Delving into the Latest Updates on Estradiol Acetate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

E3A, Estradiol 3-acetate, Estradiol acetate (USAN)

+ [5]

Target

ER

Mechanism

ERs agonists(Estrogen receptors agonists)

Therapeutic Areas

Cardiovascular DiseasesUrogenital Diseases

Active Indication

Vasomotor symptomVulvovaginal atrophy

Inactive Indication

Hot Flashes

Originator Organization

Millicent Holdings Ltd.

Active Organization

Millicent Holdings Ltd.

Inactive Organization

Warner Chilcott Ltd.Allergan Pharmaceuticals International Ltd.

Drug Highest PhaseApproved

First Approval Date

US (20 Mar 2003),

Vasomotor symptomVulvovaginal atrophy

Regulation-

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Structure

Molecular FormulaC20H26O3

InChIKeyFHXBMXJMKMWVRG-SLHNCBLASA-N

CAS Registry4245-41-4

Many women choose Depo-Provera for birth control because it is easy to use and very effective. However, a significant number of Depo-Provera users experience irregular bleeding during the first 90 days. Many users discontinue after their first injection due to irregular bleeding. This study will evaluate the effect of using an estrogen vaginal ring during the first 90 days of Depo-Provera use to see if it is acceptable to women and whether it decreases irregular bleeding during the first 90 days of use and increases continuation to a second injection.

Start Date01 Sep 2007

Sponsor / Collaborator

Columbia University

NCT01070979 / CompletedPhase 3

A Multicenter, Double-Blind, Controlled, Randomized Study to Compare the Efficacy in Relief of Hot Flushes in Women Receiving Oral Estradiol Acetate Tablets, Oral Estradiol Tablets or Oral Conjugated Equine Estrogens

Multicenter, double-blind, controlled, parallel group, randomized study to compare the clinical benefit of Estradiol acetate tablets, estradiol tablets and conjugated equine estrogen tablets, each administered orally, once daily, to postmenopausal women.

Start Date01 Feb 2003

Sponsor / Collaborator

Warner Chilcott Ltd.

100 Clinical Results associated with Estradiol Acetate

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100 Translational Medicine associated with Estradiol Acetate

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100 Patents (Medical) associated with Estradiol Acetate

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138

Literatures (Medical) associated with Estradiol Acetate

01 Mar 2024·Journal of Contaminant Hydrology

Individual and combined impact of microplastics and lead acetate on the freshwater shrimp (Caridina fossarum): Biochemical effects and physiological responses

Article

Author: Multisanti, Cristiana Roberta ; Zeidi, Amir ; Faggio, Caterina ; Gholamhosseini, Amin ; Banaee, Mahdi

Microplastics and heavy metals pollution is recognised as a major problem affecting aquatic ecosystems. For this reason, this study aims to assess the toxicity of different concentrations of polyethylene microplastics (PE-MPs) (0.0, 500, and 1000 μg L^-1) with a mean size of 15-25 μm and lead acetate Pb(C₂H₃O₂)₂ (0.0, 2.5, and 5 mg L^-1), both individually and in combination, through the exposure of the freshwater grass shrimp, Caridinia fossarum for 15 days, focusing on microplastic interaction with co-occurring contaminants. After being exposed to both contaminants, either individually or in combination, significant alterations in numerous biochemical markers were observed. Specifically, exposure to lead acetate alone resulted in significant changes across ALP, AST, ALT, LDH, GGT, and BChE enzyme activity levels indicating hepatotoxicity and neurotoxicity. Also, Pb exposure led to alterations in total antioxidant capacity, MDA, total lipids, and glycogen contents, signalling the onset of oxidative stress. Exposure to PE-MPs alone led to changes in ALP, LDH, GGT, and BChE enzyme levels, and in MDA, total lipids, and glycogen samples' contents. Remarkably, the study observed increased bioaccumulation of lead acetate in samples treated with the combination, emphasizing the synergistic impact of PE-MPs on the toxicity of lead acetate. This synergy was also evident in AST and ALT enzyme activity levels and MDA contents. This underscores the necessity for measures to address both microplastic pollution and heavy metal contamination, taking into account the synergistic behaviour of MPs in the presence of concurrent contaminants.

01 Dec 2022·The Journal of Antibiotics

Microbacterium kunmingensis sp. nov., an attached bacterium of Microcystis aeruginosa

Article

Author: Mao, Li-Na ; Zhang, Bing-Huo ; Chen, Min ; Chen, Jian ; Gui, Shan-Shan ; Peng, Yi-Ru ; Xiao, Yao

A Gram-stain positive, aerobic, rod-shaped actinobacterial strain designated as JXJ CY 27-2^T was isolated from the culture of Microcystis aeruginosa FACHB-905 (Maf) collected from Lake Kunming, southwest China. The isolate was catalase positive, oxidase negative, and able to grow at 10.0-44.0 °C, pH 5.0-10.0 and 0-5.0% NaCl. Based on the 16S rRNA gene sequences, JXJ CY 27-2^T showed high similarities of 98.54-98.55% with Microbacterium invictum DSM 19600^T, Microbacterium saccharophilum DSM 28107^T, and Microbacterium aoyamense DSM 19461^T, and less than 98.47% similarities with other members of the genus. Its major cellular fatty acids were anteiso-C_17:0 and anteiso-C_15:0. The predominant menaquinones were MK-11 and MK-12. The diagnostic diamino acid in the cell wall peptidoglycan was lysine. Whole cell sugars contained mannose, ribose, galactose, rhamnose and arabinose. The polar lipids were diphosphatidylglycerol, phosphatidylglycerol, two unidentified glycolipids, and an unidentified lipid. The DNA G + C content was 69.8%. The digital DNA-DNA hybridization and average nucleotide identity values between strain JXJ CY 27-2^T and its three closest similar strains were 18.4-20.3% and 74.9-75.7%, respectively. Based on the above data, strain JXJ CY 27-2^T was identified as a new species of the genus Microbacterium, for which the name Microbacterium kunmingensis sp. nov. is proposed. The type strain is JXJ CY 27-2^T (=CGMCC 1.17506^T = KCTC 49382^T). Strain JXJ CY 27-2^T could promote the growth of Maf by providing it with available phosphorus, nitrogen and probably other nutrients such as vitamins and indole-3-acetate.

01 Sep 2022·Steroids

Large-scale synthesis of galeterone and lead next generation galeterone analog VNPP433-3β

Article

Author: Thankan, Retheesh S ; Rudchenko, Vladimir ; Purushottamachar, Puranik ; Huang, Guangfei ; Thomas, Elizabeth ; Njar, Vincent C O

VNPP433-3β (compound 2, (3β-(1H-imidazole-1-yl)-17-(1H-benzimidazole-1-yl)-androsta-5,16-diene), a multitarget anticancer agent has emerged as our lead next generation galeterone analogs (NGGA). Here, we describe a large multi-gram (92 g) scale synthesis of compound 2 starting from the commercially available dehydroepiandrosterone-3-acetate (DHEA, 6) via Galeterone (Gal, 1), in 8 steps with a 26% overall yield and 99.5% purity. The overall yield for the synthesis of Gal from DHEA improved from previously reported 47% to 59%. The advantages of this synthesis are as follows: (1) In the first two steps of Scheme 2, the change of solvents and reagents enabled the isolation of compounds 7 and 8 from heptane triturations, as column chromatography was eliminated in both steps. (2) In step 3 (deformylation) the catalyst required was reduced from 50% to 10% (wt/wt) of compound 8 which enable easy purification of compound 9, with modest increased yield. (3) The fourth step to produce Gal (1) was improved by using methanol, eliminating the use of tetrahydrofuran (THF) and dichloromethane, solvent which may be a problem as residual solvent contaminant. (4) In the final step 8, the imidazole-ring formation, inexpensive glyoxal (40% aqueous solution) was used in the reaction instead of expensive glyoxal trimer dihydrate. The structure of the target product (2, VNPP433-3β) was established by NMR spectroscopy, mass spectrometry and elemental analysis. Gal and VNPP433-3β exhibit more potent antiproliferative activities against CWR22Rv1 human prostate cancer cells compared to clinical drugs, Abiraterone and Enzalutamide.

100 Deals associated with Estradiol Acetate

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External Link

KEGG	Wiki	ATC	Drug Bank
D04061	Estradiol Acetate	G03CA03	DB13952

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Vasomotor symptom	US	Millicent Holdings Ltd.	20 Mar 2003
Vulvovaginal atrophy	US	Millicent Holdings Ltd.	20 Mar 2003

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Hot Flashes	Discovery	US	Warner Chilcott Ltd.	01 Feb 2003
Urogenital Diseases	Discovery	US	Warner Chilcott Ltd.	01 Feb 2003

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01070979 (CTgov)	Phase 3	Hot Flashes \| Urogenital Diseases	249	Estradiol acetate (Estradiol Acetate (E3A))	tiqhbrjqwy(uwayufyuco) = zbfugtgood spnsriosvu (akorrsulvk, sdkmaklapx - mpmdqlhhuc) View more	-	08 Apr 2011
				Estradiol (Estradiol)	tiqhbrjqwy(uwayufyuco) = kwkjudmlzs spnsriosvu (akorrsulvk, nrkcjxavuj - peoaoennfb) View more