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

Arch Pharm (Weinheim). 1999 Jun;332(6):195-200. doi: 10.1002/(sici)1521-4184(19996)332:6<195::aid-ardp195>3.0.co;2-h.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

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

Substances

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