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

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

  • Sci Rep. 2025 Nov 3;15(1):38377. doi: 10.1038/s41598-025-22258-x.
Gregory M Young # 1,  Timothy H Helms # 1,  Samuel K Kulp 1,  Adeoluwa A Adeluola 1,  Hanna S Radomska 1,  Tyler A Wilson 2,  Reena Shakya 3,  Alyssa Kabat 4,  Gillian Mulcahy 1,  Abigail K Mayo 1,  Raphael A Malbrue 5,  William C Kisseberth 6,  Chad E Bennett 2 7,  Christopher C Coss 8 9
Affiliations

Affiliations

  • 1 Division of Pharmaceutics and Pharmacology, College of Pharmacy, The Ohio State University, 496 W. 12th Ave, Columbus, OH, 43210, USA.
  • 2 Drug Discovery Shared Resource, Comprehensive Cancer Center, The Ohio State University, 496 W. 12th Ave, Columbus, OH, 43210, USA.
  • 3 Preclinical Therapeutics Mouse Modeling, Comprehensive Cancer Center, The Ohio State University, 496 W. 12th Ave, Columbus, OH, 43210, USA.
  • 4 Charles River Labs, 1 Innovation , 01605, Worcester, MA, USA.
  • 5 Department of Veterinary Preventative Medicine, College of Veterinary Medicine, The Ohio State University, 1900 Coffey Road , OH, Columbus, 43210, USA.
  • 6 Department of Veterinary Clinical Sciences, College of Veterinary Medicine, The Ohio State University, 601 Vernon L Tharp St, Ohio, 43210, USA.
  • 7 Drug Development Institute, Comprehensive Cancer Center, The Ohio State University, 410 W. 12th Ave, Columbus, OH, 43210, USA.
  • 8 Division of Pharmaceutics and Pharmacology, College of Pharmacy, The Ohio State University, 496 W. 12th Ave, Columbus, OH, 43210, USA. coss.16@osu.edu.
  • 9 Drug Development Institute, Comprehensive Cancer Center, The Ohio State University, 410 W. 12th Ave, Columbus, OH, 43210, USA. coss.16@osu.edu.
  • # Contributed equally.
PMID: 41184385 DOI: 10.1038/s41598-025-22258-x
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.

Figures
Products
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z