Related Experiment Video
Updated: Apr 5, 2026

Author Spotlight: Developing Tools to Tune the Activity of Tyrosine Phosphatases
Published on: September 6, 2024
Toward rapamycin analog (rapalog)-based precision cancer therapy
Ling-hua Meng1,2, X F Steven Zheng1
1Rutgers Cancer Institute of New Jersey and Division of Cancer Pharmacology, Robert Wood Johnson Medical School Rutgers, The State University of New Jersey, New Brunswick, NJ 08903, USA.
Abstract:
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.
Insights
Rapamycin analogs (rapalogs) show modest efficacy in cancer treatment. Aberrations in the PI3K/mTOR pathway may predict response, guiding combination therapies for improved patient outcomes.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Rapamycin analogs (rapalogs) are mTOR inhibitors used in cancer therapy.
- Approved rapalogs like temsirolimus and everolimus treat breast and renal cancers.
- Current objective response rates for rapalogs are modest and variable.
Purpose of the Study:
- To review predictive biomarkers for rapalog efficacy.
- To document recent combination therapies involving rapalogs.
- To highlight the role of PI3K/mTOR pathway aberrations.
Main Methods:
- Review of literature on rapalogs and mTOR inhibitors.
- Focus on PI3K/mTOR pathway aberrations as predictive biomarkers.
- Documentation of clinical trial results for combination therapies.
Main Results:
- PI3K/mTOR pathway aberrations are potential predictive biomarkers for rapalog efficacy.
- Combination therapies with rapalogs show promise for improved efficacy.
- Next-generation sequencing and precision medicine are advancing rapalog applications.
Conclusions:
- Identifying predictive biomarkers is crucial for optimizing rapalog therapy.
- Combination strategies are essential for enhancing rapalog effectiveness.
- Rapalogs hold significant potential for future cancer patient benefits.
More Related Videos
Related Concept Videos
mTOR Signaling and Cancer Progression
The mTOR pathway or the...
mTOR Signaling and Cancer Progression
PI3K/mTOR/AKT Signaling Pathway
Targeted Cancer Therapies
There are several types of targeted therapies against...
Targeted Cancer Therapies
Combination Therapies and Personalized Medicine
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...

