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Clinical Pharmacokinetics of Toremifene

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Abstract

Toremifene is a chlorinated triphenylethylene derivative of tamoxifen approved for use in the treatment of patients with metastatic breast cancer. Toremifene is well tolerated in patients, and common adverse effects of this drag include vasomotor symptoms such as hot flashes and vaginal discharge. This compound is administered to patients orally at a dose of 60 mg/day, although alternative methods of administration have been investigated.

Oral bioavailability is estimated to be approximately 100%. At steady state, toremifene and its metabolites are highly protein bound (>95%). Toremifene is metabolised in the liver by cytochrome P450 enzymes, and it is eliminated primarily in the faeces following enterohepatic circulation. The half-life of toremifene is approximately 5 days, and steady state is reached by 6 weeks depending on the dose given.

The pharmacokinetics of toremifene have been shown to be altered by certain liver conditions, but age and kidney function do not appear to be as significant.

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Acknowledgements

This work was partially supported by National Institutes of Health (NIH) grant 5T32ES07059-NIEHS traineeship, Department of Environmental Toxicology (Tracy L. Taras).

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Authors and Affiliations

  1. Department of Internal Medicine, Division of Hematology/Oncology, Cancer Center, University of California, Davis, 4501 X Street Room 3016, Sacramento, California, 95817, USA

    Tracy L. Taras, Gregory T. Wurz, Gabriel R. Linares &  Michael W. DeGregorio

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  1. Tracy L. Taras
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  2. Gregory T. Wurz
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  3. Gabriel R. Linares
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  4. Michael W. DeGregorio
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Correspondence to Michael W. DeGregorio.

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Taras, T.L., Wurz, G.T., Linares, G.R. et al. Clinical Pharmacokinetics of Toremifene. Clin Pharmacokinet 39, 327–334 (2000). https://doi.org/10.2165/00003088-200039050-00002

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