Comparative Pharmacology
Head-to-head clinical analysis: LETROZOLE versus TESLAC.
Peer-Reviewed Evidence
Head-to-head clinical analysis: LETROZOLE versus TESLAC.
LETROZOLE vs TESLAC
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Letrozole is a nonsteroidal aromatase inhibitor. It inhibits the aromatase enzyme, which converts androgens to estrogens, thereby reducing estrogen levels in postmenopausal women and suppressing estrogen-dependent tumor growth.
Androgen receptor inhibitor; suppresses gonadotropin secretion and reduces testosterone levels.
2.5 mg orally once daily
250 mg intramuscularly three times per week
None Documented
None Documented
Terminal elimination half-life approximately 45 hours (range 42-52 hours). Steady-state achieved in 2-6 weeks with daily dosing.
Clinical Note
moderateLetrozole + Digoxin
"Letrozole may decrease the cardiotoxic activities of Digoxin."
Clinical Note
moderateLetrozole + Digitoxin
"Letrozole may decrease the cardiotoxic activities of Digitoxin."
Clinical Note
moderateLetrozole + Deslanoside
"Letrozole may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateLetrozole + Acetyldigitoxin
"Letrozole may decrease the cardiotoxic activities of Acetyldigitoxin."
Terminal half-life approximately 2-4 hours; clinical significance: requires multiple daily dosing for steady-state maintenance.
Primarily hepatic metabolism (CYP3A4, CYP2A6) with 90% excreted in urine as metabolites (glucuronide conjugates) and 10% in feces. <6% excreted unchanged in urine.
Renal (primarily as metabolites) and biliary/fecal. The drug is extensively metabolized; less than 5% is excreted unchanged in urine.
Category D/X
Category C
Aromatase Inhibitor
Aromatase Inhibitor