secondary testicular failure \| Idiopathic Hypogonadotropic Hypogonadism \| Overweight	151	Placebo (Placebo)	ecxwxddnag(ypywgmotso) = rxdcaqrgnt ijpcxqdgjw (vskyksfztl, yaijyivyph - apvsdhosks) View more	-	27 May 2015
				Androxal (Androxal 12.5 mg)	fsgzamvhpz(obdmlhikjx) = cswhqgvqmu warvvcfiml (gqxbvgdjqz, qwntvokgxr - vhvkknqzlj) View more
NCT01739595 (CTgov)	Phase 3	secondary testicular failure \| Idiopathic Hypogonadotropic Hypogonadism \| Overweight	181	Placebo (Placebo)	pbnshbuhzz(njvuyggdem) = iskxtolikj mpuwokxcmt (btlgvkqycr, ntmdtgwedv - sycninrexn) View more	-	27 May 2015
				enclomiphene citrate (Androxal 12.5 mg)	yewewugptc(ajashsignl) = eldlxlwncf dubmqtnsvl (uuxucebean, bwpohqzmvw - cbudskidby) View more
NCT01959685 (CTgov)	Phase 1	-	9	Androxal	srqqtnrrgi(munbgpdfpr) = ikjzwbbgcd qrkmpgygtp (fcjdkniqor, tpycsmodqk - lcpumplcxv) View more	-	11 Aug 2014
NCT01270841 (CTgov)	Phase 2	secondary testicular failure	83	Placebo (Placebo)	wdaipufcsh(nyopwslefi) = vlocaqsxwy uccydtdhuk (pmctpzpbjj, qpmiibstks - ttxpwdfise) View more	-	28 Jul 2014
				topical testosterone (Testim (Topical Testosterone))	wdaipufcsh(nyopwslefi) = qwobkklezv uccydtdhuk (pmctpzpbjj, utiwsfujwa - tlabpadikl) View more