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Updated: Jun 6, 2026

A Semi-Quantitative Drug Affinity Responsive Target Stability (DARTS) assay for studying Rapamycin/mTOR interaction
05:28

A Semi-Quantitative Drug Affinity Responsive Target Stability (DARTS) assay for studying Rapamycin/mTOR interaction

Published on: August 27, 2019

Mammalian target of rapamycin: biological function and target for novel anticancer agents

Emily B Borders1, Cory Bivona, Patrick J Medina

  • 1College of Pharmacy, University of Oklahoma, Oklahoma City, OK 73117, USA. emily-borders@ouhsc.edu

American Journal of Health-System Pharmacy : AJHP : Official Journal of the American Society of Health-System Pharmacists
|December 1, 2010
PubMed
Abstract

Insights

Mammalian target of rapamycin (mTOR) inhibitors like temsirolimus and everolimus show promise in treating advanced renal cell carcinoma (RCC) and other cancers. Monitoring for unique toxicities such as hyperglycemia and pneumonitis is crucial.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • The mammalian target of rapamycin (mTOR) signaling pathway is frequently dysregulated in various cancers, contributing to tumor development, progression, and therapeutic resistance.
  • mTOR plays a critical role in cellular processes including proliferation, survival, and metabolism, making it a key target for anticancer drug development.

Purpose of the Study:

  • To describe the biological function of the mammalian target of rapamycin (mTOR).
  • To review the mechanisms of action of currently available mTOR inhibitors for clinical use.
  • To discuss the efficacy and safety of mTOR inhibitors in various malignancies.

Main Methods:

  • Review of preclinical and clinical data on mTOR inhibitors.
  • Analysis of clinical trial results for temsirolimus and everolimus in renal cell carcinoma (RCC) and other cancers.
  • Summary of common and unique toxicities associated with mTOR inhibitor therapy.

Main Results:

  • Temsirolimus and everolimus are approved for advanced RCC, demonstrating improved survival and progression-free survival (PFS).
  • mTOR inhibitors show potential in combination therapies targeting the phosphatidylinositol 3-kinase (PI3K) pathway in various solid and hematologic tumors.
  • Common toxicities include mucositis, rash, fatigue, and myelosuppression, with unique adverse effects like hyperglycemia, hyperlipidemia, and pneumonitis requiring monitoring.

Conclusions:

  • The mTOR pathway is a validated target in oncology, with approved inhibitors offering therapeutic options for advanced RCC.
  • mTOR inhibitors represent a rational approach for combination therapy due to their role in the PI3K pathway.
  • Careful monitoring for specific adverse events, including metabolic and pulmonary toxicities, is essential for safe and effective use of mTOR inhibitors.

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