Imlunestrant Is an Oral, Brain-Penetrant Selective Estrogen Receptor Degrader with Potent Antitumor Activity in ESR1 Wild-Type and Mutant Breast Cancer.
Authors:Bhagwat SV,Mur C,Vandekopple M,Zhao B,Shen W,Marugán C,Capen A,Kindler L,Stephens JR,Huber L,Castanares MA,Garcia-Tapia D,Cohen JD,Bastian J,Mattioni B,Yuen E,Baker TK,Rodriguez Cruz V,Fei D,Manro JR,Pulliam N,Dowless MS,Ortiz Ruiz MJ,Yu C,Puca L,Klippel A,Bacchion F,Ismail-Khan R,Rodrik-Outmezguine V,Peng SB,Lallena MJ,Gong X,de Dios A
Journal:Cancer research
PubMed ID:39652577
Targeting of the estrogen receptor (ER) by antiestrogens is the standard of care for patients with ER+ HER2- advanced/metastatic breast cancer. Although antiestrogens that degrade ERα (fulvestrant) or block estrogen production (aromatase inhibitors) have improved patient outcomes, clinically important challenges remain related to drug administration, limited bioavailability, lack of brain ... More