-transparent.png){kind=logo}
The metabolism of lovastatin (Mevacor) was examined using isolated microsomes derived from the livers of normal and phenobarbital-treated rats and from human liver samples. Incubation of lovastatin with rat liver microsomes resulted in the formation of several polar metabolites of lovastatin. The metabolites were isolated by HPLC and identified by NMR and mass spectrometry. One fraction consisted of a 2:1 mixture of 6-hydroxy-lovastatin and the rearrangement product delta 4,5-3-hydroxy lovastatin. Addition of a trace of acid to this mixture resulted in the formation of a single aromatized product, the desacyl-delta 4a,6,8-dehydro analog of lovastatin. Another microsomal metabolite was determined to be the delta 4,8a,1-3-hydroxy-lovastatin derivative. The chromatographic pattern of metabolites produced from lovastatin by human liver microsomes was similar to that obtained with rat liver microsomes. Metabolism of lovastatin by rat liver microsomes was both time and concentration dependent; optimal microsomal metabolism occurred with 0.1 mM lovastatin, whereas higher lovastatin concentrations inhibited the reaction. The open acid form of lovastatin was poorly metabolized by both the rat and the human liver microsomes.
M D Greenspan, and
J B Yudkovitz, and
A W Alberts, and
L S Argenbright, and
B H Arison, and
J L Smith
January 1990,
Biochemical pharmacology,
M D Greenspan, and
J B Yudkovitz, and
A W Alberts, and
L S Argenbright, and
B H Arison, and
J L Smith
May 2017,
Planta medica,
M D Greenspan, and
J B Yudkovitz, and
A W Alberts, and
L S Argenbright, and
B H Arison, and
J L Smith
January 1990,
Drug metabolism and disposition: the biological fate of chemicals,
M D Greenspan, and
J B Yudkovitz, and
A W Alberts, and
L S Argenbright, and
B H Arison, and
J L Smith
January 1991,
Drug metabolism and disposition: the biological fate of chemicals,
M D Greenspan, and
J B Yudkovitz, and
A W Alberts, and
L S Argenbright, and
B H Arison, and
J L Smith
February 2005,
Yao xue xue bao = Acta pharmaceutica Sinica,
M D Greenspan, and
J B Yudkovitz, and
A W Alberts, and
L S Argenbright, and
B H Arison, and
J L Smith
March 1982,
Xenobiotica; the fate of foreign compounds in biological systems,
M D Greenspan, and
J B Yudkovitz, and
A W Alberts, and
L S Argenbright, and
B H Arison, and
J L Smith
February 2008,
Drug metabolism and disposition: the biological fate of chemicals,
M D Greenspan, and
J B Yudkovitz, and
A W Alberts, and
L S Argenbright, and
B H Arison, and
J L Smith
April 2014,
Journal of agricultural and food chemistry,
M D Greenspan, and
J B Yudkovitz, and
A W Alberts, and
L S Argenbright, and
B H Arison, and
J L Smith
April 1982,
Xenobiotica; the fate of foreign compounds in biological systems,
M D Greenspan, and
J B Yudkovitz, and
A W Alberts, and
L S Argenbright, and
B H Arison, and
J L Smith
January 2003,
European journal of drug metabolism and pharmacokinetics,
