51 However, a weak trend toward increase in clearance with lipophilicity in humans has also been noted for 670 intravenously administered drugs and clinical candidates. 52 Herein, a direct correlation between log D 7.4 and intrinsic clearance has been identified in the CYP3A4 substrates, including the marketed drugs that reside in the LipMetE range between 0 and 1 as well as for those substrates that reside in the LipMetE range of >2, as shown in Figure 1 e.
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Lipophilic Metabolic Efficiency (LipMetE) and Drug Efficiency Indices to Explore the Metabolic Properties of the Substrates of Selected Cytochrome P450 Isoforms.
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