Related Experiment Video
Updated: Jun 4, 2026

Development and Application of Rapamycin-regulated Tyrosine Phosphatases
Published on: September 6, 2024
Current and future directions in mammalian target of rapamycin inhibitors development
Angelica Fasolo1, Cristiana Sessa
1Istituto Nazionale dei Tumori, via Venezian 1, Milan, Italy.
Introduction:
The mammalian target of the rapamycin (mTOR) signalling pathway has a central role in the regulation of cell growth, survival and angiogenesis and the frequent dysregulation of this pathway in tumor cells makes it a crucial target in the treatment of cancer. Temsirolimus and everolimus are approved for use in metastatic renal cell carcinoma and temsirolimus is also approved for mantle cell lymphoma. All three rapalogs, temsirolimus, everolimus and deforolimus, are currently being evaluated in Phase III studies in several tumors.
Areas Covered:
This paper provides a review of the published literature on the mTOR pathway and related pathway signaling, analogs and novel mTOR inhibitors. The most recent and important data on the mTOR pathway, the role of mTOR inhibitors in cancer treatment and the current status of development of second-generation highly potent and selective mTOR inhibitors are overviewed.
Expert Opinion:
The published data on new mTOR inhibitors are still limited, but the available preclinical results indicate that they have a potent antiproliferative activity against a broad panel of tumor cell lines, have a favorable safety profile, can obtain disease stabilization or even tumor regression and, in some cases, enhance the efficacy of other targeted or standard-of-care anticancer drugs when used in vivo in preclinical studies.
Insights
The mammalian target of the rapamycin (mTOR) pathway is crucial for cancer treatment. New mTOR inhibitors show potent anticancer activity and a favorable safety profile in preclinical studies.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- The mammalian target of the rapamycin (mTOR) signaling pathway regulates cell growth, survival, and angiogenesis.
- Dysregulation of the mTOR pathway is common in cancer, making it a key therapeutic target.
- Rapalogs like temsirolimus and everolimus are approved for specific cancers, with others in clinical trials.
Purpose of the Study:
- To review the literature on the mTOR pathway, its inhibitors, and their role in cancer treatment.
- To overview recent data on mTOR signaling and novel mTOR inhibitors.
- To discuss the development status of second-generation mTOR inhibitors.
Main Methods:
- Literature review of published data on the mTOR pathway and inhibitors.
- Analysis of preclinical and clinical data on mTOR inhibitors in various tumors.
- Overview of signaling pathways related to mTOR.
Main Results:
- Preclinical data suggest new mTOR inhibitors possess potent antiproliferative activity.
- These novel inhibitors demonstrate a favorable safety profile.
- In preclinical studies, mTOR inhibitors achieved disease stabilization or tumor regression and enhanced other anticancer treatments.
Conclusions:
- Published data on novel mTOR inhibitors are emerging but limited.
- Preclinical results indicate significant potential for new mTOR inhibitors in cancer therapy.
- Further research is warranted to fully elucidate the efficacy and safety of novel mTOR inhibitors in clinical settings.
More Related Videos
05:28A Semi-Quantitative Drug Affinity Responsive Target Stability (DARTS) assay for studying Rapamycin/mTOR interaction
Published on: August 27, 2019
06:51Utilizing 18F-FDG PET/CT Imaging and Quantitative Histology to Measure Dynamic Changes in the Glucose Metabolism in Mouse Models of Lung Cancer
Published on: July 21, 2018
Related Concept Videos
PI3K/mTOR/AKT Signaling Pathway
mTOR Signaling and Cancer Progression
The mTOR pathway or the...
mTOR Signaling and Cancer Progression
The mTOR pathway or the...
Targeted Cancer Therapies
There are several types of targeted therapies against specific...
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include: