Evidence map›Paper›PMID 41184385›Full record

ArticleScientific reports2025

OSU-ERβ-12: a promising pre-clinical candidate selective estrogen receptor beta agonist.

Gregory M Young, Timothy H Helms, Samuel K Kulp, Adeoluwa A Adeluola, Hanna S Radomska, Tyler A Wilson, Reena Shakya, Alyssa Kabat, Gillian Mulcahy, Abigail K Mayo and 4 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Scientific reports, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

2 citing papers in PubMed.

  1. Review
  2. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

14 authors.

Gregory M Young *Division of Pharmaceutics and Pharmacology, College of Pharmacy, The Ohio State University, 496 W. 12th Ave, Columbus, OH, 43210, USA.
Timothy H Helms *Division of Pharmaceutics and Pharmacology, College of Pharmacy, The Ohio State University, 496 W. 12th Ave, Columbus, OH, 43210, USA.
Samuel K KulpDivision of Pharmaceutics and Pharmacology, College of Pharmacy, The Ohio State University, 496 W. 12th Ave, Columbus, OH, 43210, USA.
Adeoluwa A AdeluolaDivision of Pharmaceutics and Pharmacology, College of Pharmacy, The Ohio State University, 496 W. 12th Ave, Columbus, OH, 43210, USA.
Hanna S RadomskaDivision of Pharmaceutics and Pharmacology, College of Pharmacy, The Ohio State University, 496 W. 12th Ave, Columbus, OH, 43210, USA.
Tyler A WilsonDrug Discovery Shared Resource, Comprehensive Cancer Center, The Ohio State University, 496 W. 12th Ave, Columbus, OH, 43210, USA.
Reena ShakyaPreclinical Therapeutics Mouse Modeling, Comprehensive Cancer Center, The Ohio State University, 496 W. 12th Ave, Columbus, OH, 43210, USA.
Alyssa KabatCharles River Labs, 1 Innovation , 01605, Worcester, MA, USA.
Gillian MulcahyDivision of Pharmaceutics and Pharmacology, College of Pharmacy, The Ohio State University, 496 W. 12th Ave, Columbus, OH, 43210, USA.
Abigail K MayoDivision of Pharmaceutics and Pharmacology, College of Pharmacy, The Ohio State University, 496 W. 12th Ave, Columbus, OH, 43210, USA.
Raphael A MalbrueDepartment of Veterinary Preventative Medicine, College of Veterinary Medicine, The Ohio State University, 1900 Coffey Road , OH, Columbus, 43210, USA.
William C KisseberthDepartment of Veterinary Clinical Sciences, College of Veterinary Medicine, The Ohio State University, 601 Vernon L Tharp St, Ohio, 43210, USA.
Chad E BennettDrug Discovery Shared Resource, Comprehensive Cancer Center, The Ohio State University, 496 W. 12th Ave, Columbus, OH, 43210, USA.
Christopher C CossDivision of Pharmaceutics and Pharmacology, College of Pharmacy, The Ohio State University, 496 W. 12th Ave, Columbus, OH, 43210, USA. coss.16@osu.edu.

Funding

Translational Therapeutics Research Program (TT)P30CA016058 · NCI · OHIO STATE UNIVERSITY · PI Daniel G. Stover · 1985 to 2026
$132.3M
NCI NIH HHS P30 CA016058
6 · The paper itself

Abstract

Estrogen receptor beta (ERβ) is a favorable therapeutic target for mediating inflammation, attenuating fibrosis, and treating cancer. However, selectively targeting ERβ over estrogen receptor alpha (ERα) has been a longstanding challenge. Recently, we developed OSU-ERβ-12, a novel carborane-based ERβ agonist that has a greater than 100-fold selectivity for ERβ over ERα. In this study, we compare the pharmacokinetics and functional activity of OSU-ERβ-12 against the clinical comparator ERβ agonist erteberel (LY500307) in multiple model systems. Pharmacokinetic profiling revealed OSU-ERβ-12 to have superior pharmacokinetics in pre-clinical models compared to LY500307 while maintaining a similar ERβ selectivity. Additionally, OSU-ERβ-12 displayed high human liver microsome stability and negligible CYP, hERG, and off-target interactions. Overall, OSU-ERβ-12 is a potent, selective, pharmacokinetically superior ERβ agonist that warrants additional study.

Indexed as

Estrogen Receptor betaAnimalsEstrogen Receptor alphaFemaleHumansMaleMiceMicrosomes, LiverRatsEstrogen Receptor alphaEstrogen Receptor beta

Identifiers

PMID41184385
PMCPMC12583746

What OpenQuestion holds

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LicenceCC BY-NC-ND
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Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.