Publications after 2012

2017

Involvement of Organic Cation Transporters in the Kinetics of Trimethylamine N-oxide.

Miyake T, Mizuno T, Mochizuki T, Kimura M, Matsuki S, Irie S, Ieiri I, Maeda K, Kusuhara H. J Pharm Sci. 2017 Sep;106(9):2542-2550. doi: 10.1016/j.xphs.2017.04.067. Epub 2017 May 4.
Pubmed DOI

Cyclosporin derivatives inhibit hepatitis B virus entry without interfering with NTCP transporter activity.

Shimura S, Watashi K, Fukano K, Peel M, Sluder A, Kawai F, Iwamoto M, Tsukuda S, Takeuchi JS, Miyake T, Sugiyama M, Ogasawara Y, Park SY, Tanaka Y, Kusuhara H, Mizokami M, Sureau C, Wakita T. J Hepatol. 2017 Apr;66(4):685-692. doi: 10.1016/j.jhep.2016.11.009. Epub 2016 Nov 25.
Pubmed DOI

2016

Pim-1L Protects Cell Surface-Resident ABCA1 From Lysosomal Degradation in Hepatocytes and Thereby Regulates Plasma High-Density Lipoprotein Level.

Katsube A, Hayashi H, Kusuhara H. Arterioscler Thromb Vasc Biol. 2016 Dec;36(12):2304-2314.
Pubmed DOI

Review

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. J Pharm Sci. 2016;105(2):431-42.
Pubmed DOI

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. Drug Metab Dispos. 2016;44(12):1925-1933.
Pubmed DOI

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. Drug Metab Dispos. 2016;44(11):1808-1818.
Pubmed DOI

Analysis of Mechanism-Based Inhibition of CYP 3A4 by a Series of Fluoroquinolone Antibacterial Agents.

Watanabe A, Takakusa H, Kimura T, Inoue S, Kusuhara H, Ando O. Drug Metab Dispos. 2016;44(10):1608-16.
Pubmed DOI

Clarification of the Mechanism of Clopidogrel-Mediated Drug-Drug Interaction in a Clinical Cassette Small-dose Study and Its Prediction Based on In Vitro Information.

Kim SJ, Yoshikado T, Ieiri I, Maeda K, Kimura M, Irie S, Kusuhara H, Sugiyama Y. Drug Metab Dispos. 2016;44(10):1622-32.
Pubmed DOI

Impact of Experimental Conditions on the Evaluation of Interactions between Multidrug and Toxin Extrusion Proteins and Candidate Drugs.

Lechner C, Ishiguro N, Fukuhara A, Shimizu H, Ohtsu N, Takatani M, Nishiyama K, Washio I, Yamamura N, Kusuhara H. Drug Metab Dispos. 2016;44(8):1381-9.
Pubmed DOI

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. J Pharm Sci. 2016;105(7):2222-30.
Pubmed DOI

Quantitative Analyses of Hepatic OATP-Mediated Interactions Between Statins and Inhibitors Using PBPK Modeling With a Parameter Optimization Method.

Yoshikado T, Yoshida K, Kotani N, Nakada T, Asaumi R, Toshimoto K, Maeda K, Kusuhara H, Sugiyama Y. Clin Pharmacol Ther. 2016;100(5):513-523.
Pubmed DOI

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. J Pharm Sci. 2016;105(2):891-6.
Pubmed DOI

Effects of 4-phenylbutyrate therapy in a preterm infant with cholestasis and liver fibrosis.

Ito S, Hayashi H, Sugiura T, Ito K, Ueda H, Togawa T, Endo T, Tanikawa K, Kage M, Kusuhara H, Saitoh S. Pediatr Int. 2016;58(6):506-509.
Pubmed DOI

Investigation of utility of cerebrospinal fluid drug concentration as a surrogate for interstitial fluid concentration using microdialysis coupled with cisternal cerebrospinal fluid sampling in wild-type and Mdr1a(-/-) rats.

Nagaya Y, Nozaki Y, Takenaka O, Watari R, Kusano K, Yoshimura T, Kusuhara H. Drug Metab Pharmacokinet. 2016;31(1):57-66.
Pubmed DOI

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. Mol Pharm. 2016;13(2):438-48.
Pubmed DOI

Successful treatment with 4-phenylbutyrate in a patient with benign recurrent intrahepatic cholestasis type 2 refractory to biliary drainage and bilirubin absorption.

Hayashi H, Naoi S, Hirose Y, Matsuzaka Y, Tanikawa K, Igarashi K, Nagasaka H, Kage M, Inui A, Kusuhara H. Hepatol Res. 2016;46(2):192-200.
Pubmed DOI

2015

Impaired Hepatic Uptake by Organic Anion-Transporting Polypeptides Is Associated with Hyperbilirubinemia and Hypercholanemia in Atp11c Mutant Mice.

Matsuzaka Y, Hayashi H, Kusuhara H. Mol Pharmacol. 2015;88(6):1085-92.
Pubmed DOI

A clinical pharmacokinetic microdosing study of docetaxel with Japanese patients with cancer.

Fujita K, Yoshino E, Kawara K, Maeda K, Kusuhara H, Sugiyama Y, Yokoyama T, Kaneta T, Ishida H, Sasaki Y. Cancer Chemother Pharmacol. 2015;76(4):793-801.
Pubmed DOI

Effect of Knockout of Mdr1a and Mdr1b ABCB1 Genes on the Systemic Exposure of a Doxorubicin-Conjugated Block Copolymer in Mice.

Sakai-Kato K, Nanjo K, Kusuhara H, Nishiyama N, Kataoka K, Kawanishi T, Okuda H, Goda Y. Mol Pharm. 2015;12(9):3175-83.
Pubmed DOI

Molecular characterization and pathogenicity of a genogroup GVI feline norovirus.

Takano T, Kusuhara H, Kuroishi A, Takashina M, Doki T, Nishinaka T, Hohdatsu T. Vet Microbiol. 2015;178(3-4):201-7.
Pubmed DOI

Solute Carrier Family of the Organic Anion-Transporting Polypeptides 1A2- Madin-Darby Canine Kidney II: A Promising In Vitro System to Understand the Role of Organic Anion-Transporting Polypeptide 1A2 in Blood-Brain Barrier Drug Penetration.

Liu H, Yu N, Lu S, Ito S, Zhang X, Prasad B, He E, Lu X, Li Y, Wang F, Xu H, An G, Unadkat JD, Kusuhara H, Sugiyama Y, Sahi J. Drug Metab Dispos. 2015;43(7):1008-18.
Pubmed DOI

Effects of Cremophor EL on the absorption of orally administered saquinavir and fexofenadine in healthy subjects.

Tomaru A, Takeda-Morishita M, Maeda K, Banba H, Takayama K, Kumagai Y, Kusuhara H, Sugiyama Y. Drug Metab Pharmacokinet. 2015;30(3):221-6.
Pubmed DOI

Cellular Cholesterol Accumulation Facilitates Ubiquitination and Lysosomal Degradation of Cell Surface-Resident ABCA1.

Mizuno T, Hayashi H, Kusuhara H. Arterioscler Thromb Vasc Biol. 2015;35(6):1347-56.
Pubmed DOI

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. Pharm Res. 2015;32(8):2538-47.
Pubmed DOI

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. Pharm Res. 2015;32(7):2192-204.
Pubmed DOI

Quantitative Analysis of the ABCG2 c.421C>A Polymorphism Effect on In Vivo Transport Activity of Breast Cancer Resistance Protein (BCRP) Using an Intestinal Absorption Model.

Tanaka Y, Kitamura Y, Maeda K, Sugiyama Y. J Pharm Sci. 2015;104(9):3039-48.
Pubmed DOI

The synthesis of [18F]pitavastatin as a tracer for hOATP using the Suzuki coupling.

Yagi Y, Kimura H, Arimitsu K, Ono M, Maeda K, Kusuhara H, Kajimoto T, Sugiyama Y, Saji H. Org Biomol Chem. 2015;13(4):1113-21.
Pubmed DOI

Investigation of the impact of substrate selection on in vitro organic anion transporting polypeptide 1B1 inhibition profiles for the prediction of drug-drug interactions.

Izumi S, Nozaki Y, Maeda K, Komori T, Takenaka O, Kusuhara H, Sugiyama Y. Drug Metab Dispos. 2015;43(2):235-47.
Pubmed DOI

2014

In silico prediction of major drug clearance pathways by support vector machines with feature-selected descriptors.

Toshimoto K, Wakayama N, Kusama M, Maeda K, Sugiyama Y and Akiyama Y. Drug Metab Dispos 2014;42(11):1811-9.
Pubmed DOI

Kinetic Interpretation of the Importance of OATP1B3 and MRP2 in Docetaxel-Induced Hematopoietic Toxicity.

Yamada A, Maeda K, Kiyotani K, Mushiroda T, Nakamura Y and Sugiyama Y. CPT Pharmacometrics Syst Pharmacol 2014;3:e126.
Pubmed DOI

Utility of Cerebrospinal Fluid Drug Concentration as a Surrogate for Unbound Brain Concentration in Nonhuman Primates.

Nagaya Y, Nozaki Y, Kobayashi K, Takenaka O, Nakatani Y, Kusano K, Yoshimura T, Kusuhara H.
Drug Metab Pharmacokinet. 2014;29(5):419-26.
Pubmed DOI

Effects of one-time apple juice ingestion on the pharmacokinetics of fexofenadine enantiomers.

Akamine Y, Miura M, Komori H, Saito S, Kusuhara H, Tamai I, Ieiri I, Uno T, Yasui-Furukori N.
Eur J Clin Pharmacol. 2014;70(9):1087-95.
Pubmed DOI

Intractable itch relieved by 4-phenylbutyrate therapy in patients with progressive familial intrahepatic cholestasis type 1.

Hasegawa Y, Hayashi H, Naoi S, Kondou H, Bessho K, Igarashi K, Hanada K, Nakao K, Kimura T, Konishi A, Nagasaka H, Miyoshi Y, Ozo no K, Kusuhara H. Orphanet J Rare Dis. 2014;9:89.
Pubmed DOI

Evaluation of [(11)C]oseltamivir uptake into the brain during immune activation by systemic polyinosine-polycytidylic acid injection: a quantitative PET study using juvenile monkey models of viral infection.

Seki C, Oh-Nishi A, Nagai Y, Minamimoto T, Obayashi S, Higuchi M, Takei M, Furutsuka K, Ito T, Zhang MR, Ito H, Ito M, Ito S, Kusuhara H, Sugiyama Y, Suhara T. EJNMMI Res. 2014;4:24.
Pubmed DOI

How far should we go? Perspective of drug-drug interaction studies in drug development.

Kusuhara H. Drug Metab Pharmacokinet. 2014;29(3):227-8.
Pubmed DOI

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. J Pediatr. 2014;164(5):1219-1227.e3.
Pubmed DOI picture

Inhibitory effects of p-aminohippurate and probenecid on the renal clearance of adefovir and benzylpenicillin as probe drugs for organic anion transporter (OAT) 1 and OAT3 in humans.

Maeda K, Tian Y, Fujita T, Ikeda Y, Kumagai Y, Kondo T, Tanabe K, Nakayama H, Horita S, Kusuhara H, Sugiyama Y. Eur J Pharm Sci. 2014;59:94-103.
Pubmed DOI

Quantitative investigation of the brain-to-cerebrospinal fluid unbound drug concentration ratio under steady-state conditions in rats using a pharmacokinetic model and scaling factors for active efflux transporters.

Kodaira H, Kusuhara H, Fuse E, Ushiki J, Sugiyama Y. Drug Metab Dispos. 2014;42(6):983-9.
Pubmed DOI

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. J Pediatr. 2014;164(5):1219-1227.e3.
Pubmed DOI

6β-Hydroxycortisol is an endogenous probe for evaluation of drug-drug interactions involving a multispecific renal organic anion transporter, OAT3/SLC22A8, in healthy subjects.

Imamura Y, Tsuruya Y, Damme K, Heer D, Kumagai Y, Maeda K, Murayama N, Okudaira N, Kurihara A, Izumi T, Sugiyama Y, Kusuhara H. Drug Metab Dispos. 2014;42(4):685-94.
Pubmed DOI

Evaluation of the potency of telaprevir and its metabolites as inhibitors of renal organic cation transporters, a potential mechanism for the elevation of serum creatinine.

Nakada T, Kito T, Inoue K, Masuda S, Inui K, Matsubara K, Moriyama Y, Hisanaga N, Adachi Y, Suzuki M, Yamada I, Kusuhara H. Drug Metab Pharmacokinet. 2014;29(3):266-71.
Pubmed

Differential roles of ubiquitination in the degradation mechanism of cell surface-resident bile salt export pump and multidrug resistance-associated protein 2.

Aida K, Hayashi H, Inamura K, Mizuno T, Sugiyama Y. Mol Pharmacol. 2014;85(3):482-91.
Pubmed DOI

Cyclosporin A and its analogs inhibit hepatitis B virus entry into cultured hepatocytes through targeting a membrane transporter, sodium taurocholate cotransporting polypeptide (NTCP).

Watashi K, Sluder A, Daito T, Matsunaga S, Ryo A, Nagamori S, Iwamoto M, Nakajima S, Tsukuda S, Borroto-Esoda K, Sugiyama M, Tanaka Y, Kanai Y, Kusuhara H, Mizokami M, Wakita T. Hepatology. 2014;59(5):1726-37.
Pubmed DOI

Evaluation and identification of hepatitis B virus entry inhibitors using HepG2 cells overexpressing a membrane transporter NTCP.

Iwamoto M, Watashi K, Tsukuda S, Aly HH, Fukasawa M, Fujimoto A, Suzuki R, Aizaki H, Ito T, Koiwai O, Kusuhara H, Wakita T. Biochem Biophys Res Commun. 2014;443(3):808-13.
Pubmed DOI

Elucidating the molecular mechanism for the intracellular trafficking and fate of block copolymer micelles and their components.

Sakai-Kato K, Un K, Nanjo K, Nishiyama N, Kusuhara H, Kataoka K, Kawanishi T, Goda Y, Okuda H. Biomaterials. 2014;35(5):1347-58.
Pubmed DOI

Investigation of endogenous compounds for assessing the drug interactions in the urinary excretion involving multidrug and toxin extrusion proteins.

Kato K, Mori H, Kito T, Yokochi M, Ito S, Inoue K, Yonezawa A, Katsura T, Kumagai Y, Yuasa H, Moriyama Y, Inui K, Kusuhara H, Sugiyama Y. Pharm Res. 2014;31(1):136-47.
Pubmed DOI

Book

トランスポーターと疾患研究の最前線(別冊・医学のあゆみ)

楠原洋之 編集 医歯薬出版株式会社

2013

Book chapter

In vivo characterization of interactions on transporters. In Transporters in Drug Development (Sugiyama Y and Steffansen B eds)

Kusuhara H, Yoshida K and Sugiyama Y. pp 67-98, Springer, New York, 2013.

Book chapter

Prediction of hepatic transporter-mediated drug-drug interaction from in vitro data. In Transporters in Drug Development (Sugiyama Y and Steffansen B eds)

Maeda K and Sugiyama Y. pp 121-154, Springer, New York, 2013

Evaluation of the potency of telaprevir and its metabolites as inhibitors of renal organic cation transporters, a potential mechanism for elevation of serum creatinine.

Nakada T, Kito T, Inoue K, Masuda S, Inui KI, Matsubara K, Moriyama Y, Hisanaga N, Adachi Y, Suzuki M, Yamada I, Kusuhara H. Drug Metab Pharmacokinet. 2013 [Epub ahead of print]
Pubmed DOI

Review

Transporter biology in drug approval: regulatory aspects.

Maeda K, Sugiyama Y. Mol Aspects Med. 2013;34(2-3):711-8.
Pubmed DOI

Review

Ethnic variability in the plasma exposures of OATP1B1 substrates such as HMG-CoA reductase inhibitors: a kinetic consideration of its mechanism.

Tomita Y, Maeda K, Sugiyama Y. Clin Pharmacol Ther. 2013;94(1):37-51.
Pubmed DOI

Review

Hepatic and intestinal drug transporters: prediction of pharmacokinetic effects caused by drug-drug interactions and genetic polymorphisms.

Yoshida K, Maeda K, Sugiyama Y. Annu Rev Pharmacol Toxicol. 2013;53:581-612.
Pubmed DOI

Review

Clinical significance of organic anion transporting polypeptides (OATPs) in drug disposition: their roles in hepatic clearance and intestinal absorption.

Shitara Y, Maeda K, Ikejiri K, Yoshida K, Horie T, Sugiyama Y. Biopharm Drug Dispos. 2013;34(1):45-78.
Pubmed DOI

Review

Imaging in the study of membrane transporters.

Kusuhara H. Clin Pharmacol Ther. 2013;94(1):33-6.
Pubmed DOI

Review

Bile salt export pump (BSEP/ABCB11): trafficking and sorting disturbances.

Hayashi H, Sugiyama Y. Curr Mol Pharmacol. 2013;6(2):95-103.
Pubmed

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. Bioorg Med Chem. 2013;21(24):7584-90.
Pubmed DOI

Automated extraction of information on chemical-P-glycoprotein interactions from the literature.

Yoshida S, Yamashita F, Ose A, Maeda K, Sugiyama Y, Hashida M. J Chem Inf Model. 2013;53(10):2506-10.
Pubmed DOI

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. J Pharmacol Exp Ther. 2013;347(1):193-202.
Pubmed DOI

Substrate-dependent inhibition of organic anion transporting polypeptide 1B1: comparative analysis with prototypical probe substrates estradiol-17β-glucuronide, estrone-3-sulfate, and sulfobromophthalein.

Izumi S, Nozaki Y, Komori T, Maeda K, Takenaka O, Kusano K, Yoshimura T, Kusuhara H, Sugiyama Y. Drug Metab Dispos. 2013;41(10):1859-66.
Pubmed DOI

Epigenetic regulation of organic anion transporting polypeptide 1B3 in cancer cell lines.

Imai S, Kikuchi R, Tsuruya Y, Naoi S, Nishida S, Kusuhara H, Sugiyama Y. Pharm Res. 2013;30(11):2880-90.
Pubmed DOI

Investigation of the effect of the uneven distribution of CYP3A4 and P-glycoprotein in the intestine on the barrier function against xenobiotics: a simulation study.

Watanabe T, Maeda K, Nakai C, Sugiyama Y. J Pharm Sci. 2013;102(9):3196-204.
Pubmed DOI

Microdose pharmacogenetic study of 1?C-tolbutamide in healthy subjects with accelerator mass spectrometry to examine the effects of CYP2C9?3 on its pharmacokinetics and metabolism.

Ikeda T, Aoyama S, Tozuka Z, Nozawa K, Hamabe Y, Matsui T, Kainuma M, Hasegawa S, Maeda K, Sugiyama Y. Eur J Pharm Sci. 2013;49(4):642-8.
Pubmed DOI

Investigation of the role of transporters on the hepatic elimination of an LAT1 selective inhibitor JPH203.

Toyoshima J, Kusuhara H, Wempe MF, Endou H, Sugiyama Y. J Pharm Sci. 2013;102(9):3228-38.
Pubmed DOI

Investigation of the effect of active efflux at the blood-brain barrier on the distribution of nonsteroidal aromatase inhibitors in the central nervous system.

Miyajima M, Kusuhara H, Takahashi K, Takashima T, Hosoya T, Watanabe Y, Sugiyama Y. J Pharm Sci. 2013;102(9):3309-19.
Pubmed DOI

Relationship between the urinary excretion mechanisms of drugs and their physicochemical properties.

Ito S, Ando H, Ose A, Kitamura Y, Ando T, Kusuhara H, Sugiyama Y. J Pharm Sci. 2013;102(9):3294-301.
Pubmed DOI

Involvement of carnitine/organic cation transporter OCTN1/SLC22A4 in gastrointestinal absorption of metformin.

Nakamichi N, Shima H, Asano S, Ishimoto T, Sugiura T, Matsubara K, Kusuhara H, Sugiyama Y, Sai Y, Miyamoto K, Tsuji A, Kato Y. J Pharm Sci. 2013;102(9):3407-17.
Pubmed DOI

Drugs interacting with organic anion transporter-1 affect uptake of Tc-99m-mercaptoacetyl-triglycine (MAG3) in the human kidney: therapeutic drug interaction in Tc-99m-MAG3 diagnosis of renal function and possible application of Tc-99m-MAG3 for drug development.

Takahara N, Saga T, Inubushi M, Kusuhara H, Seki C, Ito S, Oyama N, Yokoyama O, Sugiyama Y, Fujibayashi Y. Nucl Med Biol. 2013;40(5):643-50.
Pubmed DOI

Direct and rapid genotyping of SLCO1B1 388A>G and 521T>C in human blood specimens using the SmartAmp-2 method.

Yoshida K, Takano J, Ishizu Y, Lezhava A, Ieiri I, Maeda K, Hayashizaki Y, Sugiyama Y. AAPS J. 2013;15(2):618-22.
Pubmed DOI

Mechanisms of pharmacokinetic enhancement between ritonavir and saquinavir; micro/small dosing tests using midazolam (CYP3A4), fexofenadine (p-glycoprotein), and pravastatin (OATP1B1) as probe drugs.

Ieiri I, Tsunemitsu S, Maeda K, Ando Y, Izumi N, Kimura M, Yamane N, Okuzono T, Morishita M, Kotani N, Kanda E, Deguchi M, Matsuguma K, Matsuki S, Hirota T, Irie S, Kusuhara H, Sugiyama Y. J Clin Pharmacol. 2013;53(6):654-61.
Pubmed DOI

Evaluation of breast cancer resistance protein function in hepatobiliary and renal excretion using PET with 11C-SC-62807.

Takashima T, Wu C, Takashima-Hirano M, Katayama Y, Wada Y, Suzuki M, Kusuhara H, Sugiyama Y, Watanabe Y. J Nucl Med. 2013;54(2):267-76.
Pubmed DOI

Effect of coadministration of single and multiple doses of rifampicin on the pharmacokinetics of fexofenadine enantiomers in healthy subjects.

Kusuhara H, Miura M, Yasui-Furukori N, Yoshida K, Akamine Y, Yokochi M, Fukizawa S, Ikejiri K, Kanamitsu K, Uno T, Sugiyama Y. Drug Metab Dispos. 2013;41(1):206-13.
Pubmed DOI

Effect of the fluoroquinolone antibacterial agent DX-619 on the apparent formation and renal clearances of 6β-hydroxycortisol, an endogenous probe for CYP3A4 inhibition, in healthy subjects.

Imamura Y, Murayama N, Okudaira N, Kurihara A, Inoue K, Yuasa H, Izumi T, Kusuhara H, Sugiyama Y. Pharm Res. 2013;30(2):447-57.
Pubmed DOI

DNA methylation and histone modification profiles of mouse organic anion transporting polypeptides.

Imai S, Kikuchi R, Kusuhara H, Sugiyama Y. Drug Metab Dispos. 2013;41(1):72-8.
Pubmed DOI

Cost-effectiveness analysis of microdose clinical trials in drug development.

Yamane N, Igarashi A, Kusama M, Maeda K, Ikeda T, Sugiyama Y. Drug Metab Pharmacokinet. 2013;28(3):187-95.
Pubmed

Studies on the intestinal absorption characteristics of sulfasalazine, a breast cancer resistance protein (BCRP) substrate.

Tomaru A, Morimoto N, Morishita M, Takayama K, Fujita T, Maeda K, Kusuhara H, Sugiyama Y. Drug Metab Pharmacokinet. 2013;28(1):71-4.
Pubmed

2012

N-methylnicotinamide is an endogenous probe for evaluation of drug-drug interactions involving multidrug and toxin extrusions (MATE1 and MATE2-K).

Ito S, Kusuhara H, Kumagai Y, Moriyama Y, Inoue K, Kondo T, Nakayama H, Horita S, Tanabe K, Yuasa H, Sugiyama Y. Clin Pharmacol Ther. 2012;92(5):635-41.
Pubmed DOI

Pharmacogenomic/pharmacokinetic assessment of a four-probe cocktail for CYPs and OATPs following oral microdosing.

Ieiri I, Fukae M, Maeda K, Ando Y, Kimura M, Hirota T, Nakamura T, Iwasaki K, Matsuki S, Matsuguma K, Kanda E, Deguchi M, Irie S, Sugiyama Y. Int J Clin Pharmacol Ther. 2012;50(10):689-700.
Pubmed DOI

E297G mutated bile salt export pump (BSEP) function enhancers derived from GW4064: structural development study and separation from farnesoid X receptor-agonistic activity.

Misawa T, Hayashi H, Makishima M, Sugiyama Y, Hashimoto Y. Bioorg Med Chem Lett. 2012;22(12):3962-6.
Pubmed DOI

Transporter-mediated drug--drug interactions involving OATP substrates: predictions based on in vitro inhibition studies.

Yoshida K, Maeda K, Sugiyama Y. Clin Pharmacol Ther. 2012;91(6):1053-64.
Pubmed DOI

PET imaging-based evaluation of hepatobiliary transport in humans with (15R)-11C-TIC-Me.

Takashima T, Kitamura S, Wada Y, Tanaka M, Shigihara Y, Ishii H, Ijuin R, Shiomi S, Nakae T, Watanabe Y, Cui Y, Doi H, Suzuki M, Maeda K, Kusuhara H, Sugiyama Y, Watanabe Y. J Nucl Med. 2012;53(5):741-8.
Pubmed DOI

Discovery and structural development of small molecules that enhance transport activity of bile salt export pump mutant associated with progressive familial intrahepatic cholestasis type 2.

Misawa T, Hayashi H, Sugiyama Y, Hashimoto Y. Bioorg Med Chem. 2012;20(9):2940-9.
Pubmed DOI

Whole-body distribution and radiation dosimetry of [11C]telmisartan as a biomarker for hepatic organic anion transporting polypeptide (OATP) 1B3.

Shimizu K, Takashima T, Yamane T, Sasaki M, Kageyama H, Hashizume Y, Maeda K, Sugiyama Y, Watanabe Y, Senda M. Nucl Med Biol. 2012;39(6):847-53.
Pubmed DOI

Sorting nexin 27 interacts with multidrug resistance-associated protein 4 (MRP4) and mediates internalization of MRP4.

Hayashi H, Naoi S, Nakagawa T, Nishikawa T, Fukuda H, Imajoh-Ohmi S, Kondo A, Kubo K, Yabuki T, Hattori A, Hirouchi M, Sugiyama Y. J Biol Chem. 2012;287(18):15054-65.
Pubmed DOI

Association of multidrug resistance-associated protein 2 single nucleotide polymorphism rs12762549 with the basal plasma levels of phase II metabolites of isoflavonoids in healthy Japanese individuals.

Kato K, Kusuhara H, Kumagai Y, Ieiri I, Mori H, Ito S, Nakai Y, Maeda K, Sugiyama Y. Pharmacogenet Genomics. 2012;22(5):344-54.
Pubmed DOI

Pharmacokinetic interaction study of sulphasalazine in healthy subjects and the impact of curcumin as an in vivo inhibitor of BCRP.

Kusuhara H, Furuie H, Inano A, Sunagawa A, Yamada S, Wu C, Fukizawa S, Morimoto N, Ieiri I, Morishita M, Sumita K, Mayahara H, Fujita T, Maeda K, Sugiyama Y. Br J Pharmacol. 2012;166(6):1793-803.
Pubmed DOI

AP2 adaptor complex mediates bile salt export pump internalization and modulates its hepatocanalicular expression and transport function.

Hayashi H, Inamura K, Aida K, Naoi S, Horikawa R, Nagasaka H, Takatani T, Fukushima T, Hattori A, Yabuki T, Horii I, Sugiyama Y. Hepatology. 2012;55(6):1889-900.
Pubmed DOI

4-Phenylbutyrate modulates ubiquitination of hepatocanalicular MRP2 and reduces serum total bilirubin concentration.

Hayashi H, Mizuno T, Horikawa R, Nagasaka H, Yabuki T, Takikawa H, Sugiyama Y. J Hepatol. 2012;56(5):1136-44.
Pubmed DOI

In vivo biliary clearance should be predicted by intrinsic biliary clearance in sandwich-cultured hepatocytes.

Nakakariya M, Ono M, Amano N, Moriwaki T, Maeda K, Sugiyama Y. Drug Metab Dispos. 2012;40(3):602-9.
Pubmed DOI

Regulation of tissue-specific expression of renal organic anion transporters by hepatocyte nuclear factor 1 α/β and DNA methylation.

Jin L, Kikuchi R, Saji T, Kusuhara H, Sugiyama Y. J Pharmacol Exp Ther. 2012;340(3):648-55.
Pubmed DOI

Competitive inhibition of the luminal efflux by multidrug and toxin extrusions, but not basolateral uptake by organic cation transporter 2, is the likely mechanism underlying the pharmacokinetic drug-drug interactions caused by cimetidine in the kidney.

Ito S, Kusuhara H, Yokochi M, Toyoshima J, Inoue K, Yuasa H, Sugiyama Y. J Pharmacol Exp Ther. 2012;340(2):393-403.
Pubmed DOI

Metabolism and pharmacokinetic studies of JPH203, an L-amino acid transporter 1 (LAT1) selective compound.

Wempe MF, Rice PJ, Lightner JW, Jutabha P, Hayashi M, Anzai N, Wakui S, Kusuhara H, Sugiyama Y, Endou H. Drug Metab Pharmacokinet. 2012;27(1):155-61.
Pubmed

Microdosing clinical study: pharmacokinetic, pharmacogenomic (SLCO2B1), and interaction (grapefruit juice) profiles of celiprolol following the oral microdose and therapeutic dose.

Ieiri I, Doi Y, Maeda K, Sasaki T, Kimura M, Hirota T, Chiyoda T, Miyagawa M, Irie S, Iwasaki K, Sugiyama Y. J Clin Pharmacol. 2012;52(7):1078-89.
Pubmed DOI