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Pharmacokinetics and Pharmacodynamics of Estramustine Phosphate

  • Review Article
  • Pharmacokinetic-Pharmacodynamic Relationships
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Abstract

Estramustine phosphate (estramustine phosphate sodium), a carbamate ester combining 17β-estradiol and nor-nitrogen mustard, is a cytotoxic drug used in the treatment of advanced prostatic carcinoma. Because of the radiosensitising effect of this drug there has been a recent increase in interest concerning estramustine phosphate and its clinical use. It has also been found that the early recommendations of drug administration together with food or milk were inappropriate, since calcium containing food and antacids hamper drug uptake. This may have obscured results from earlier clinical studies with estramustine phosphate. Estramustine phosphate is currently being re-evaluated for the treatment of other tumours such as glioma and mammary carcinoma.

This review summarises the present relatively limited knowledge concerning the pharmacokinetic and pharmacodynamic aspects of estramustine phosphate and its metabolites.

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  1. Department of Neurosurgery, Umeå University Hospital, Umeå, Sweden

    A. Tommy Bergenheim

  2. Department of Oncology, Umeå University Hospital, S-901 85, Umeå, Sweden

    Roger Henriksson

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  1. A. Tommy Bergenheim
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Bergenheim, A.T., Henriksson, R. Pharmacokinetics and Pharmacodynamics of Estramustine Phosphate. Clin Pharmacokinet 34, 163–172 (1998). https://doi.org/10.2165/00003088-199834020-00004

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