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Published on: September 13, 2017
Everolimus
1Department Innere Medizin, Klinik für Innere Medizin I, Schwerpunkt Hämatologie, Onkologie und Stammzelltransplantation, Hugstetter Str. 55, 79102, Freiburg, Germany, jens.hasskarl@uniklinik-freiburg.de.
Abstract:
Everolimus (RAD001, Afinitor®) is an oral protein kinase inhibitor of the mammalian target of rapamycin (mTOR) serine/threonine kinase signal transduction pathway. The mTOR pathway regulates cell growth, proliferation, and survival and is frequently deregulated in cancer. Everolimus has been approved by the FDA and the EMA for the treatment of advanced renal cell carcinoma (RCC), subependymal giant cell astrocytoma (SEGA) associated with tuberous sclerosis (TSC), pancreatic neuroendocrine tumors (PNET), in combination with exemestane in advanced hormone-receptor (HR)-positive, HER2-negative breast cancer. Everolimus shows promising clinical activity in additional indications. Multiple phase 2 and phase 3 trials of everolimus alone or in combination are ongoing and will help to further elucidate the role of mTOR in oncology. For a review on everolimus as immunosuppressant, please consult other sources.
Insights
Everolimus is an oral mTOR inhibitor approved for advanced cancers like renal cell carcinoma and breast cancer. Ongoing trials explore its broader role in oncology, targeting cell growth and proliferation pathways.
Area of Science:
- Oncology
- Pharmacology
- Molecular Biology
Background:
- The mammalian target of rapamycin (mTOR) pathway is crucial for cell growth and proliferation.
- Deregulation of the mTOR pathway is common in various cancers.
- Everolimus is an oral mTOR inhibitor targeting this pathway.
Purpose of the Study:
- To summarize the approved indications and ongoing research for everolimus in oncology.
- To highlight the role of mTOR inhibition in cancer treatment.
Main Methods:
- Review of FDA and EMA approved indications for everolimus.
- Summary of ongoing phase 2 and phase 3 clinical trials.
- Focus on everolimus's mechanism as a protein kinase inhibitor.
Main Results:
- Everolimus is approved for advanced renal cell carcinoma, tuberous sclerosis-associated SEGA, pancreatic neuroendocrine tumors, and HR+/HER2- breast cancer.
- The drug demonstrates promising clinical activity in other cancer types.
- Multiple trials are investigating everolimus's efficacy alone and in combination therapies.
Conclusions:
- Everolimus is an established mTOR inhibitor with significant applications in oncology.
- Further clinical trials are essential to fully understand its therapeutic potential in various cancers.
- The mTOR pathway remains a key target for cancer therapy development.
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