mTOR inhibitors are a class of drugs that block the mammalian target of rapamycin, a serine or threonine specific protein kinase that regulates cell growth. By targeting the protein's two complexes, mTORC1 and mTORC2, these drugs are used to treat cancer, autoimmune conditions, and neurodegenerative disease. The most established members are the rapalogs, rapamycin and its derivatives, which have shown tumor responses across a range of cancer types in clinical testing. Beyond oncology, mTOR inhibitors are used as immunosuppressants to prevent transplant rejection and have been built into coronary stents to prevent arteries from renarrowing.
Facts
Drug ClassClass of pharmaceutical drugs used to treat cancer, autoimmune disease and neurodegeneration 1 Mechanism of ActionInhibit mTOR, a kinase that regulates cell metabolism, growth and proliferation through the mTORC1 and mTORC2 complexes 1 Approved UseRapamycin is used as an immunosuppressant; other class members are approved for specific cancers such as renal cell carcinoma 1 First Approved / Isolated Year Significant RiskMost frequent adverse events include stomatitis, rash, anemia, fatigue, hyperglycemia or hypertriglyceridemia, decreased appetite, nausea and diarrhea, with interstitial lung disease as a risk of particular concern 1 Classification
Approval StatusInvestigational / Clinical Trial 1 ATC ClassSourced to the subject's own accountL: Antineoplastic and Immunomodulating Agents 2 Connections
Sources
1. mTOR inhibitors (Wikipedia)
Lead section, opening sentence
treat several human diseases, including cancer, autoimmune diseases, and neurodegeneration
Lead section, mTOR description
regulates cellular metabolism, growth, and proliferation by forming and signaling through two protein complexes, mTORC1 and mTORC2
Infobox, class identifiers
Immunosuppression (rapamycin)
History section
was first discovered in 1975 in a soil sample from Easter Island
Adverse events section
Most frequently occurring adverse events are stomatitis, rash, anemia, fatigue, hyperglycemia/hypertriglyceridemia, decreased appetite, nausea, and diarrhea.
Lead section, approval-status statement
The most established mTOR inhibitors are so-called rapalogs (rapamycin and its analogs), which have shown tumor responses in clinical trials against various tumor types.
View the Source2. Anatomical Therapeutic Chemical Classification System (Wikipedia)
WikipediaFirst-level anatomical group codes, Code LQuote, First-level anatomical group codes, Code L
Antineoplastic and immunomodulating agents
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