2008
DOI: 10.1016/j.pharmthera.2008.01.006
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In vitro measurements of metabolism for application in pharmacokinetic modeling

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Cited by 107 publications
(68 citation statements)
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“…As noted in Table 3, the fraction of compound unbound to plasma proteins was high except for SF-11. In addition, in vitro intrinsic hepatic clearance (Cl hepatic ) was calculated using methods similar to those described previously (Lipscomb and Poet, 2008). Overall, BIIE0246 had the lowest hepatic clearance; the hepatic clearance of the five HTS-derived antagonists was high except for SF-11 and SF-31, in which it was less than 10 (Table 3).…”
Section: Resultsmentioning
confidence: 99%
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“…As noted in Table 3, the fraction of compound unbound to plasma proteins was high except for SF-11. In addition, in vitro intrinsic hepatic clearance (Cl hepatic ) was calculated using methods similar to those described previously (Lipscomb and Poet, 2008). Overall, BIIE0246 had the lowest hepatic clearance; the hepatic clearance of the five HTS-derived antagonists was high except for SF-11 and SF-31, in which it was less than 10 (Table 3).…”
Section: Resultsmentioning
confidence: 99%
“…To estimate the ability of the liver to remove compounds from the blood in the absence of confounding factors, in vitro intrinsic hepatic clearances were calculated from the microsome and protein plasma binding studies (Lipscomb and Poet, 2008). Studies in mouse, rat, and human microsomes (Table 3) showed that across all species, the antagonists exhibited moderate to low stability (in terms of T 1/2 ) compared with BIIE0246.…”
Section: Discussionmentioning
confidence: 99%
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“…However, several articles relate that for the same CYP450, the activity of rhCYP450 and HLM is not always impacted in the same manner for all substrates. For example, for CYP1A2, Venkatakrishnan and colleagues reported a 4-fold difference in the RAF when comparing methoxyresorufin or phenacetin (Lipscomb & Poet, 2008;Venkatakrishnan et al, 2000). The same phenomenon was identified for CYP2C9 using diclofenac, tolbutamine and Swarfarin (Crewe et al, 2011;Kumar et al, 2006;Locuson et al, 2007) and with CYP3A4, a 2-fold difference between nifedipine and testosterone (Emoto & Iwasaki, 2007;Patki et al, 2003) is evident.…”
Section: Discussionmentioning
confidence: 99%
“…This assumption has been chosen since most of the mathematical models that have been presented to describe the metabolic kinetics of drug during its diffusion through skin follow the first order kinetics as compared to Michaelis-Menten kinetics (Sugibayashi et al, 1999;Sugibayashi, et al 1996;Higuchi et al, 1983). Furthermore, Lipscomb and Poet (2008) concluded that in vivo drug concentration is usually below the Michaelis-Menten constant (Km) which leads to essentially consider the first order kinetics. In particular, the transdermal drug delivery has been reported to follow first order kinetics (Papa et al, 2009;Prodduturi et al 2009;Shakeel et al, 2008).…”
Section: Model Assumptionsmentioning
confidence: 99%