[meso-1,2-bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamine] sulfatoplatinum(II)--pharmacokinetic studies.
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.
Lehrstuhl für Pharmazeutische Chemie II, Institut für Pharmazie, Universität Regensburg, Germany.
G
G
Bernhardt
M
M
Koch
T
T
Spruss
R
R
Gust
R
R
Krauser
R
R
Schlemmer
M
M
Hollstein
F
F
Lux
H
H
Schönenberger
D000818:Animals; D000970:Antineoplastic Agents / Q000493:pharmacokinetics* / Q000494:pharmacology; D001798:Blood Proteins / Q000378:metabolism; D002945:Cisplatin / Q000493:pharmacokinetics; D004247:DNA / Q000378:metabolism; D006801:Humans; D008297:Male; D051379:Mice; D009944:Organoplatinum Compounds / Q000493:pharmacokinetics*; D011485:Protein Binding; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D001798:Blood Proteins; D009944:Organoplatinum Compounds; D004247:DNA; C042922:dichloro(1,2-bis(4-hydroxyphenyl)ethylenediamine)platinum II; D002945:Cisplatin