Delving into the Latest Updates on Estradiol Valerate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Estradiol valerate (JAN/USP/INN)

+ [10]

Target

ER

Mechanism

ERs agonists(Estrogen receptors agonists)

Therapeutic Areas

NeoplasmsNervous System DiseasesCardiovascular Diseases+ [3]

Active Indication

Oestrogen deficiencyAmenorrheaAndropause+ [10]

Inactive Indication-

Originator Organization

Endo International Plc

Active Organization

Endo Operations Ltd.

Hubei Huazhong Pharmaceutical Co. Ltd.

Mochida Pharmaceutical Co., Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

US (15 Jul 1954),

HypoestrogenismProstatic CancerVasomotor symptom+ [1]

Regulation-

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Structure

Molecular FormulaC23H32O3

InChIKeyRSEPBGGWRJCQGY-RBRWEJTLSA-N

CAS Registry979-32-8

An Open Label, Prospective, Randomized, Multi-Center, Three-arm Clinical Trial to Compare the Efficacy and Safety of Estradiol hemihydrate Tablet 2mg Vs Estradiol Valerate Vs Estradiol hemihydrate Tablet (2 mg) plus Estradiol TG (Topical Gel) in Patients who are Candidate for Frozen Embryo Transfer (FET) Cycle - NIL

Start Date31 Jul 2024

Sponsor / Collaborator-

CTRI/2024/06/068270 / Not yet recruitingPhase 4IIT

Comparing The Effect Of Estradiol Valerate And Conjugated Equine Estrogen In The Patients With Premature Ovarian Insufficiency A Randomized Control Trial - NIL

Start Date15 Jun 2024

Sponsor / Collaborator

Guru Teg Bahadur Hospital

CTR20240788 / CompletedNot Applicable

戊酸雌二醇片在中国健康绝经后女性参与者中单中心、随机、开放、两周期、自身交叉、单次给药的空腹和餐后状态下生物等效性研究

[Translation] A single-center, randomized, open-label, two-period, self-crossover, single-dose bioequivalence study of estradiol valerate tablets in healthy Chinese postmenopausal female participants under fasting and fed conditions

主要目的：考察空腹及餐后状态下单次口服受试制剂戊酸雌二醇片（规格：1 mg/片，武汉九珑人福药业有限责任公司生产）与参比制剂戊酸雌二醇片（补佳乐®，规格：1 mg/片；Jenapharm GmbH & Co. KG持证）在中国健康绝经后女性参与者体内的药代动力学特征，评价空腹及餐后状态口服两种制剂的生物等效性。次要目的：考察受试制剂戊酸雌二醇片（规格：1 mg/片）和参比制剂戊酸雌二醇片（补佳乐®，规格：1 mg/片）在中国健康绝经后女性参与者中的安全性。

[Translation]

Primary objective: To investigate the pharmacokinetic characteristics of the test preparation estradiol valerate tablets (specification: 1 mg/tablet, produced by Wuhan Jiulong Renfu Pharmaceutical Co., Ltd.) and the reference preparation estradiol valerate tablets (Progynova®, specification: 1 mg/tablet; certified by Jenapharm GmbH & Co. KG) in healthy Chinese postmenopausal female participants after a single oral administration in the fasting and fed state, and to evaluate the bioequivalence of the two preparations in the fasting and fed state. Secondary objective: To investigate the safety of the test preparation estradiol valerate tablets (specification: 1 mg/tablet) and the reference preparation estradiol valerate tablets (Progynova®, specification: 1 mg/tablet) in healthy Chinese postmenopausal female participants.

Start Date03 Apr 2024

Sponsor / Collaborator

Wuhan Jiulong Renfu Pharmaceutical Co., Ltd.

100 Clinical Results associated with Estradiol Valerate

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100 Translational Medicine associated with Estradiol Valerate

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100 Patents (Medical) associated with Estradiol Valerate

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1,944

Literatures (Medical) associated with Estradiol Valerate

31 Dec 2024·Journal of Obstetrics and Gynaecology

Decoction of Yougui Wan combined with Wuzi Yanzong Wan ameliorates thin endometrium in a mouse model

Article

Author: Zhou, Xiaohong ; Su, Aifang ; Xiang, Jun

BACKGROUNDThis study aimed to determine the effect and mechanism of the Decoction of Yougui Wan combined with Wuzi Yanzong Wan (DYWWYW), a traditional Chinese herbal formula, in a mouse model with thin endometrium induced by 95% ethanol.METHODSThin endometrium mice were treated with progynova (0.002 mg) as well as a low and high dose of DYWWYW (0.05 and 0.5 mL DYWWYW, respectively, diluted in 2 mL normal saline). Western blotting and qRT-PCR analyses were performed to determine the protein and mRNA expression levels, respectively, of integrin αγβ3 and leukaemia inhibitor factor (LIF) in uterus tissues. Serum oestradiol and progesterone concentrations were determined via ELISA. The remaining thin endometrium mice were mated with male mice, and the number of embryos implanted in the different groups was calculated.RESULTSA high dose of DYWWYW effectively ameliorated the injury of endometrium caused by 95% ethanol. The levels of oestradiol, progesterone, αγβ3 and LIF in thin endometrium mice treated with a high dose of DYWWYW were also significantly elevated. Additionally, a high dose of DYWWYW remarkably increased the number of embryo implantations in mice with thin endometrium.CONCLUSIONDYWWYW has improvement effects on thin endometrium by elevating the levels of endogenous oestradiol, progesterone, αγβ3, and LIF in a mouse model.

01 Dec 2024·International Journal of Biological Macromolecules

Evaluating the estrogen degradation potential of laccase and peroxidase from Bacillus ligniniphilus L1 through integrated computational and experimental approaches

Article

Author: Zhe, Liang ; Zhu, Daochen ; Khalid, Hafiz Rameez ; Nawaz, Muhammad Zohaib ; Haider, Syed Zeeshan ; Alghamdi, Huda Ahmad ; Mirza, Muhammad Usman

This study investigated the degradation potential of laccase and catalase-peroxidase from the extremophilic marine bacterium Bacillus ligniniphilus L1 against endogenous and synthetic estrogen compounds using an integrated computational and experimental approach. Molecular docking identified five estrogen compounds exhibiting reliable bindings with enzymes, which were then subjected to enzyme activity assays. The degradation potential of the two enzymes against five selected estrogen compounds were investigated and compared with their commercial counterparts. Laccase from L1 showed higher degradation potential against estrone (47.02 % without and 62.21 % with ABTS) compared to commercial laccase (39 % without and 54.20 % with ABTS). For estradiol valerate, commercial laccase showed a slightly higher degradation (52.47 %) than L1 laccase (49.94 %), but with ABTS, L1 laccase performed better (74.15 % vs. 68.03 %). Notably, L1 catalase-peroxidase demonstrated significantly higher degradation for all tested compounds compared to its commercial counterpart with efficiencies of 96.16 %, 89.09 %, 74.94 %, 64.91 %, and 62.80 % against estropipate, quinestrol, estradiol valerate, estriol and estrone, respectively, revealing its potential for commercial applications. Molecular dynamics simulations revealed the interaction and stability of enzyme-estrogen complexes, with MMGBSA binding energy calculations supporting experimental results. These findings highlight the usefulness of the computational approach in elucidating the molecular mechanisms underlying enzyme-mediated bioremediation of environmental contaminants.

01 Nov 2024·The Journal of Nutrition

Alginate Oligosaccharides Enhance Gut Microbiota and Intestinal Barrier Function, Alleviating Host Damage Induced by Deoxynivalenol in Mice

Article

Author: Mi, Jinqiu ; Li, Tiantian ; Zhang, Qiyue ; Lin, Gang ; Tong, Yaoyi ; Ma, Qiugang ; Wang, Qingfeng ; Wang, Yanwei ; Huang, Shimeng ; Wang, Yue

BACKGROUNDAlginate oligosaccharides (AOS) exhibits notable effects in terms of anti-inflammatory, antibacterial, and antioxidant properties. Deoxynivalenol (DON) has the potential to trigger intestinal inflammation by upregulating pro-inflammatory cytokines and apoptosis, thereby compromising the integrity of the intestinal barrier function and perturbing the balance of the gut microbiota.OBJECTIVESWe assessed the impact of AOS on mitigating DON-induced intestinal damage and systemic inflammation in mice.METHODSAfter a 1-wk acclimatization period, the mice were divided into 4 groups. For 3 wk, the AOS and AOS + DON groups were gavaged daily with 200 μL of AOS [200 mg/kg body weight (BW)], whereas the CON and DON groups received an equivalent volume of sterile Phosphate-Buffered Saline (PBS). Subsequently, for 1 wk, the DON and AOS + DON groups received 100 μL of DON (4.8 mg/kg BW) daily, whereas the control (CON) and AOS groups continued receiving PBS.RESULTSAfter administering DON via gavage to mice, there was a significant decrease (P < 0.05) in body weights compared with the CON group. Interestingly, AOS exhibited a tendency to mitigate this weight loss in the AOS + DON group. In the feces of mice treated with both AOS and DON, the concentration of DON significantly increased (P < 0.05) compared with the DON group alone. Histological analysis revealed that DON exposure caused increased intestinal damage, including shortened villi and eroded epithelial cells, which was ameliorated by presupplementation with AOS, alleviating harm to the intestinal barrier function. In both jejunum and colon tissues, DON exposure significantly reduced (P < 0.05) the expression of tight junction proteins (claudin and occludin in the colon) and the mucin protein mucin 2, compared with the CON group. Prophylactic administration of AOS alleviated these reductions, thereby improving the expression levels of these key proteins. Additionally, AOS supplementation protected DON-exposed mice by increasing the abundance of probiotics such as Bifidobacterium, Faecalibaculum, and Romboutsia. These gut microbes are known to enhance (P < 0.05) anti-inflammatory responses and the production of short-chain fatty acids (SCFAs), including total SCFAs, acetate, and valerate, compared with the DON group.CONCLUSIONSThis study unveils that AOS not only enhances gut microbiota and intestinal barrier function but also significantly mitigates DON-induced intestinal damage.

100 Deals associated with Estradiol Valerate

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External Link

KEGG	Wiki	ATC	Drug Bank
D01413	Estradiol Valerate	G03CA03	DB13956

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Oestrogen deficiency	CN	Hubei Huazhong Pharmaceutical Co. Ltd.	01 Jan 1983
Amenorrhea	JP	Mochida Pharmaceutical Co., Ltd.	01 Nov 1954
Andropause	JP	Mochida Pharmaceutical Co., Ltd.	01 Nov 1954
Dysmenorrhea	JP	Mochida Pharmaceutical Co., Ltd.	01 Nov 1954
Hypomenorrhea	JP	Mochida Pharmaceutical Co., Ltd.	01 Nov 1954
Infertility	JP	Mochida Pharmaceutical Co., Ltd.	01 Nov 1954
Menorrhagia	JP	Mochida Pharmaceutical Co., Ltd.	01 Nov 1954
Metrorrhagia	JP	Mochida Pharmaceutical Co., Ltd.	01 Nov 1954
Ovarian Diseases	JP	Mochida Pharmaceutical Co., Ltd.	01 Nov 1954
Hypoestrogenism	US	Endo Operations Ltd.	15 Jul 1954
Prostatic Cancer	US	Endo Operations Ltd.	15 Jul 1954
Vasomotor symptom	US	Endo Operations Ltd.	15 Jul 1954
Vulvovaginal atrophy	US	Endo Operations Ltd.	15 Jul 1954

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03300518 (Pubmed \| Hum Reprod)	Not Applicable	-	552	Estrogen valerate pretreatment	xpuibinsdx(wzuidyixwo) = efjigbpnxn pbzdqxqioh (uvgztyhqid )	Negative	23 Apr 2022
				Estrogen valerate (Control group)	xpuibinsdx(wzuidyixwo) = ithodbqcxh pbzdqxqioh (uvgztyhqid )
NCT04537078 (CTgov)	Phase 3	Infertility, Female	90	Combined Oral Contraceptive+Decapeptyl+Cyclo-Progynova+progesterone+Gonadotropin+Duphaston (the Progestin Primed Double Stimulation Group)	gplhorabes(deqjxuobep) = zrfuaugvxj hhbocaavvp (jkavlvoxtf, gxaflpuhfv - qnvanzgmbl) View more	-	17 Feb 2022
				Combined Oral Contraceptive+Cetrotide Injectable Product+Decapeptyl+Cyclo-Progynova+progesterone+Chorionic Gonadotropin+Gonadotropin (the Flexible GnRh Antagonist)	vixzukkonj(fufhnfswjb) = dinowygyim kdslowcmvc (tfvwwnnehc, hpgbcenhgm - ftkxenphhl) View more
NCT00816556 (CTgov)	Phase 3	Atrophic Vaginitis	63	Estriol (Estriol)	caaxvwaosn(gsamztibln) = elyygyfvpe lsfwgsknjz (lxsxbgrpvf, hshujmwzhv - twxlrxbvia) View more	-	28 Mar 2014
				estradiol valerate (Estradiol)	caaxvwaosn(gsamztibln) = zzmisftmlc lsfwgsknjz (lxsxbgrpvf, qiyfmhaspd - mvhasktnxw) View more