Identification of cis-dichloro-bis-isopropylamine platinum(II) as a major metabolite of iproplatin in humans.
Lakshmi Pendyalaa, J. Wayne Cowens, Girish B. Chheda, Shib P. Dutta, Patrick J. Creaven
- aDepartment of Clinical Pharmacology and Therapeutics, Roswell Park Memorial Institute, Buffalo, New York 14263
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Abstract
Iproplatin is a quadrivalent second-generation platinum complex undergoing clinical evaluation. In plasma and urine of patients receiving this drug, iproplatin- and platinum-containing metabolites of iproplatin were separated by reverse-phase gradient high performance liquid chromatography. One of the metabolites was identified by cochromatography and electron impact mass spectrometry as cis-dichloro-bisisopropylamineplatinum(II), a metabolite formed by reduction of iproplatin. Incubation of iproplatin with ascorbic acid and cysteine, in vitro, indicates that iproplatin can be easily reduced to cis-dichloro-bis-isopropylamineplatinum(II) by reducing agents. It is hypothesized that the reduction of the quadrivalent complex iproplatin to cis-dichloro-bisisopropylamineplatinum(II) occurs intracellularly.
TL;DRIt is hypothesized that the reduction of the quadrivalent second-generation platinum complex iproplatin to cis-dichloro-bisisopropylamineplatinum(II) occurs intracellularly. (Semantic Scholar)