Everolimus and temsirolimus

mTOR inhibitors

Everolimus is an oral mTOR inhibitor that acts as an intracellular signal transduction inhibitor in cancer. It is indicated as second line therapy in good- to intermediate risk* metastatic clear cell renal cancer. (* according to Motzer classification) It is given on a once daily continuous schedule.

Temsirolimus is an intravenous mTOR inhibitor that is indicated in first line metastatic setting in poor risk metastatic clear cell renal cancer. It is given in a weekly iv schedule.

 

Inhibition of the protein kinase mTOR results in decreased synthesis of proteins involved in cell division and thus ultimately disturbs cell division.

Main toxicities of both drugs include dyslipidemia (increase in total cholesterol and triglycerides) and for everolimus also mucositis and for temsirolimus also pleural effusion.

See also non-calcineurin agents in the section of Immunology.