Tamoxifen and its main metabolites serum and tissue concentrations in breast cancer women

Mario Furlanut, Loretta Franceschi, Enrico Pasqual, Stefano Bacchetti, Donatella Poz, Giorgio Giorda, Pierpaolo Cagol

Research output: Contribution to journalArticle

27 Citations (Scopus)

Abstract

Because of a possible relationship between tamoxifen (T) concentrations and clinical effects, we initiated a preliminary investigation on serum and tissue concentrations of T and its main active metabolites, and 4-hydroxytamoxifen, in women with positive breast cancer estrogen receptor. One hundred forty-eight patients were studied: 80 were admitted for monitoring of therapeutic serum drug concentrations, 22 had tissue concentrations taken at surgery, and 46 patients had uterine mucosa levels measured at diagnostic hysteroscopy. Steady-state serum concentrations were reached after 1 month of continuous treatment, with desmethyltamoxifen being the highest represented derivative from the third week onward. There was no relationship between dose (in mg/kg body weight) and steady-state serum concentrations during therapeutic drug monitoring of patients. The highest tissue concentrations were observed in breast lymph-nodes, cancer tissue, and uterine mucosa. On the basis of these data, we speculate that T and its active metabolites may exert both a defensive role (ie, an obstacle to the diffusion of malignant cells through the local lymphatic system) and a harmful one (induction of uterine malignancies).

Original languageEnglish
Pages (from-to)349-352
Number of pages4
JournalTherapeutic Drug Monitoring
Volume29
Issue number3
DOIs
Publication statusPublished - Jun 2007

Fingerprint

Tamoxifen
Metabolites
Tissue
Breast Neoplasms
Drug Monitoring
Serum
Mucous Membrane
Hysteroscopy
Lymphatic System
Uterine Neoplasms
Monitoring
Estrogen Receptors
Pharmaceutical Preparations
Surgery
Breast
Lymph Nodes
Body Weight
Derivatives
Neoplasms
Therapeutics

Keywords

  • Active metabolites
  • Breast cancer
  • Tamoxifen
  • Tissue concentrations

ASJC Scopus subject areas

  • Toxicology
  • Health, Toxicology and Mutagenesis
  • Pharmacology
  • Biochemistry
  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology (medical)
  • Public Health, Environmental and Occupational Health

Cite this

Tamoxifen and its main metabolites serum and tissue concentrations in breast cancer women. / Furlanut, Mario; Franceschi, Loretta; Pasqual, Enrico; Bacchetti, Stefano; Poz, Donatella; Giorda, Giorgio; Cagol, Pierpaolo.

In: Therapeutic Drug Monitoring, Vol. 29, No. 3, 06.2007, p. 349-352.

Research output: Contribution to journalArticle

Furlanut, Mario ; Franceschi, Loretta ; Pasqual, Enrico ; Bacchetti, Stefano ; Poz, Donatella ; Giorda, Giorgio ; Cagol, Pierpaolo. / Tamoxifen and its main metabolites serum and tissue concentrations in breast cancer women. In: Therapeutic Drug Monitoring. 2007 ; Vol. 29, No. 3. pp. 349-352.
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