LNS8801: An Enantiomerically Pure Agonist of the G Protein-Coupled Estrogen Receptor Suitable for Clinical Development

  • Cancer Res Commun. 2025 Apr 1;5(4):556-568. doi: 10.1158/2767-9764.CRC-24-0632.
Christopher A Natale  #  1  2 ,  Sophia Mercado  #  2 ,  Richard Zhuang  2 ,  Cristina Aguirre-Portolés  2 ,  Israel Olayide  3 ,  Christopher K Arnatt  3 ,  John T Seykora  2 ,  Tina K Garyantes  1 ,  Wayne Luke  1 ,  Todd W Ridky  2
Affiliations
  • 1. Linnaeus Therapeutics, Haddonfield, New Jersey.
  • 2. Department of Dermatology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania.
  • 3. Department of Chemistry and Biochemistry, Saint Louis University, St. Louis, Missouri.
  • # Contributed equally.
PMID: 40066851 DOI: 10.1158/2767-9764.CRC-24-0632
Abstract

GPER is broadly expressed in human tissues and has tumor-suppressive activity. No FDA-approved agents selectively target GPER. LNS8801 is a synthetic, orally bioavailable, enantiomerically pure, GPER agonist with potent Anticancer activity in vivo. LNS8801 response is attenuated by a common germline coding variant present in roughly half of humans.

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