[meso-1,2-bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamine] sulfatoplatinum(II)--pharmacokinetic studies.

Abstract

The maximally attainable level of the non-plasma protein bound fraction of a single 10.0 mumol/kg i.p. dose of [meso-1,2-bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamine] sulfatoplatinum(II), a drug active on the murine, hormone-sensitive MXT-M-3.2 breast cancer, lies markedly below the concentration causing a significant cytotoxic effect on a cell line derived from this tumor. This result confirms our opinion that the strong in vivo activity of this drug on hormone-sensitive breast cancers is mediated by its estrogenic potency by analogy with high dosed steroidal and non-steroidal estrogens. A specific cytotoxic effect utilizing the estrogen receptor as carrier, as formerly postulated, is unlikely.

• Authors: G Bernhardt, M Koch, T Spruss, R Gust, R Krauser, R Schlemmer, M Hollstein, F Lux, H Schönenberger
• Journal: Archiv der Pharmazie (Arch Pharm (Weinheim)) Vol. 332 Issue 6 Pg. 195-200 (Jun 1999) ISSN: 0365-6233 [Print] Germany
• PMID: 10399488 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Blood Proteins
• Organoplatinum Compounds
• DNA
• dichloro(1,2-bis(4-hydroxyphenyl)ethylenediamine)platinum II
• Cisplatin

Topics

• Animals
• Antineoplastic Agents (pharmacokinetics, pharmacology)
• Blood Proteins (metabolism)
• Cisplatin (pharmacokinetics)
• DNA (metabolism)
• Humans
• Male
• Mice
• Organoplatinum Compounds (pharmacokinetics)
• Protein Binding
• Structure-Activity Relationship