Mechanisms of resistance to selective estrogen receptor down-regulator in metastatic breast cancer.
Biochim Biophys Acta Rev Cancer
; 1868(1): 148-156, 2017 Aug.
Article
en En
| MEDLINE
| ID: mdl-28344099
ABSTRACT
Based on the prominent role estrogen receptor (ER) plays in breast cancer, endocrine therapy has been developed to block the ER pathway and has shown great effectiveness. Fulvestrant, the first selective ER down-regulator (SERD), was demonstrated to completely suppress ERα and notably efficient. However, resistance to fulvestrant occurs, either intrinsic or acquired during the treatment. Several potential mechanisms inducing fulvestrant resistance have been proposed, composed of activated ERα-independent compensatory growth factor signaling, stimulated downstream kinases, altered cell cycle mediators, etcetera. Experimentally, combinations of fulvestrant with targeted treatments were reported to eliminate the resistance and improve the effect of fulvestrant. Meanwhile, some clinical trials associated with the targeted combination therapies are in progress. This review focuses on the underlying mechanisms that contribute to fulvestrant resistance in ER-positive breast cancer and provides an overview of combined fulvestrant with targeted agents to shed light on optimal therapies for patients with ER-positive breast cancer.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Neoplasias de la Mama
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Receptores de Estrógenos
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Regulación hacia Abajo
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Resistencia a Antineoplásicos
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Moduladores de los Receptores de Estrógeno
Límite:
Animals
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Female
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Humans
Idioma:
En
Revista:
Biochim Biophys Acta Rev Cancer
Año:
2017
Tipo del documento:
Article