- •New ER inhibitors show improved pharmacokinetics and pharmacodynamics compared to fulvestrant.
- •Composition of the side chain of oral SERDs affects their efficacy for efficacy.
- •Five oral SERDs are in phase III trials in the advanced setting and two in the adjuvant setting.
- •New ER inhibitors/degraders under investigation: SERCA, CERAN, PROTAC, and SERM/SERD hybrid.
- •Oral route and potency render the agents ideal endocrine backbone for combination therapies.
Abbreviations:AI: (Aromatase Inhibitor), AF-1 and AF2: (Activation Fuctions 1 and 2 regions of ER), CDK4/6: (Cyclin Dependent Kinase 4 and 6), CERAN: (Complete ER ANtagonists), cfDNA: (cell free DNA), DCIS: (Ductal Carcinoma In Situ), EMA: (European Medicine Agency), ESR1: (Estrogen Receptor 1), FDA: (Food and Drug Administration), HER2- : (Human Epidermal growth factor Receptor 2 negative), HR+ : (Hormone Receptors positive), OS: (Overall Survival), PFS: (Progression-Free Survival), PI3K: (Phosphatidylinositol 3-kinase), PK: (Pharmacokinetics), PROTAC: (PROteolysis TArgeting Chimera), SERCA: (Selective Estrogen Receptor Covalent Antagonist), SERD: (Selective Estrogen Receptor Degrader), SERM: (Selective Estrogen Receptor Modulator)
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