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2015 ; 58
(12
): 4883-7
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gab.com Text
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English Wikipedia
Oral Selective Estrogen Receptor Downregulators (SERDs), a Breakthrough Endocrine
Therapy for Breast Cancer
#MMPMID26039356
McDonnell DP
; Wardell SE
; Norris JD
J Med Chem
2015[Jun]; 58
(12
): 4883-7
PMID26039356
show ga
Drugs that inhibit estrogen receptor alpha (ER?) or that block the production of
estrogens remain frontline interventions in the treatment and management of
breast cancer at all stages. However, resistance to endocrine therapies,
especially in the setting of advanced disease, remains an impediment to durable
clinical responses. Although the mechanisms underlying resistance to existing
agents are complex, preclinical studies suggest that selective estrogen receptor
downregulators (SERDs), molecules which eliminate ER? expression, may have
particular utility in the treatment of breast cancers that have progressed on
tamoxifen and/or aromatase inhibitors. The discovery and development of orally
bioavailable SERDs provide the opportunity to evaluate the utility of eliminating
ER? expression in advanced metastatic breast cancers.