Yuichi SUGIYAMA GROUP     SITE

  • Pharmacol Ther. 2021;In press. Consideration of albumin-mediated hepatic uptake for highly protein-bound anionic drugs: Bridging the gap of hepatic uptake clearance between in vitro and in vivo. Miyauchi S, Kim SJ, Lee W, Sugiyama Y. PubMed
  • Nat Rev Drug Discov. 2020;19:801-818. Phase 0/microdosing approaches: time for mainstream application in drug development? Burt T, Young G, Lee W, Kusuhara H, Langer O, Rowland M, Sugiyama Y. PubMed
  • J Pharm Sci. 2021;110:365-375. Transient, tunable expression of NTCP and BSEP in MDCKII cells for kinetic delineation of the rate-determining process and inhibitory effects of Rifampicin in hepatobiliary transport of taurocholate. Ito S, Lee W, Park JE, Yasunaga M, Mori A, Ohtsuki S, Sugiyama Y. PubMed
  • J Pharm Sci. 2021;110:376-387. Evaluation of hepatic uptake of OATP1B substrates by short term-cultured plated human hepatocytes: Comparison with isolated suspended hepatocytes. Yoshikado T, Lee W, Toshimoto K, Morita K, Kiriake A, Chu X, Lee N, Kimoto E, Varma MVS, Kikuchi R, Scialis RJ, Shen H, Ishiguro N, Lotz R, Li AP, Maeda K, Kusuhara H, Sugiyama Y. PubMed
  • AAPS J. 2020;22:133. Cell-to-Medium concentration ratio overshoot in the uptake of statins by human hepatocytes in suspension, but not in monolayer: Kinetic analysis suggesting a partial loss of functional OATP1Bs. Lee W, Koyama S, Morita K, Kiriake A, Kikuchi R, Chu X, Lee N, Scialis RJ, Shen H, Kimoto E, Tremaine L, Ishiguro N, Lotz R, Maeda K, Kusuhara H, Sugiyama Y. PubMed
  • J Pharm Sci. 2021;110:517-528Improved prediction of the drug-drug interactions of pemafibrate caused by cyclosporine A and rifampicin via PBPK modeling: Consideration of the albumin-mediated hepatic uptake of pemafibrate and inhibition constants with preincubation against OATP1B. Park JE, Shitara Y, Lee W, Morita S, Sahi J, Toshimoto K, Sugiyama Y. PubMed
  • J Biol Chem. 2020;295:17349-17364. Post-translational regulation of the major drug transporters in the families of organic anion transporters and organic anion-transporting polypeptides. Lee W, Ha JM, Sugiyama Y. PubMed
  • Clin Pharmacol Ther. 2021;109:55-64. Intestinal P-gp and putative hepatic OATP1B induction: ITC perspective on drug development mplications. Zamek-Gliszczynski MJ, Patel M, Yang X, Lutz JD, Chu X, Brouwer KLR, Lai Y, Lee CA, Neuhoff S, Paine MF, Sugiyama Y, Taskar KS, Galetin A. PubMed
  • Mol Pharm. 2020;17:1884-1898. Practical synthesis of [18F]Pitavastatin and evaluation of hepatobiliary transport activity in rats by Positron Emission Tomography. Nakaoka T, Uetake Y, Kaneko KI, Niwa T, Ochiai H, Irie S, Suezaki Y, Otsuka N, Hayashinaka E, Wada Y, Cui Y, Maeda K, Kusuhara H, Sugiyama Y, Hosoya T, Watanabe Y. PubMed
  • Mol Pharm. 2020;17:722-723. Relative Activity Factor (RAF)-based scaling of uptake clearance mediated by Organic Anion Transporting Polypeptide (OATP) 1B1 and OATP1B3 in human hepatocytes. Izumi S, Nozaki Y, Kusuhara H2, Hotta K, Mochizuki T, Komori T, Maeda K, Sugiyama Y. PubMed
  • Clin Pharmacol Ther. 2020;107:96-101. Expanding precompetitive multisector collaborations to advance drug development and pharmacogenomics. Yee SW, Do TP, Huang SM, Krauss RM, Kusuhara H, Sugiyama Y, Unadkat JD, Giacomini KM. PubMed
  • Expert Opin Drug Metab Toxicol. 2019;15:897-911. Comparative and quantitative assessment on statin efficacy and safety: insights into inter-statin and inter-individual variability via dose- and exposure-response relationships. Iwaki Y, Lee W, Sugiyama Y. PubMed
  • Clin Pharmacol Ther. 2020;107:1082-1115. Physiologically-Based Pharmacokinetic Models for evaluating membrane transporter mediated Drug-Drug Interactions: Current capabilities, case studies, future opportunities, and recommendations. Taskar KS, Pilla Reddy V, Burt H, Posada MM, Varma M, Zheng M, Ullah M, Emami Riedmaier A, Umehara KI, Snoeys J, Nakakariya M, Chu X, Beneton M, Chen Y, Huth F, Narayanan R, Mukherjee D, Dixit V, Sugiyama Y, Neuhoff S. PubMed
  • Clin Pharmacol Ther. 2020;107:1004-1013. Dose-dependent inhibition of OATP1B by Rifampicin in healthy volunteers: Comprehensive evaluation of candidate biomarkers and OATP1B probe drugs. Mori D, Kimoto E, Rago B, Kondo Y, King-Ahmad A, Ramanathan R, Wood LS, Johnson JG, Le VH, Vourvahis M, David Rodrigues A, Muto C, Furihata K, Sugiyama Y, Kusuhara H. PubMed
  • Drug Metab Pharmacokinet. 2019;34:387-395. Microdosing clinical study to clarify pharmacokinetic and pharmacogenetic characteristics of atorvastatin in Japanese hypercholesterolemic patients. Lee N, Maeda K, Fukizawa S, Ieiri I, Tomaru A, Akao H, Takeda K, Iwadare M, Niwa O, Masauji T, Yamane N, Kajinami K, Kusuhara H, Sugiyama Y. PubMed
  • Drug Metab Pharmacokinet. 2019;34:293-299. Quantitative investigation of hepatobiliary transport of [11C]telmisartan in humans by PET imaging. Maeda K, Ohnishi A, Sasaki M, Ikari Y, Aita K, Watanabe Y, Kusuhara H, Sugiyama Y, Senda M. PubMed
  • CPT Pharmacometrics Syst Pharmacol. 2019;8:845-857. Expanded Physiologically-Based Pharmacokinetic Model of Rifampicin for predicting interactions with drugs and an endogenous biomarker via complex mechanisms including Organic Anion Transporting Polypeptide 1B induction. Asaumi R, Menzel K, Lee W, Nunoya KI, Imawaka H, Kusuhara H, Sugiyama Y. PubMed
  • CPT Pharmacometrics Syst Pharmacol. 2019;8:396-406. Physiologically-Based Pharmacokinetic Modeling analysis for quantitative prediction of renal transporter-mediated interactions between Metformin and Cimetidine. Nishiyama K, Toshimoto K, Lee W, Ishiguro N, Bister B, Sugiyama Y. PubMed
  • Drug Metab Pharmacokinet. 2019;34:78-86. Effect of OATP1B1 genotypes on plasma concentrations of endogenous OATP1B1 substrates and drugs, and their association in healthy volunteers. Mori D, Kashihara Y, Yoshikado T, Kimura M, Hirota T, Matsuki S, Maeda K, Irie S, Ieiri I, Sugiyama Y, Kusuhara H. PubMed
  • Drug Metab Dispos. 2019;47:94-103. Extrapolation of in vivo hepatic clearance from in vitro uptake clearance by suspended human hepatocytes for anionic drugs with high binding to human albumin: improvement of in vitro-to-in vivo extrapolation by considering the "albumin-mediated" hepatic uptake mechanism on the basis of the "facilitated-dissociation model". Kim SJ, Lee KR, Miyauchi S, Sugiyama Y. PubMed
  • Clin Pharmacol Ther. 2018;104:836-864. Clinical probes and endogenous biomarkers as substrates for transporter drug-drug interaction evaluation: Perspectives from the International Transporter Consortium. Chu X, Liao M, Shen H, Yoshida K, Zur AA, Arya V, Galetin A, Giacomini KM, Hanna I, Kusuhara H, Lai Y, Rodrigues D, Sugiyama Y, Zamek-Gliszczynski MJ, Zhang L; International Transporter Consortium. PubMed
  • CPT Pharmacometrics Syst Pharmacol. 2018;7:739-747. PBPK Modeling of Coproporphyrin I as an Endogenous Biomarker for Drug Interactions Involving Inhibition of Hepatic OATP1B1 and OATP1B3. Yoshikado T, Toshimoto K, Maeda K, Kusuhara H, Kimoto E, Rodrigues AD, Chiba K, Sugiyama Y. PubMed
  • Clin Pharmacol Ther. 2018;104:865-889. Advancing predictions of tissue and intracellular drug concentrations using in vitro, imaging and PBPK modeling approaches. Guo Y, Chu X, Parrott NJ, Brouwer KLR, Hsu V, Nagar S, Matsson P, Sharma P, Snoeys J, Sugiyama Y1, Tatosian D, Unadkat JD, Huang SM, Galetin A; International Transporter Consortium. PubMed
  • Drug Metab Pharmacokinet. 2018;33:164-172. Total hepatocellular disposition profiling of rosuvastatin and pitavastatin in sandwich-cultured human hepatocytes. Kanda K, Takahashi R, Yoshikado T, Sugiyama Y. PubMed
  • Drug Metab Dispos. 2018;46:924-933. Quantitative analysis of complex drug-drug interactions between Cerivastatin and metabolism/transport inhibitors using physiologically based pharmacokinetic modeling. Yao Y, Toshimoto K, Kim SJ, Yoshikado T, Sugiyama Y. PubMed
  • Clin Pharmacol Ther. 2018;104:803-817. Influence of transporter polymorphisms on drug disposition and response: a perspective from the International Transporter Consortium. Yee SW, Brackman DJ, Ennis EA, Sugiyama Y, Kamdem LK, Blanchard R, Galetin A, Zhang L, Giacomini KM1. PubMed
  • Drug Metab Dispos. 2018;46:719-728. A clinical quantitative evaluation of hepatobiliary transport of [11C]Dehydropravastatin in humans using Positron Emission Tomography. Kaneko K, Tanaka M, Ishii A, Katayama Y, Nakaoka T, Irie S, Kawahata H, Yamanaga T, Wada Y, Miyake T, Toshimoto K, Maeda K, Cui Y, Enomoto M, Kawamura E, Kawada N, Kawabe J, Shiomi S, Kusuhara H, Sugiyama Y, Watanabe Y. PubMed
  • Drug Metab Dispos. 2018;46:652-657. Organic Anion Transporting Polypeptide 1a4 is responsible for the hepatic uptake of cardiac Glycosides in mice. Takano J, Maeda K, Kusuhara H, Sugiyama Y. PubMed
  • Drug Metab Dispos. 2018;46:259-267. The phenomenon of albumin-mediated hepatic uptake of Organic Anion Transport Polypeptide substrates: prediction of the in vivo uptake clearance from the in vitro uptake by isolated hepatocytes using a facilitated-dissociation model. Miyauchi S, Masuda M, Kim SJ, Tanaka Y, Lee KR, Iwakado S, Nemoto M, Sasaki S, Shimono K, Tanaka Y, Sugiyama Y. PubMed
  • Clin Pharmacol Ther. 2018;103:434-448. Endogenous probes for drug transporters: balancing vision with reality. Rodrigues AD, Taskar KS, Kusuhara H, Sugiyama Y. PubMed
  • J Pharm Sci. 2017;106:2345-2356. Possibility of predicting Serotonin transporter occupancy from the in vitro inhibition constant for Serotonin transporter, the clinically relevant plasma concentration of unbound drugs, and their profiles for substrates of transporters. Yahata M, Chiba K, Watanabe T, Sugiyama Y. PubMed
  • J Pharm Sci. 2017;106:2558-2565. Possible role of Organic Cation Transporters in the distribution of [11C]Sulpiride, a dopamine D2 receptor antagonist. Takano H, Ito S, Zhang X, Ito H, Zhang MR, Suzuki H, Maeda K, Kusuhara H, Suhara T, Sugiyama Y. PubMed
  • J Pharm Sci. 2017;106:2739-2750. Quantitative analyses of the influence of parameters governing rate-Determining process of hepatic elimination of drugs on the magnitudes of drug-drug interactions via hepatic OATPs and CYP3A using physiologically based pharmacokinetic models. Yoshikado T, Maeda K, Kusuhara H, Furihata KI, Sugiyama Y. PubMed
  • Drug Metab Dispos. 2017;45:779-789. Comparison of methods for estimating unbound intracellular-to-medium concentration ratios in rat and human hepatocytes using statins. Yoshikado T, Toshimoto K, Nakada T, Ikejiri K, Kusuhara H, Maeda K, Sugiyama Y. PubMed
  • J Pharm Sci. 2017;106:2566-2575. Investigation of the importance of multidrug resistance-associated protein 4 (Mrp4/Abcc4) in the active efflux of anionic drugs across the blood-brain barrier. Kanamitsu K1 Kusuhara H, Schuetz JD, Takeuchi K, Sugiyama Y. PubMed
  • Pharm Res. 2017;34:1584-1600. Virtual clinical studies to examine the probability distribution of the AUC at target tissues using physiologically-based pharmacokinetic modeling: application to analyses of the effect of genetic polymorphism of enzymes and transporters on Irinotecan induced side effects. Toshimoto K, Tomaru A, Hosokawa M, Sugiyama Y. PubMed
  • J Pharm Sci. 2017;106:2688-2694. Small-dosing clinical study: pharmacokinetic, pharmacogenomic (SLCO2B1 and ABCG2), and interaction (Atorvastatin and grapefruit juice) profiles of 5 probes for OATP2B1 and BCRP. Kashihara Y, Ieiri I, Yoshikado T, Maeda K, Fukae M, Kimura M, Hirota T, Matsuki S, Irie S, Izumi N, Kusuhara H, Sugiyama Y. PubMed
  • Pharmacol Ther. 2017;177:67-80. Preincubation-dependent and long-lasting inhibition of organic anion transporting polypeptide (OATP) and its impact on drug-drug interactions. Shitara Y, Sugiyama Y. PubMed
  • J Pharm Sci. 2017;106:2678-2687. Comparison of the predictability of human hepatic clearance for Organic Anion Transporting Polypeptide substrate drugs between different in vitro-in vivo extrapolation approaches. Izumi S, Nozaki Y, Komori T, Takenaka O, Maeda K, Kusuhara H, Sugiyama Y. PubMed
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  • AAPS J. 2017;19:286-297. Pharmacokinetic modeling and Monte Carlo simulation to predict interindividual variability in human exposure to Oseltamivir and its active metabolite, Ro 64-0802. Ito M, Kusuhara H, Ose A, Kondo T, Tanabe K, Nakayama H, Horita S, Fujita T, Sugiyama Y. PubMed
  • Drug Metab Dispos. 2016;44:1925-1933. Investigation of endogenous compounds applicable to drug-drug interaction studies involving the renal Organic Anion Transporters, OAT1 and OAT3, in humans. Tsuruya Y, Kato K, Sano Y, Imamura Y, Maeda K, Kumagai Y, Sugiyama Y, Kusuhara H. PubMed
  • Drug Metab Dispos. 2016;44:1808-1818. The prediction of the relative importance of CYP3A/P-glycoprotein to the nonlinear intestinal absorption of drugs by advanced compartmental absorption and transit model. Takano J, Maeda K, Bolger MB, Sugiyama Y. PubMed
  • J Pharm Sci. 2016;105:2222-30. Development of a support vector machine-based system to predict whether a compound is a substrate of a given drug transporter using its chemical structure. Ose A, Toshimoto K, Ikeda K, Maeda K, Yoshida S, Yamashita F, Hashida M, Ishida T, Akiyama Y, Sugiyama Y. PubMed
  • J Pharm Sci. 2016;105:891-6. Usefulness of a model-based approach for estimating in vitro P-Glycoprotein inhibition potency in a transcellular transport assay. Kishimoto W, Ishiguro N, Ludwig-Schwellinger E, Ebner T, Maeda K, Sugiyama Y. PubMed
  • J Pharm Sci. 2016;105:431-42. Explication of definitional description and empirical use of fraction of orally administered drugs absorbed from the intestine (Fa) and intestinal availability (Fg): effect of P-glycoprotein and CYP3A on Fa and Fg.Tanaka Y, Kitamura Y, Maeda K, Sugiyama Y. PubMed
  • Mol Pharm. 2016;13:438-48. Investigation of fluorescein derivatives as substrates of Organic Anion Transporting Polypeptide (OATP)1B1 to develop sensitive fluorescence-based OATP1B1 Inhibition assays. Izumi S, Nozaki Y, Komori T, Takenaka O, Maeda K, Kusuhara H, Sugiyama Y. PubMed
  • Food Chem Toxicol. 2015;83:229-36. Okadaic acid is taken-up into the cells mediated by human hepatocytes transporter OATP1B3. Ikema S, Takumi S, Maeda Y, Kurimoto T, Bohda S, Chigwechokha PK, Sugiyama Y, Shiozaki K, Furukawa T, Komatsu M. PubMed
  • Environ Toxicol Pharmacol. 2015;39:974-81. Naringin attenuates the cytotoxicity of hepatotoxin microcystin-LR by the curious mechanisms to OATP1B1- and OATP1B3-expressing cells. Takumi S, Ikema S, Hanyu T, Shima Y, Kurimoto T, Shiozaki K, Sugiyama Y, Park HD, Ando S, Furukawa T, Komatsu M. PubMed
  • Pharm Res. 2015;32:2538-47. PET imaging. Quantitative evaluation of mMate1 function based on minimally invasive measurement of tissue concentration using PET with [(11)C]Metformin in mouse. Shingaki T, Hume WE, Takashima T, Katayama Y, Okauchi T, Hayashinaka E, Wada Y, Cui Y, Kusuhara H, Sugiyama Y, Watanabe Y. PubMed
  • Pharm Res. 2015;32:2192-204.  Involvement of organic cation transporters in the clearance and milk secretion of thiamine in mice. Kato K, Moriyama C, Ito N, Zhang X, Hachiuma K, Hagima N, Iwata K, Yamaguchi J, Maeda K, Ito K, Suzuki H, Sugiyama Y, Kusuhara H. PubMed
  • Org Biomol Chem. 2015;13:1113-21. PET imaging. The synthesis of [18F]pitavastatin as a tracer for hOATP using the Suzuki coupling. Yagi Y1, Kimura H, Arimitsu K, Ono M, Maeda K, Kusuhara H, Kajimoto T, Sugiyama Y, Saji H. PubMed
  • J Pediatr. 2014;164:1219-1227.e3. Improved liver function and relieved pruritus after 4-phenylbutyrate therapy in a patient with progressive familial intrahepatic cholestasis type 2. Naoi S, Hayashi H, Inoue T, Tanikawa K, Igarashi K, Nagasaka H, Kage M, Takikawa H, Sugiyama Y, Inui A, Nagai T, Kusuhara H. PubMed
  • Bioorg Med Chem. 2013;21:7584-90. PET imaging. The synthesis and biodistribution of [(11)C]metformin as a PET probe to study hepatobiliary transport mediated by the multi-drug and toxin extrusion transporter 1 (MATE1) in vivo. Hume WE, Shingaki T, Takashima T, Hashizume Y, Okauchi T, Katayama Y, Hayashinaka E, Wada Y, Kusuhara H, Sugiyama Y, Watanabe Y. PubMed
  • J Pharmacol Exp Ther. 2013;347:193-202. PET imaging. Evaluation of Oatp and Mrp2 activities in hepatobiliary excretion using newly developed positron emission tomography tracer [11C]dehydropravastatin in rats. Shingaki T, Takashima T, Ijuin R, Zhang X, Onoue T, Katayama Y, Okauchi T, Hayashinaka E, Cui Y, Wada Y, Suzuki M, Maeda K, Kusuhara H, Sugiyama Y, Watanabe Y. PubMed

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Last update: June 2021