Comparative preclinical drug metabolism and pharmacokinetic evaluation of novel 4- aminoquinoline anti-malarials Charles B. Davis, Ramesh Bambal, Ganesh.

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Presentation transcript:

Comparative preclinical drug metabolism and pharmacokinetic evaluation of novel 4- aminoquinoline anti-malarials Charles B. Davis, Ramesh Bambal, Ganesh S. Moorthy, Erin Hugger, Hong Xiang, Brian Kevin Park, Allison E. Shone, Paul M. O’Neill, Stephen A. Ward Journal of Pharmaceutical Sciences Volume 98, Issue 1, Pages 362-377 (January 2009) DOI: 10.1002/jps.21469 Copyright © 2008 Wiley-Liss, Inc. Terms and Conditions

Figure 1 Structure of N-tert-butyl isoquine (NTBI, Panel A), isoquine (ISO, Panel B), des-ethyl isoquine (DEI, Panel C), amodiaquine (ADQ, Panel D), and des-ethyl amodiaquine (DEA, Panel E). Journal of Pharmaceutical Sciences 2009 98, 362-377DOI: (10.1002/jps.21469) Copyright © 2008 Wiley-Liss, Inc. Terms and Conditions

Figure 2 Mean (±SD) plasma concentration versus time profiles after iv (●) or oral (○) administration of NTBI to animals. Panel A: Male CD-1 mice; Panel B: male Sprague–Dawley rats; Panel C: male beagle dogs; Panel D: male Cynomolgus monkeys. Data from the oral legs were dose-normalized for comparison with the iv data. Journal of Pharmaceutical Sciences 2009 98, 362-377DOI: (10.1002/jps.21469) Copyright © 2008 Wiley-Liss, Inc. Terms and Conditions

Figure 3 Linearity of the oral pharmacokinetics of NTBI in mouse (squares), rat (circles) and monkey (triangles). Mean dose-normalized oral AUCs are compared by dose and specie. Filled symbols represent female animals. Rodent exposures represent mean data (n=3) or were derived from composite study designs. Monkey exposures are from individual animals (1M, 1F/group). Journal of Pharmaceutical Sciences 2009 98, 362-377DOI: (10.1002/jps.21469) Copyright © 2008 Wiley-Liss, Inc. Terms and Conditions

Figure 4 Metabolites of NTBI and DEI following incubation with animal and human liver microsomes and hepatocytes in vitro. Solid arrows designate pathways common to both compounds and dashed arrows designate divergent pathways. For both compounds, glucuronidation metabolites of parent, M5 and M6 were detected in liver microsomes and hepatocytes. M1 was detected only with DEI; M7 was detected only with NTBI. Journal of Pharmaceutical Sciences 2009 98, 362-377DOI: (10.1002/jps.21469) Copyright © 2008 Wiley-Liss, Inc. Terms and Conditions