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Evaluation of New Chemical Entities as Substrates of Liver Transporters in the Pharmaceutical Industry: Response to Regulatory Requirements and Future.

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Presentation on theme: "Evaluation of New Chemical Entities as Substrates of Liver Transporters in the Pharmaceutical Industry: Response to Regulatory Requirements and Future."— Presentation transcript:

1 Evaluation of New Chemical Entities as Substrates of Liver Transporters in the Pharmaceutical Industry: Response to Regulatory Requirements and Future Steps  Noriko Okudaira  Journal of Pharmaceutical Sciences  Volume 106, Issue 9, Pages (September 2017) DOI: /j.xphs Copyright © 2017 American Pharmacists Association® Terms and Conditions

2 Figure 1 Studies conducted for hepatic transporter substrates during drug discovery and development. Journal of Pharmaceutical Sciences  , DOI: ( /j.xphs ) Copyright © 2017 American Pharmacists Association® Terms and Conditions

3 Figure 2 Total body clearance of bromosulphophthalein (BSP) and statins in rats after a single intravenous administration with and without oral rifampicin (30 mg/kg). Dose of BSP and statins were 3 mg/kg and 1 mg/kg, respectively. Closed bar and open bar represent total body clearance (CLtot) without and with rifampicin, respectively. Data are expressed as mean ± SE (n = 3). **p < 0.01, *p < 0.05. Data were obtained from the study by Imaoka et al.15 Journal of Pharmaceutical Sciences  , DOI: ( /j.xphs ) Copyright © 2017 American Pharmacists Association® Terms and Conditions

4 Figure 3 The hepatic Kp ratios for OATP substrates and non-OATP substrates. Hepatic Kp ratio: The ratio of hepatic Kp to the mean Kp values of adrenal gland, fat, heart, kidney, lung, pancreas, skeletal muscle, skin spleen, and thymus. Data were obtained from the study by Mikkaichi et al.19 Journal of Pharmaceutical Sciences  , DOI: ( /j.xphs ) Copyright © 2017 American Pharmacists Association® Terms and Conditions

5 Figure 4 Media-loss assay and metabolic stability assay for atorvastatin and midazolam in freshly isolated female SD rat hepatocytes. The percentages of each residual compound found at 0.25 min in the media-loss assay with or without 100 μM of rifampicin and at 0 min in the metabolic stability assay are plotted. Average of duplicate assays. Journal of Pharmaceutical Sciences  , DOI: ( /j.xphs ) Copyright © 2017 American Pharmacists Association® Terms and Conditions


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