Comparative Pharmacology
Head-to-head clinical analysis: FARESTON versus NOLVADEX.
Peer-Reviewed Evidence
Head-to-head clinical analysis: FARESTON versus NOLVADEX.
FARESTON vs NOLVADEX
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Selective estrogen receptor modulator (SERM) that competitively binds to estrogen receptors, exerting antiestrogenic effects in breast tissue.
NOLVADEX (tamoxifen citrate) is a nonsteroidal selective estrogen receptor modulator (SERM) that competitively inhibits estrogen binding to estrogen receptors in breast tissue, thereby blocking estrogen-mediated cell proliferation. It also has partial agonist activity in other tissues such as bone and endometrium.
60 mg orally once daily.
20-40 mg orally once daily; for breast cancer, 20 mg/day. For adjuvant therapy, 20 mg/day for 5 years. For ductal carcinoma in situ, 20 mg/day for 5 years. For reduction of breast cancer incidence in high-risk women, 20 mg/day for 5 years.
None Documented
None Documented
The terminal elimination half-life of toremifene is approximately 5 days (range 2-10 days). The half-life of its main metabolite, N-desmethyltoremifene, is about 11 days. This long half-life supports once-daily dosing.
Tamoxifen: 5-7 days (terminal). N-desmethyltamoxifen (active metabolite): 14 days. Steady-state achieved in 3-4 weeks.
FARESTON (toremifene) is extensively metabolized in the liver. Excretion is primarily fecal (approximately 70%) with renal excretion accounting for less than 10% of the dose as unchanged drug and metabolites.
Primarily fecal (65%) as conjugates; renal excretion accounts for approximately 25% as metabolites and <0.5% as unchanged drug. Biliary elimination contributes 10%.
Category C
Category C
Selective Estrogen Receptor Modulator
Selective Estrogen Receptor Modulator