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Clinical pharmacokinetics of toremifene
T L Taras1, G T Wurz, G R Linares
1Department of Internal Medicine, Cancer Center, University of California, Davis, Sacramento 95817, USA.
Clinical Pharmacokinetics
|December 7, 2000
Summary
Toremifene, a tamoxifen derivative, effectively treats metastatic breast cancer with common side effects like hot flashes. This drug is orally administered, well-absorbed, and primarily metabolized by the liver.
Area of Science:
- Oncology
- Pharmacology
- Drug Metabolism
Background:
- Toremifene is a chlorinated triphenylethylene derivative of tamoxifen.
- It is approved for treating patients with metastatic breast cancer.
- Common adverse effects include vasomotor symptoms like hot flashes.
Purpose of the Study:
- To summarize the pharmacokinetic profile of toremifene.
- To describe its metabolism, elimination, and dosing.
- To highlight factors affecting its pharmacokinetics.
Main Methods:
- Review of existing literature on toremifene pharmacokinetics.
- Analysis of absorption, distribution, metabolism, and excretion (ADME) data.
- Assessment of drug interactions and influencing factors.
Main Results:
- Toremifene is orally administered at 60 mg/day with ~100% bioavailability.
- It is highly protein-bound (>95%) and metabolized by cytochrome P450 enzymes.
- Elimination occurs via feces after enterohepatic circulation; half-life is ~5 days.
Conclusions:
- Toremifene is well-tolerated and effectively used for metastatic breast cancer.
- Liver function significantly impacts toremifene pharmacokinetics.
- Age and kidney function have minimal impact on toremifene pharmacokinetics.