Biodistribution and pharamacokinetics of /sup 195m/Pt-labeled cis-dichlorotrans-dihydroxo-bis(isopropylamine)platinum(IV), CHIP, in normal female Fischer 344 rat

Conference · Sat Jan 01 04:00:00 EST 1983

OSTI ID:5920243

Hoeschele, J D; Ferren, L A; Roberts, J A; Whitfield, L R

The discovery and successful clinical application of the potent anti-tumor compound, cis-Dichlorodiammineplatinum(II), cis-DDP* has stimulated considerable interest in developing effective but less toxic second-generation platinum antitumor drugs. One such candidate drug is cis-Dichloro-trans-dihydroxo-bis-(isopropylamine)platinum(IV), cis-trans-(PtCl/sub 2/(OH)/sub 2/(i-PrNH/sub 2/)/sub 2/), (CHIP). An important feature of this Pt(IV) agent is that in addition to exhibiting a generally milder clinical toxicity than cisplatin, the dose-limiting toxicity of CHIP is the more common myelosuppression rather than the less desirable nephrotoxicity. Also, CHIP has been reported recently to be more effective than cisplatin against both alkylating agent sensitive and resistant strains of the Yoshida sarcoms. A microscale synthesis for /sup 195m/Pt-labelled CHIP and the tissue distribution and pharmacokinetic properties of this agent in normal female Fischer 344 rats are reported. A comparison with similar data for /sup 195m/Pt-cis-DDP is included. (ACR)

• Research Organization: Warner-Lambert Co., Ann Arbor, MI (USA). Parke-Davis Pharmaceutical Research Div.; Oak Ridge National Lab., TN (USA)
• DOE Contract Number: W-7405-ENG-26
• OSTI ID: 5920243
• Report Number(s): CONF-8306109-1; ON: DE83015503
• Country of Publication: United States
• Language: English

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62 RADIOLOGY AND NUCLEAR MEDICINE
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
AMINES
ANIMALS
ANTINEOPLASTIC DRUGS
CHEMICAL PREPARATION
COMPARATIVE EVALUATIONS
COMPLEXES
DAYS LIVING RADIOISOTOPES
DISTRIBUTION
DRUGS
EVEN-ODD NUCLEI
HEAVY NUCLEI
INTERNAL CONVERSION RADIOISOTOPES
ISOMERIC TRANSITION ISOTOPES
ISOTOPES
LABELLED COMPOUNDS
MAMMALS
METABOLISM
NUCLEI
ORGANIC CHLORINE COMPOUNDS
ORGANIC COMPOUNDS
ORGANIC HALOGEN COMPOUNDS
PLATINUM 195
PLATINUM COMPLEXES
PLATINUM ISOTOPES
RADIOISOTOPES
RATS
RODENTS
STABLE ISOTOPES
SYNTHESIS
TISSUE DISTRIBUTION
TRANSITION ELEMENT COMPLEXES
VERTEBRATES