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Last update 08 May 2025

Estropipate

Last update 08 May 2025

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Estra-1,3,5 (10)-triene-17-one-3-yl-sulfate, Estrone 3-sulfate, Estrone bisulfate

+ [9]

Target

Action

agonists

Mechanism

ERs agonists(Estrogen receptors agonists)

Therapeutic Areas

Endocrinology and Metabolic DiseaseNeoplasmsSkin and Musculoskeletal Diseases

Active Indication

Endocrine System DiseasesBreast Cancer

Inactive Indication-

Originator Organization-

Active Organization

University of Toronto

Inactive Organization-

License Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC18H22O5S

InChIKeyJKKFKPJIXZFSSB-CBZIJGRNSA-N

CAS Registry481-97-0

View All Structures (2)

100 Clinical Results associated with Estropipate

100 Translational Medicine associated with Estropipate

100 Patents (Medical) associated with Estropipate

2,562

Literatures (Medical) associated with Estropipate

01 Jul 2025·The Journal of Steroid Biochemistry and Molecular Biology

Evaluation of the effects of estrogens on endometrial cancer cells of different grades

Article

Author: Rižner, Tea Lanišnik ; Pušić, Maja Novak ; Pavlič, Renata

Endometrial cancer (EC) is the most common gynecological malignancy in the Western world. The molecular basis and effects of various agents are frequently studied in model EC cell lines, but the most commonly used cell lines Ishikawa, HEC-1-A, RL95-2 and KLE have not been thoroughly and systematically investigated. We characterized EC cell lines of different grades by reassessing the expression of estrogen receptors ERα, ERβ, and GPER by qPCR and Western blot and investigated the effects of estrogens, estrone-sulfate, estrone and estradiol on their proliferation, migration, and clonogenicity. Estradiol promoted the proliferation of grade 1 Ishikawa EC cells and grade 2 RL95-2 cells. Estrone and estrone sulfate also stimulated the proliferation of Ishikawa, showed a tendency to increase the proliferation of HEC-1-A and RL95-2 cells, but decreased the proliferation of KLE. Estrogens had no effect on the migration and clonogenicity of these four EC cell lines, however, there was a trend toward a smaller colony area for cells incubated with higher estrogen concentrations. We have previously shown that in EC estradiol forms from inactive estrone sulfate via the sulfatase pathway. This study showed that estrogens significantly promote the proliferation of grade 1 Ishikawa EC cells, and grade 2 RL95-2 and decrease the proliferation of grade 3 KLE cells. These differences in proliferation were associated with ERα positivity of Ishikawa cells and GPER expression in other cells.

01 Jun 2025·Drug Metabolism and Pharmacokinetics

Exploring the effect of intracellular loop 1 genetic variants in human ABCG2 on transport activity and protein abundance

Article

Author: Sjöstedt, Noora ; Auriola, Seppo ; Vellonen, Kati-Sisko ; Bhattacharya, Madhushree ; Suominen, Laura ; Timmermans, Ritchie G M ; Vieraankivi, Marika ; Kidron, Heidi

ABCG2 (breast cancer resistance protein, BCRP), can affect drug disposition, and thus, variation in the ABCG2 gene may alter drug exposure. We studied non-synonymous naturally occurring single-nucleotide variants (SNVs) in intracellular loop 1 (ICL1), which contains a coupling helix that transmits conformational changes in the protein. Reference ABCG2, the common SNVs V12M and Q141K, and five SNVs (K453R, I456V, H457R, G462R and G462V) in ICL1 were expressed in HEK293 cells. Additionally, combinations of selected SNVs were expressed to determine if an activating substitution in ICL1 could compensate for an inactivating substitution elsewhere. Transport of Lucifer yellow, estrone sulfate and rosuvastatin was studied using membrane vesicles and the ABCG2 abundance was quantified. While K453R and I456V abundance was similar to the reference ABCG2, abundance was lower for H457R and G462R/V. Apparent transport activities were partially substrate dependent, but excluding G462R/V, the ICL variants transported at least one of the substrates similarly to the reference ABCG2. In double substitutions, I456V had a more consistent effect than H457R on both transport activity and protein abundance. Altogether, SNVs in ICL1 can have both detrimental and beneficial effects on ABCG2 activity. Effects may be hard to predict, especially if more than one SNV is present.

01 Jun 2025·Journal of Pharmaceutical Sciences

In vitro characterization of SLCO2B1 genetic variants

Article

Author: Miinalainen, Annika ; Kivioja, Saara ; Niemi, Mikko ; Sinokki, Alli ; Kidron, Heidi ; Auriola, Seppo ; Bhattacharya, Madhushree ; Kiander, Wilma ; Huttunen, Kristiina M ; Vellonen, Kati-Sisko ; Gynther, Mikko

OATP2B1, encoded by SLCO2B1, is a drug transporter expressed widely throughout the body in tissues such as the intestine and liver. Genetic variation of this transporter may lead to altered disposition of OATP2B1 substrate drugs, but especially the effects of rare variants are poorly understood. The aim of this study was to characterize the effects of naturally occurring missense single nucleotide variants of SLCO2B1 (c.601G>A, c.935G>A, c.953C>T, c.1175C>, c.1457C>T, c.1559G>C, c.1596C>A, and the c.601G>A + c.935G>A haplotype) on the in vitro functionality of OATP2B1. To characterize transport activity, cellular uptake of dibromofluorescein, 5-carboxyfluorescein, estrone sulfate, and rosuvastatin was compared in OATP2B1 reference- and variant-expressing HEK293 cells. The abundance of OATP2B1 variants in HEK293 crude membrane preparations was quantified with LC-MS/MS-based quantitative targeted absolute proteomics analysis. Variant c.1559G>C impaired OATP2B1-mediated uptake of all tested substrates almost completely, but protein abundance was not reduced to the same extent. Other studied variants had comparable or only modestly reduced protein abundance and transport function compared to reference OATP2B1. These results can be utilized to understand findings from clinical pharmacogenetic studies. More importantly, the results can aid in predicting the consequences of rare variants, such as the loss-of-function variant c.1559G>C, which can be difficult to detect in clinical studies.

100 Deals associated with Estropipate

External Link

KEGG	Wiki	ATC	Drug Bank
D00948	Estropipate	G03CA07 G03CC04	DB04574

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Endocrine System Diseases	United States	-	-

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Breast Cancer	Preclinical	Canada	University of Toronto	15 Apr 2013

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