Interspecies scaling of renally secreted drugs
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Preclinical prediction of human pharmacokinetics
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2013, Comprehensive Analytical ChemistryCitation Excerpt :Although from an environmental perspective, oxidative metabolism appears advantageous in terms of generating products with largely reduced biological activity, synthetic strategies rather aim to reduce the relevance of this pathway. Regardless the balance of phase I and phase II metabolism, or combinations thereof, the extent of direct renal or biliary excretion in humans is difficult to predict based on the outcomes of excretion studies in preclinical species [65,66]. Prior to selecting drug candidates for development, mass balance studies are conducted in animals by collecting urine and feces (or preferably of bile if bile duct ligation is technically feasible) following intravenous bolus administration.
Preclinical Prediction of Human Pharmacokinetics
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