title: [Lidamycin metabolism in vitro].
abstract: This paper is to report the study of the metabolism of lidamycin in vitro including in plasma and microsomes to guide clinical therapy. Lidamycin was quantified by detecting its active ingredient using HPLC-MS/MS. The metabolic stability of lidamycin in rat, Beagle dog, monkey and human plasma and liver microsomes, and its inhibition to cytochrome P450 isoforms in human liver microsomes were studied. Results showed that lidamycin was metabolized in the four species of plasma, and the sequence of metabolic rates in plasma were in rat > in dog > in human > in monkey. But among the four species of liver microsomes, lidamycin was metabolized only in monkey liver microsomes. There was almost no inhibition to cytochrome P450 isoforms at the concentrations of between 0.0005 and 10 ng x mL(-1). Therefore, the property of lidamycin metabolism in human is similar with that in dog, and metabolism of other drugs would not be decreased by cytochrome P450 as used along with lidamycin in clinic.
authors: Institute of Transfusion Medicine, Academy of Military Medical Sciences, Beijing 100850, China.
authors: Yan-qing
authors: YQ
authors: Wen
authors: Zhi-yun
authors: ZY
authors: Meng
authors: Shu-zhen
authors: SZ
authors: Chen
authors: Xiao-xia
authors: XX
authors: Zhu
authors: Gui-fang
authors: GF
authors: Dou
mesh_terms: D000617:Aminoglycosides / Q000097:blood / Q000378:metabolism*; D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000097:blood / Q000378:metabolism*; D002851:Chromatography, High Pressure Liquid; D019388:Cytochrome P-450 CYP1A2 / Q000378:metabolism; D003577:Cytochrome P-450 Enzyme System / Q000378:metabolism*; D004285:Dogs; D053281:Enediynes / Q000097:blood / Q000378:metabolism*; D004789:Enzyme Activation; D006801:Humans; D008251:Macaca; D008862:Microsomes, Liver / Q000378:metabolism*; D051381:Rats; D053719:Tandem Mass Spectrometry
chemical_list: D000617:Aminoglycosides; D000903:Antibiotics, Antineoplastic; D053281:Enediynes; C058024:C 1027; D003577:Cytochrome P-450 Enzyme System; D019388:Cytochrome P-450 CYP1A2