Publications after 2012

2015

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

The synthesis of [(18)F]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 and 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 and Sugiyama Y. Drug Metab Dispos. 2015;43(2):235-47.
Pubmed DOI

Review
Organic Anion Transporting Polypeptide (OATP)1B1 and OATP1B3 as Important Regulators of the Pharmacokinetics of Substrate Drugs.

Maeda K. Biol Pharm Bull. 2015;38(2):155-168.
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 Jan 30. doi: 10.1002/jps.24366.
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 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

2013

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 ¹⁴C-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