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mTOR inhibitors are a class of drugs used to treat several human diseases, including cancer, autoimmune diseases, and neurodegeneration. They function by inhibiting the mammalian target of rapamycin (mTOR) (also known as the mechanistic target of rapamycin), which is a serine/threonine-specific protein kinase that belongs to the family of phosphatidylinositol-3 kinase (PI3K) related kinases ...
GSK2636771 (PIK3CB inhibitor) has undergone several phase II trials as a potential treatment for different cancers, one of which have been completed, with no results published as of March 2022. [85] SF1126 is a peptidic prodrug targeting integrin receptors that converts to LY294002, one of the most widely studied dual PI3K/mTOR inhibitors. [86]
Idelalisib is the first PI3K inhibitor approved by the US Food and Drug Administration and is utilized in the treatment of relapsed/refractory chronic lymphocytic leukemia/small lymphocytic lymphoma and follicular lymphoma. Copanlisib is approved for relapsed follicular lymphoma in patients who have received at least two prior systemic ...
It is the 40-O-(2-hydroxyethyl) derivative of sirolimus and works similarly to sirolimus as an inhibitor of mammalian target of rapamycin (mTOR). [ 12 ] It is marketed by Novartis under the trade names Zortress (US) and Certican (European Union and other countries) in transplantation medicine, and as Afinitor (general tumours) and Votubia ...
Temsirolimus is a specific inhibitor of mTOR and interferes with the synthesis of proteins that regulate proliferation, growth, and survival of tumor cells. Though temsirolimus shows activity on its own, it is also known to be converted to sirolimus (rapamycin) in vivo; [4] therefore, its activity may be more attributed to its metabolite rather than the prodrug itself (despite claims to the ...
The mammalian target of rapamycin (mTOR), [5] also referred to as the mechanistic target of rapamycin, and sometimes called FK506-binding protein 12-rapamycin-associated protein 1 (FRAP1), is a kinase that in humans is encoded by the MTOR gene. [6] [7] [8] mTOR is a member of the phosphatidylinositol 3-kinase-related kinase family of protein ...
Ridaforolimus (also known as AP23573 and MK-8669; formerly known as deforolimus [1]) is an investigational targeted and small-molecule inhibitor of the protein mTOR, a protein that acts as a central regulator of protein synthesis, cell proliferation, cell cycle progression and cell survival, integrating signals from proteins, such as PI3K, AKT and PTEN known to be important to malignancy.
A MEK inhibitor is a chemical or drug that inhibits the mitogen-activated protein kinase enzymes MEK1 and/or MEK2. They can be used to affect the MAPK/ERK pathway which is often overactive in some cancers.