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2015 ; 36
(10
): 1163-9
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Toward rapamycin analog (rapalog)-based precision cancer therapy
#MMPMID26299952
Meng LH
; Zheng XF
Acta Pharmacol Sin
2015[Oct]; 36
(10
): 1163-9
PMID26299952
show ga
Rapamycin and its analogs (rapalogs) are the first generation of mTOR inhibitors,
which have the same molecular scaffold, but different physiochemical properties.
Rapalogs are being tested in a wide spectrum of human tumors as both monotherapy
and a component of combination therapy. Among them, temsirolimus and everolimus
have been approved for the treatment of breast and renal cancer. However,
objective response rates with rapalogs in clinical trials are modest and
variable. Identification of biomarkers predicting response to rapalogs, and
discovery of drug combinations with improved efficacy and tolerated toxicity are
critical to moving this class of targeted therapeutics forward. This review
focuses on the aberrations in the PI3K/mTOR pathway in human tumor cells or
tissues as predictive biomarkers for rapalog efficacy. Recent results of
combinational therapy using rapalogs and other anticancer drugs are documented.
With the rapid development of next-generation genomic sequencing and precision
medicine, rapalogs will provide greater benefits to cancer patients.
|Animals
[MESH]
|Antibiotics, Antineoplastic/*chemistry/pharmacology/*therapeutic use
[MESH]