Comparative Pharmacology
Head-to-head clinical analysis: TEMSIROLIMUS versus TORISEL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: TEMSIROLIMUS versus TORISEL.
TEMSIROLIMUS vs TORISEL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Temsirolimus is a specific inhibitor of mTOR (mammalian target of rapamycin) kinase. It binds to FKBP-12, and the Temsirolimus-FKBP-12 complex binds to and inhibits mTOR, thereby blocking the translation of cell cycle regulatory proteins (e.g., cyclin D1, c-myc) and hypoxia-inducible factor (HIF) subunits, leading to cell cycle arrest in G1 phase and antiangiogenic effects.
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.
25 mg intravenously over 30-60 minutes once weekly.
25 mg intravenously over 30-60 minutes once weekly.
None Documented
None Documented
Clinical Note
moderateTemsirolimus + Digoxin
"Temsirolimus may decrease the cardiotoxic activities of Digoxin."
Clinical Note
moderateTemsirolimus + Digitoxin
"Temsirolimus may decrease the cardiotoxic activities of Digitoxin."
Clinical Note
moderateTemsirolimus + Deslanoside
"Temsirolimus may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateTemsirolimus + Acetyldigitoxin
"Temsirolimus may decrease the cardiotoxic activities of Acetyldigitoxin."
17.3 hours in patients with advanced solid tumors; range 9-27 hours. Renal impairment (CrCl <30 mL/min) may prolong half-life. No dose adjustment needed for mild-moderate hepatic impairment.
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 via feces (78%) and urine (4.6%) after IV administration; unchanged drug is minimal, with metabolites abundant.
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