Imlunestrant Is an Oral, Brain-Penetrant Selective Estrogen Receptor Degrader with Potent Antitumor Activity in ESR1 Wild-Type and Mutant Breast Cancer.

doi:10.1158/0008-5472.CAN-24-2608

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Imlunestrant Is an Oral, Brain-Penetrant Selective Estrogen Receptor Degrader with Potent Antitumor Activity in ESR1 Wild-Type and Mutant Breast Cancer.

Cancer research - 17 Feb 2025

Bhagwat Shripad V, Mur Cecilia, Vandekopple Matthew, Zhao Baohui, Shen Weihua, Marugán Carlos, Capen Andrew, Kindler Lisa, Stephens Jennifer R, Huber Lysiane, Castanares Mark A, Garcia-Tapia David, Cohen Jeff D, Bastian Jolie, Mattioni Brian, Yuen Eunice, Baker Thomas K, Rodriguez Cruz Vivian, Fei Dongling, Manro Jason R, Pulliam Nicholas, Dowless Michele S, Ortiz Ruiz Maria Jesus, Yu Chunping, Puca Loredana, Klippel Anke, Bacchion Francesca, Ismail-Khan Roohi, Rodrik-Outmezguine Vanessa, Peng Sheng-Bin, Lallena María Jose, Gong Xueqian, de Dios Alfonso

Abstract excerpt

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 exposure, and acquired...

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PMID: 39652577
DOI: 10.1158/0008-5472.CAN-24-2608
PMCID: PMC11831106

Genes

ESR1
CDK4

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