Disposition of cisplatin derivatives -3H-cis-1,2-diaminocyclohexanedichloroplatinum (II) and 3H-cis-1,2-diaminocyclohexanemalonatoplatinum (II) in BDF1 mice.
The disposition of 3H-cis-1,2-diaminocyclohexanedichloroplatinum (II) and 3H-cis-1,2-diaminocyclohexanemalonatoplatinum (II) was investigated in P388 tumor-bearing BDF1 mice. Fifteen minutes after IP administration of the drugs, the serum contained 12% of the 3H-chloride derivative and 20% of the malonate derivative. Both drugs distributed to all organs of the body but were not sequestered in any major internal organ. However, substantial amounts of the drugs were found in the carcass and skin. After 24 hr, approximately 43% of the radioactivity was excreted in the urine. Only 5 to 8% of the radioactivity was eliminated in the feces. The radioactivity half-life (t1/2 beta) for the 3H-chloride derivative was estimated from urinary excretion data to be 22.7 hr, and 30.0 hr for the 3H-malonate derivative.
Oswald
C B
CB
Division of Medicinal Chemistry, School of Pharmacy, University of North Carolina, Chapel Hill 27599.
Wyrick
S D
SD
Chaney
S G
SG
Shrewsbury
R O
RO
Hall
I H
IH
D000818:Animals; D000970:Antineoplastic Agents / Q000493:pharmacokinetics*; D001798:Blood Proteins / Q000378:metabolism; D002945:Cisplatin / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D004273:DNA, Neoplasm / Q000378:metabolism; D005243:Feces / Q000032:analysis; D007941:Leukemia P388 / Q000378:metabolism; D051379:Mice; D008815:Mice, Inbred Strains; D009363:Neoplasm Proteins / Q000378:metabolism; D009944:Organoplatinum Compounds / Q000493:pharmacokinetics*; D011485:Protein Binding; D012334:RNA, Neoplasm / Q000378:metabolism; D014018:Tissue Distribution
D000970:Antineoplastic Agents; D001798:Blood Proteins; D004273:DNA, Neoplasm; D009363:Neoplasm Proteins; D009944:Organoplatinum Compounds; D012334:RNA, Neoplasm; C011076:platinum(II) 1,2-diaminocyclohexane malonate; C013933:dichloro-1,2-diaminocyclohexane platinum complex; D002945:Cisplatin