A progress curve mechanistic modeling approach for assessing time - dependent inhibition of CYP 3 A 4 Howard
نویسندگان
چکیده
250 words Introduction: 701 words Discussion: 1500 words Abbreviations used are: DDI, drug-drug interaction; HLM, human liver microsomes; fuinc, fraction unbound in incubation; MBI, mechanism-based inhibition; MIC, metabolite intermediate complex; Km, Michaelis-Menten constant; kinact, inactivation rate constant; KI, irreversible inhibition constant; Ki, reversible inhibition constant. This article has not been copyedited and formatted. The final version may differ from this version. DMD Fast Forward. Published on May 23, 2012 as DOI: 10.1124/dmd.112.046078 at A PE T Jornals on Jne 1, 2017 dm d.aspurnals.org D ow nladed from
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Progress curve mechanistic modeling approach for assessing time-dependent inhibition of CYP3A4.
A progress curve method for assessing time-dependent inhibition of CYP3A4 is based on simultaneous quantification of probe substrate metabolite and inhibitor concentrations during the experiment. Therefore, it may overcome some of the issues associated with the traditional two-step method and estimation of inactivation rate (k(inact)) and irreversible inhibition (K(I)) constants. In the current...
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