A Phase 2, Randomized, Double-blind, Placebo-controlled Proof-of-Concept Study to Evaluate the Efficacy and Safety of Estetrol in Postmenopausal Subjects With Female Sexual Arousal Disorder

The goal of this clinical trial is investigating estetrol (E4) in women after menopause, suffering from sexual arousal disorder. The main question it aims to answer is: is 20 mg estetrol monohydrate effective in the treatment of sexual arousal disorder in women after their menopause. Participants will visit the clinic 7 times and complete a daily diary while receiving estetrol or placebo for 12 weeks. Placebo is a pill that looks the same as estetrol but has no active ingredient. Researchers will compare estetrol and placebo to see if estetrol has an effect on the sexual arousal of the participants.

开始日期2024-01-29

申办/合作机构

Estetra SRL

EUCTR2022-002476-36-DE / Unknown status临床2期

A RANDOMIZED, DOUBLE-BLIND, PLACEBO-CONTROLLED, PHASE 2 STUDY TO ASSESS THE INFLUENCE OF ESTETROL (E4) ON SKIN PARAMETERS IN POSTMENOPAUSAL WOMEN (PILOT STUDY)

开始日期2023-01-24

申办/合作机构

Estetra SRL

EUCTR2019-003002-27-PL / Not yet recruiting临床3期

A Multicenter, Open-label, Single-Arm Study to Evaluate the Safety, Compliance and Pharmacokinetics associated with the use of a Combined Oral Contraceptive Containing 15 mg Estetrol monohydrate and 3 mg Drospirenone in Post-menarchal Female Adolescents for 6 cycles

开始日期2022-08-19

申办/合作机构

Estetra SRL

100 项与雌四醇相关的临床结果

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100 项与雌四醇相关的转化医学

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100 项与雌四醇相关的专利（医药）

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203

项与雌四醇相关的文献（医药）

2024-03-03·Journal of biomolecular structure & dynamics

Effectiveness of estrogen and its derivatives over dexamethasone in the treatment of COVID-19

Article

作者: Shaquiquzzaman, M. ; Sheikh, Khursheed A. ; Amin, Shaista ; Parveen, Darakhshan ; Ali, Ruhi ; Akhter, Mymoona ; Ahmed Khan, Mohammad ; Alam, M. Mumtaz ; Anwer, Tarique ; Azam, Faizul ; Das, Anwesha

Coronavirus disease (COVID-19) is an infectious disease caused by the SARS-CoV-2 virus and dexamethasone is a glucocorticoid widely used for its treatment. Dexamethasone is not used in non-severe cases due to its immunosuppressant action. So, considering this, Estrogen and Estetrol were tested for the treatment of COVID-19 as they all possess a common steroid ring and dislike dexamethasone, they are immunoenhancer. Virtual screening of test ligands was performed through molecular docking, MM-GBSA, simulations, in silico ADMET and drug-likeness prediction to identify their potential to inhibit the effects of SARS-CoV-2. Results showed that test ligands possess drug-like properties and they are safe as drug candidates. The protein-ligand interaction study revealed that they bind with the amino acid residues at the active site of the target proteins and the test ligands possess better binding potential than Dexamethasone. With protein M^pro, Estetrol and Estrogen showed docking score of -7.240 and -5.491 kcal/mol, and with protein ACE2, Estetrol and Estrogen showed docking score of -5.269 and -4.732 kcal/mol, respectively. Further, MD Simulation was carried out and most of the interactions of molecular docking are preserved during simulation. The prominent interactions that our test ligands showed during MD Simulation are similar to drugs that possess in vitro anticovid activity as shown in recent studies. Hence, our test ligands possessed potential for anticovid activity and they should be further tested through in vitro and in vivo studies for their activity against COVID-19.Communicated by Ramaswamy H. Sarma.

2024-02-01·Contraception

Comparison of estrogenic components used for hormonal contraception

Review

作者: Stanczyk, Frank Z ; Archer, David F ; Foidart, Jean-Michel ; Winer, Sharon A

Attempts have been made over the years to replace ethinyl estradiol (EE) in combined oral contraceptives (COCs) with the less potent natural estrogen estradiol (E₂), or its prodrug, E₂ valerate (E₂V), to improve their safety and tolerability. Recently, a COC incorporating a novel weak natural estrogen, estetrol (E₄), combined with drospirenone, has become available. We present a comparative analysis of the three prevailing estrogens used in COCs, focusing on their structure-function relationships, receptor-binding affinity, potency, metabolism, pharmacokinetic parameters, and pharmacodynamics. The binding affinity of EE to estrogen receptor (ER)α is twice that of E₂, whereas its affinity for ERβ is about one-half that of E₂. E₄ has a lower binding affinity for the ERs than E₂. The high potency of EE is notable in its dramatic increase in estrogen-sensitive hepatic globulins and coagulation factors. EE and E₂ undergo extensive and comparable metabolism, while E₄ produces only a very limited number of metabolites. E₄ has the highest bioavailability among the three estrogens, with E₂ having <5%. Studies demonstrate consistent ovulation inhibition, although a higher dose of E₄ (15 mg) in COCs is required to achieve follicular suppression compared to E₂ (1-3 mg) and EE (0.01-0.035 mg). E₂ and E₄ in COCs may be less stimulatory of coagulant proteins than EE. Studies with E₂/dienogest suggest a comparable risk of venous thromboembolism to EE/levonorgestrel, while data assessing risk with an E₄-based COC are insufficient. Nevertheless, the E₄-based formulation shows promise as a potential alternative to EE and E₂ due to its lower potency and possibly fewer side effects.

2024-01-13·Biology of reproduction

Reversible female contraceptives: historical, current, and future perspectives

Review

作者: Stephens, Kalli K ; Winuthayanon, Wipawee ; Allred, Stephanie I ; Woodall, Kirby A ; Erickson, Jeffery A ; Jeffries, Jenna M ; Hunter, Mark I ; Barton, Brooke E

Abstract:

Contraception is a practice with extensive and complicated social and scientific histories. From cycle tracking, to the very first prescription contraceptive pill, to now having over-the-counter contraceptives on demand, family planning is an aspect of healthcare that has undergone and will continue to undergo several transformations through time. This review provides a comprehensive overview of current reversible hormonal and non-hormonal birth control methods as well as their mechanism of action, safety, and effectiveness specifically for individuals who can become pregnant. Additionally, we discuss the latest Food and Drug Administration (FDA)-approved hormonal method containing estetrol and drospirenone that has not yet been used worldwide as well as the first FDA-approved hormonal over-the-counter progestin-only pills. We also review available data on novel hormonal delivery through microchip, microneedle, and the latest FDA-approved non-hormonal methods such as vaginal pH regulators. Finally, this review will assist in advancing female contraceptive method development by underlining constructive directions for future pursuits. Information was gathered from the NCBI and Google Scholars databases using English and included publications from 1900 to present. Search terms included contraceptive names as well as efficacy, safety, and mechanism of action. In summary, we suggest that investigators consider the side effects and acceptability together with the efficacy of contraceptive candidate towards their development.

项与雌四醇相关的新闻（医药）

2024-06-12

·Pharmaceutical Technology

Bankrupt Mithra cashes in on remaining assets for $188.2m

Mithra’s efforts to extend its cash runway earlier this year were unsuccessful. Image credit: Shutterstock/Nudphon Phuengsuwan. A day after filing for bankruptcy, Mithra has sold its share in two of its daughter pharmaceutical companies along with rights to its female hormone drug portfolio for €175m ($188.2m). Recommended Buyer's Guides Buyer's Guide Leading Guide to Packaging Materials, Containers and Containment Services for the Pharmaceutical Industry Buyer's Guide Leading Guide to Compliance Software for the Pharmaceutical Industry The deal saw Budapest-headquartered pharma company Gedeon Richter buy all of Mithra’s shares in Neuralis and Estetra – both subsidiaries of the struggling women’s health pharmaceutical company. Gedeon Richter also gained assets related to the manufacturing of estetrol. The funds, after deduction of financial debts, will be used to repay Mithra’s creditors, meaning the sale does not create any value for the shareholders of Mithra Pharmaceuticals , according to a 10 June press release. Belgium-based Mithra has faced severe financial difficulties in the past few years with share prices tanking by more than 90%. Efforts to extend its cash runway , which included raising $13.7m by selling its stake in Mayne Pharma , were unsuccessful, forcing the company to file for bankruptcy and siphon off its remaining holdings. The transfer will see Gedeon Richter gain rights to Mithra’s Estelle (estetrol-E4 / drospirenone), marketed as Nextstellis and Drovelis in the US and EU respectively. Estelle netted Mithra €2.6m in the first half of 2023. See Also: NPX-267 by NextPoint Therapeutics for Triple-Negative Breast Cancer (TNBC): Likelihood of Approval NPX-267 by NextPoint Therapeutics for Non-Small Cell Lung Cancer: Likelihood of Approval Gedeon Richter will also take on development duties for Mithra’s menopause treatment candidate Donesta which produced positive topline Phase III results in mid-2023. The orally administered estetrol (E4) hormone therapy is slated for US approval in 2024 and EU approval in 2025. Mithra said that “all 49 members of the personnel engaged by the transferred entities will be able to pursue their activities with Gedeon Richter,” along with 17 other employees who have been offered jobs by the latter company. Two of Mithra’s other properties – Novalon, a long-acting drug specialist entity it acquired in 2015, and a contract development and manufacturing organisation (CDMO) facility – remain unaffected by the deal with Gedeon Richter and stay under protection. Mithra said it expects offers to come in by mid-month subject to judicial protection measures being extended. In a statement released on 10 June announcing bankruptcy filing, Mithra stated its employees’ research and future progress “will outlive Mithra and will continue under a different banner from now on. We all hope that these efforts will lead to the development of new solutions that will benefit as many people as possible.”

临床3期并购临床结果

2024-05-28

·GlobeNewswire-Health Care

Mithra postpones its annual general meeting

Liege, Belgium, 28 May 2024 – 15:00 CEST – Mithra (Euronext Brussels: MITRA), a company dedicated to women’s health, today announces that in the context of the monetization process and the uncertainties related thereto, Mithra postpones its Annual General Shareholders’ Meeting, previously planned for 30 May 2024, to a later date to be determined. Background Information: On 5 March 2024, Mithra announced the launch of a comprehensive monetization process, exploring potential sales of selected assets, notably Estetra SRL, and potentially the entire business. Additionally, Mithra announced the entry into a secured bridge loan facility (“the Facility”) for an amount of up to EUR 13.5 million to be drawn in multiple tranches upon the satisfaction of certain milestones, as well as an uncommitted EUR 5 million "accordion" facility (which could be used once the committed amount has been fully drawn and only if the lenders consent). The lenders under the Facility consist of funds managed by Highbridge Capital Management, LLC and funds managed by Whitebox Advisors, LLC. The monetization process for Mithra’s CDMO and Novalon SA assets are proceeding under court protection measures from the Liege Company Courts. The Mithra CDMO asset in Flemalle, Belgium was granted “Transfer under Judicial Supervision” with court-designated trustees to oversee negotiations with potential bidders and select the best offer while safeguarding the interests of the company, its creditors, and its employees. The Judicial reorganization proceedings to restructure the debt of Novalon SA, Mithra’s complex therapeutics business, involves reaching an amicable agreement with some creditors and implementing a court-sanctioned debt-restructuring plan therewith. The protection measures are expected to remain in effect until 19 June 2024. For more information, please contact: Mithra Pharmaceuticals SAAlex Sokolowski, PhDHead of IR & Communicationsinvestorrelations@mithra.com +32 (0)4 349 28 22 Frédérique Depraetere Communications Directorinfo@mithra.com+32 (0)4 349 28 22 About Mithra Mithra Pharmaceuticals SA (Euronext: MITRA) is a Belgian biopharmaceutical company dedicated to transforming women’s health by offering new choices through innovation, with a particular focus on contraception and menopause. Mithra’s goal is to develop products offering better efficacy, safety and convenience, meeting women’s needs throughout their life span. Mithra explores the potential of the unique native estrogen estetrol in a wide range of applications in women health and beyond. After having successfully launched the first estetrol-based product in 2021, the contraceptive pill ESTELLE®, Mithra is now focusing on its second product DONESTA®, the next-generation hormone therapy. Mithra also offers partners a complete spectrum of solutions from early drug development, clinical batches and commercial manufacturing of complex polymeric products (vaginal ring, implants) and complex liquid injectables and biologicals (vials, pre-filled syringes or cartridges) at its technological platform Mithra CDMO. Active in more than 100 countries around the world, is headquartered in Liège, Belgium. www.mithra.comESTELLE® and DONESTA® are registered trademarks of Mithra Pharmaceuticals or one of its affiliates. Important informationThe contents of this announcement include statements that are, or may be deemed to be, "forward-looking statements". These forward-looking statements can be identified by the use of forward-looking terminology, including the words "believes", "estimates," "anticipates", "expects", "intends", "may", "will", "plans", "continue", "ongoing", "potential", "predict", "project", "target", "seek" or "should", and include statements the Company makes concerning the intended results of its strategy. By their nature, forward-looking statements involve risks and uncertainties, and readers are cautioned that any such forward-looking statements are not guarantees of future performance. The Company's actual results may differ materially from those predicted by the forward-looking statements. The Company undertakes no obligation to publicly update or revise forward-looking statements, except as may be required by law.

2024-04-29

·GlobeNewswire-Health Care

Mithra updates on offers received in the context of its monetization process and on its Annual Report 2023

Mithra has received binding offers for selected assets, including Estetra SRL, as part of its monetization process. As it stands, the aggregate amount of these offers is insufficient to ensure full repayment of all creditors of Mithra, and, therefore, the offers do not allow to create value for Mithra’s shareholders at the present time.Mithra has requested the suspension of trading of its shares on Euronext Brussels pending continuing negotiations with offering parties.Mithra postpones the publication of its Annual Report 2023 to a later date due to the current circumstances to reflect a situation in discontinuity. LIEGE, Belgium, April 29, 2024 (GLOBE NEWSWIRE) -- Mithra (Euronext Brussels: MITRA), a company dedicated to women’s health, announces that it has received several binding offers1 for selected Mithra assets (particularly Estetra SRL) during the week of 22 April 2024, as part of its ongoing monetization process— first announced on 05 March 2024. In collaboration with Stifel Investment Bank and other expert advisors, Mithra is diligently analyzing these offers, which include all shares in Estetra SRL and certain other activities and assets within the Mithra group. Mithra continues to seek potential buyers for all its activities and assets (i.e., Mithra CDMO, Novalon, Mithra R&D, Neuralis, Mithra parent co.). As it stands, the aggregate amount of these offers is insufficient to ensure full repayment of all creditors of Mithra. Therefore, the offers received will not create value for the shareholders of Mithra. Mithra remains committed to negotiating with the offering parties to enhance the value offered, acting in the best interest of all stakeholders. The Company is also considering taking appropriate action, including continuing negotiations for the relevant assets under court proceedings (as is the case for other assets of the Mithra group), to advance these discussions further if necessary. Consequently, Mithra has requested the Financial Services and Markets Authority (FSMA) to suspend trading of the Company’s shares on Euronext Brussels pending the on-going negotiations. Mithra remains committed to executing its monetization process with diligence and transparency representing the interests of all stakeholders and will continue providing timely updates to the market and stakeholders as appropriate. Additionally, Mithra will postpone the publication of its Annual Report 2023 (originally scheduled for 30 April 2024) as it was prepared based on a going concern assumption. Instead, considering the recent events, an annual report will be prepared and published for Mithra reflecting a situation "in discontinuity" at a later date, which will be announced in a subsequent communication. About MithraMithra Pharmaceuticals SA (Euronext: MITRA) is a Belgian biopharmaceutical company dedicated to transforming women’s health by offering new choices through innovation, with a particular focus on contraception and menopause. Mithra’s goal is to develop products offering better efficacy, safety and convenience, meeting women’s needs throughout their life span. Mithra explores the potential of the unique native estrogen estetrol in a wide range of applications in women health and beyond. After having successfully launched the first estetrol-based product in 2021, the contraceptive pill ESTELLE®, Mithra is now focusing on its second product DONESTA®, the next-generation hormone therapy. Mithra also offers partners a complete spectrum of solutions from early drug development, clinical batches and commercial manufacturing of complex polymeric products (vaginal ring, implants) and complex liquid injectables and biologicals (vials, pre-filled syringes or cartridges) at its technological platform Mithra CDMO. Active in more than 100 countries around the world, is headquartered in Liège, Belgium. www.mithra.com ESTELLE® and DONESTA® are registered trademarks of Mithra Pharmaceuticals or one of its affiliates. Important informationThe contents of this announcement include statements that are, or may be deemed to be, "forward-looking statements". These forward-looking statements can be identified by the use of forward-looking terminology, including the words "believes", "estimates," "anticipates", "expects", "intends", "may", "will", "plans", "continue", "ongoing", "potential", "predict", "project", "target", "seek" or "should", and include statements the Company makes concerning the intended results of its strategy. By their nature, forward-looking statements involve risks and uncertainties, and readers are cautioned that any such forward-looking statements are not guarantees of future performance. The Company's actual results may differ materially from those predicted by the forward-looking statements. The Company undertakes no obligation to publicly update or revise forward-looking statements, except as may be required by law. 1 subject to certain / customary conditions

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100 项与雌四醇相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D11513	雌四醇	-	DB12235

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
绝经期综合征	临床3期	美国	Estetra SRL	2019-09-27
绝经期综合征	临床3期	加拿大	Estetra SRL	2019-09-27
血管舒缩症	临床3期	美国	Estetra SRL	2019-09-27
血管舒缩症	临床3期	加拿大	Estetra SRL	2019-09-27
更年期综合症	临床3期	-	Mithra Pharmaceuticals SA	-
潮热	临床2期	比利时	Donesta Bioscience BV	2016-05-01
避孕	临床2期	芬兰	Estetra SRL	2010-09-01

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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


NCT02720224 (CTgov)	临床1期	避孕	6	Estetrol	選衊製觸構構襯窪廠繭(觸醖壓鑰窪膚膚醖製艱) = 衊廠簾廠餘糧繭選顧鏇衊觸觸簾範築簾淵蓋廠 (壓鹽構積鏇繭艱簾鏇艱, 簾膚淵構鏇廠鹽築鑰淵 ~ 積衊製鹽壓糧簾鹹衊醖) 更多	-	2018-12-10