Comparative Pharmacology
Head-to-head clinical analysis: EVEROLIMUS versus TORISEL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EVEROLIMUS versus TORISEL.
EVEROLIMUS vs TORISEL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Everolimus is an inhibitor of mammalian target of rapamycin (mTOR), a serine-threonine kinase. It binds to FKBP-12, forming a complex that inhibits mTOR complex 1 (mTORC1) signaling, reducing cell proliferation, angiogenesis, and glucose uptake.
Temsirolimus, a selective inhibitor of mammalian target of rapamycin (mTOR), forms a complex with FKBP-12, which binds to and inhibits mTOR kinase activity, thereby blocking signaling pathways involved in cell growth, proliferation, and angiogenesis.
10 mg orally once daily for advanced RCC or pancreatic NET; 10 mg orally once daily for subependymal giant cell astrocytoma; 5 mg orally once daily for renal angiomyolipoma. For breast cancer: 10 mg orally once daily with exemestane 25 mg orally daily. For renal transplant rejection prophylaxis: 0.75 mg (maximum 1.5 mg) orally twice daily with cyclosporine and corticosteroids, with therapeutic drug monitoring (trough 3-8 ng/mL).
25 mg intravenously over 30-60 minutes once weekly.
None Documented
None Documented
Clinical Note
moderateEverolimus + Digoxin
"The serum concentration of Digoxin can be increased when it is combined with Everolimus."
Clinical Note
moderateEverolimus + Digitoxin
"Everolimus may decrease the cardiotoxic activities of Digitoxin."
Clinical Note
moderateEverolimus + Deslanoside
"Everolimus may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateEverolimus + Acetyldigitoxin
"Everolimus may decrease the cardiotoxic activities of Acetyldigitoxin."
Terminal half-life ~30 hours (range 26–38 h) in stable renal transplant patients; supports once-daily dosing.
Terminal elimination half-life of temsirolimus is approximately 17.3 hours (range: 11 to 26 hours). For its active metabolite sirolimus, half-life is about 15 hours (range: 10 to 30 hours). Steady-state is reached within 1 week.
Primarily fecal (80%) with 5% renal excretion as metabolites; unchanged drug minimal in urine.
Primarily fecal (78%), with renal elimination accounting for 4.6% of the administered dose. Less than 5% of the dose is excreted unchanged in urine or feces.
Category D/X
Category C
mTOR Inhibitor
mTOR Inhibitor