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Discovery of Palazestrant (OP-1250), a Potent and Orally Bioavailable Complete Estrogen Receptor Antagonist (CERAN) and Selective Estrogen Receptor Degrader (SERD)
Introduction Click to copy section linkSection link copied! Breast cancer is the second most common cause of cancer death in women worldwide after lung cancer. (1) In 2023, approximately 298,000 women in the U.S. were diagnosed with breast cancer. Around 80% of all breast cancers express estrogen receptor alpha (ER). (2) The transcriptional regulatory activities of ER occur via two activation functions (AF), AF1 and AF2 (Figure 1).
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