PMID- 22994502
OWN - NLM
STAT- MEDLINE
DCOM- 20130418
LR  - 20211203
IS  - 1744-7658 (Electronic)
IS  - 1354-3784 (Linking)
VI  - 21
IP  - 12
DP  - 2012 Dec
TI  - Everolimus in the treatment of hormone receptor-positive breast cancer.
PG  - 1835-43
LID - 10.1517/13543784.2012.726218 [doi]
AB  - INTRODUCTION: The phosphoinositide triphosphate kinase (PI3K)/AKT/mammalian 
      target of rapamycin (mTOR) is a central regulatory pathway involved in cell 
      proliferation, growth, differentiation, metabolism and survival. Deregulation of 
      this pathway is well described in breast cancer and is associated to the 
      development of endocrine resistance among hormone receptor (HR)-positive tumors. 
      Everolimus , an mTOR-inhibitor has clinical activity against breast cancer and 
      has shown to restore sensitivity to endocrine therapy. AREAS COVERED: We review 
      the clinical data and the results of the recently published clinical trials 
      evaluating the use of everolimus in HR-positive breast cancer patients in 
      combination with endocrine therapy. We discuss the data regarding efficacy but 
      also describe in detail the side effect profile of this drug. EXPERT OPINION: 
      Everolimus represents a new therapeutic alternative for the treatment of 
      HR-positive metastatic breast cancer. Everolimus is in general a well-tolerated 
      drug, however, stomatitis, fatigue and hematological abnormalities are common. It 
      is still unclear if there are specific subgroups of patients that receive greater 
      benefit from everolimus and whether there is a relationship between the presence 
      of PIK3CA mutations and efficacy. The results of biomarker studies will hopefully 
      provide information that will help us determine which patients are most likely to 
      benefit from this treatment.
FAU - Chavez-MacGregor, Mariana
AU  - Chavez-MacGregor M
AD  - The University of Texas, MD Anderson Cancer Center, Department of Breast Medical 
      Oncology, 1155 Herman P Pressler, CPB5.3540, Houston, TX 77030, USA.
FAU - Gonzalez-Angulo, Ana Maria
AU  - Gonzalez-Angulo AM
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PT  - Review
DEP - 20120920
PL  - England
TA  - Expert Opin Investig Drugs
JT  - Expert opinion on investigational drugs
JID - 9434197
RN  - 0 (Antineoplastic Agents)
RN  - 0 (Receptors, Steroid)
RN  - 9HW64Q8G6G (Everolimus)
RN  - EC 2.7.1.1 (MTOR protein, human)
RN  - EC 2.7.11.1 (Proto-Oncogene Proteins c-akt)
RN  - EC 2.7.11.1 (TOR Serine-Threonine Kinases)
RN  - W36ZG6FT64 (Sirolimus)
SB  - IM
MH  - Antineoplastic Agents/pharmacology/*therapeutic use
MH  - Breast Neoplasms/*drug therapy/metabolism
MH  - Everolimus
MH  - Humans
MH  - Phosphatidylinositol 3-Kinases/metabolism
MH  - Proto-Oncogene Proteins c-akt/metabolism
MH  - Receptors, Steroid
MH  - Sirolimus/*analogs & derivatives/pharmacology/therapeutic use
MH  - TOR Serine-Threonine Kinases/antagonists & inhibitors/metabolism
EDAT- 2012/09/22 06:00
MHDA- 2013/04/20 06:00
CRDT- 2012/09/22 06:00
PHST- 2012/09/22 06:00 [entrez]
PHST- 2012/09/22 06:00 [pubmed]
PHST- 2013/04/20 06:00 [medline]
AID - 10.1517/13543784.2012.726218 [doi]
PST - ppublish
SO  - Expert Opin Investig Drugs. 2012 Dec;21(12):1835-43. doi: 
      10.1517/13543784.2012.726218. Epub 2012 Sep 20.