PI3K inhibition to overcome endocrine resistance in breast cancer.
Expert Opin Investig Drugs
; 27(1): 1-15, 2018 01.
Article
em En
| MEDLINE
| ID: mdl-29252036
ABSTRACT
INTRODUCTION:
Activation of the phosphatidylinositol-3 kinase (PI3K) pathway is a critical step in oncogenesis and plays a role in the development of treatment resistance for both estrogen receptor (ER) positive and human epidermal growth factor receptor 2 (HER2) positive breast cancers. Hence, there have been efforts to therapeutically inhibit this pathway. AREAS COVERED Several inhibitors of PI3K are now progressing through clinical trials with varying degrees of efficacy and toxicity to date. Numerous unresolved questions remain concerning the optimal isoform selectivity of PI3K inhibitors and use of predictive biomarkers. This review examines the most important PI3K inhibitors in ER positive breast cancer to date, with a particular focus on their role in overcoming endocrine therapy resistance and the possible use of PIK3CA mutations as a predictive biomarker. EXPERT OPINION We discuss some of the emerging challenges and questions encountered during the development of PI3K inhibitors from preclinical to phase III studies, including other novel biomarkers and future combinations to overcome endocrine resistance.Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Neoplasias da Mama
/
Inibidores de Fosfoinositídeo-3 Quinase
/
Antineoplásicos
Tipo de estudo:
Prognostic_studies
Limite:
Female
/
Humans
Idioma:
En
Revista:
Expert Opin Investig Drugs
Assunto da revista:
TERAPIA POR MEDICAMENTOS
Ano de publicação:
2018
Tipo de documento:
Article
País de afiliação:
Irlanda