Yurong LAI (Gilead)
Pharmacol Ther. 2022 Oct;238:108271. The next frontier in ADME science: Predicting transporter-based drug disposition, tissue concentrations and drug-drug interactions in humans. Storelli F, Yin M, Kumar AR, Ladumor MK, Evers R, Chothe PP, Enogieru OJ, Liang X, Lai Y, Unadkat JD. PubMed
Acta Pharm Sin B. 2022;12:2751-2777. Recent advances in the translation of drug metabolism and pharmacokinetics science for drug discovery and development. Lai Y, Chu X, Di L, Gao W, Guo Y, Liu X, Lu C, Mao J, Shen H, Tang H, Xia CQ, Zhang L, Ding X. PubMed
Clin Pharmacol Ther. 2022;112:573-592. Clinical Relevance of Hepatic and Renal P-gp/BCRP Inhibition of Drugs: An International Transporter Consortium Perspective. Taskar KS, Yang X, Neuhoff S, Patel M, Yoshida K, Paine MF, Brouwer KLR, Chu X, Sugiyama Y, Cook J, Polli JW, Hanna I, Lai Y, Zamek-Gliszczynski M; ITC. PubMed
Clin Pharmacol Ther. 2022;112:527-539. Transporters and Toxicity: Insights From the International Transporter Consortium Workshop 4. Hafey MJ, Aleksunes LM, Bridges CC, Brouwer KR, Chien HC, Leslie EM, Hu S, Li Y, Shen J, Sparreboom A, Sprowl J, Tweedie D, Lai Y. PubMed
Clin Transl Sci. 2022;15:1519-1531. Physiologically-based pharmacokinetic model-based translation of OATP1B-mediated drug-drug interactions from coproporphyrin I to probe drugs. Mochizuki T, Aoki Y, Yoshikado T, Yoshida K, Lai Y, Hirabayashi H, Yamaura Y, Rockich K, Taskar K, Takashima T, Chu X, Zamek-Gliszczynski MJ, Mao J, Maeda K, Furihata K, Sugiyama Y, Kusuhara H. PubMed
Clin Pharmacol Ther. 2022;111:1315-1323.Effect of Cyclosporin A and impact of dose staggering on OATP1B1/1B3 endogenous substrates and drug probes for assessing clinical drug interactions. Mochizuki T, Zamek-Gliszczynski MJ, Yoshida K, Mao J, Taskar K, Hirabayashi H, Chu X, Lai Y, Takashima T, Rockich K, Yamaura Y, Fujiwara K, Mizuno T, Maeda K, Furihata K, Sugiyama Y, Kusuhara H. PubMed
Drug Metab Dispos. 2021;49:1063-1069. Endogenous plasma Kynurenic acid in human: A newly discovered biomarker for Drug-Drug Interactions involving Organic Anion Transporter 1 and 3 inhibition. Tang J, Shen H, Zhao X, Holenarsipur VK, Mariappan TT, Zhang Y, Panfen E, Zheng J, Humphreys WG, Lai Y. PubMed
Expert Opin Drug Metab Toxicol. 2021;17:869-8861. Overcoming the shortcomings of the extended-clearance concept: a framework for developing a physiologically-based pharmacokinetic (PBPK) model to select drug candidates involving transporter-mediated clearance. Liang X, Lai Y. PubMed
Drug Metab Dispos. 2021;49:159-168. Prediction of transporter-mediated Rosuvastatin hepatic uptake clearance and drug interaction in humans using proteomics-informed REF approach. Kumar V, Yin M, Ishida K, Salphati L, Hop CECA, Rowbottom C, Xiao G, Lai Y, Mathias A, Chu X, Humphreys WG, Liao M, Nerada Z, Szilvásy N, Heyward S, Unadkat JD. PubMed
Drug Metab Dispos. 2020;48:1283-1292. In vitro hepatic uptake in human and monkey hepatocytes in the presence and absence of serum protein and its in vitro to in vivo extrapolation. Liang X, Park Y, DeForest N, Hao J, Zhao X, Niu C, Wang K, Smith BJ, Lai Y. PubMed
Drug Metab Dispos. 2020;48:724-734. Absorption and disposition of Coproporphyrin I (CPI) in Cynomolgus monkeys and mice: Pharmacokinetic evidence to support the use of CPI to inform the potential for Organic Anion-Transporting Polypeptide inhibition. Gu X, Wang L, Gan J, Fancher RM, Tian Y, Hong Y, Lai Y, Sinz M, Shen H. PubMed
Clin Pharmacol Ther. 2020; In press. Intestinal P-gp and putative hepatic OATP1B induction: International Transporter Consortium perspective on drug development implications. 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
Drug Metab Dispos. 2020;48:205-216. Induction of human intestinal and hepatic Organic Anion Transporting Polypeptides: Where is the evidence for its relevance in Drug-Drug Interactions? Rodrigues AD, Lai Y, Shen H, Varma MVS, Rowland A, Oswald S. PubMed
Drug Metab Dispos. 2019;47:1433-1442. Organic Anion-Transporting Polypeptide genes are not induced by the Pregnane X Receptor Activator Rifampin: Studies in hepatocytes in vitro and in monkeys in vivo. Niu C, Wang Y, Zhao X, Tep S, Murakami E, Subramanian R, Smith B, Lai Y. PubMed
Drug Metab Dispos. 2019;47:1122-1135. Drug concentration asymmetry in tissues and plasma for small molecule-related therapeutic modalities. Zhang D, Hop CECA, Patilea-Vrana G, Gampa G, Seneviratne HK, Unadkat JD, Kenny JR, Nagapudi K, Di L, Zhou L, Zak M, Wright MR, Bumpus NN, Zang R, Liu X, Lai Y, Khojasteh SC. PubMed
Clin Pharmacol Ther. 2019;106:1056-1066. Positron Emission Tomography imaging of [11C]Rosuvastatin hepatic concentrations and hepatobiliary transport in humans in the absence and presence of Cyclosporin A. Billington S, Shoner S, Lee S, Clark-Snustad K, Pennington M, Lewis D, Muzi M, Rene S, Lee J, Nguyen TB, Kumar V, Ishida K, Chen L, Chu X, Lai Y, Salphati L, Hop CECA, Xiao G, Liao M, Unadkat JD. PubMed
Clin Transl Sci. 2019;12:388-399. Organic Anion Transporter Polypeptide 1B1 polymorphism modulates the extent of Drug-Drug Interaction and associated biomarker levels in healthy volunteers. Yee SW, Giacomini MM, Shen H, Humphreys WG, Horng H, Brian W, Lai Y, Kroetz DL, Giacomini KM. PubMed
Clin Pharmacol Ther. 2019;106:228-237. Interindividual and regional variability in drug transporter abundance at the human Blood-Brain Barrier measured by quantitative targeted proteomics. Billington S, Salphati L, Hop CECA, Chu X, Evers R, Burdette D, Rowbottom C, Lai Y, Xiao G, Humphreys WG, Nguyen TB, Prasad B, Unadkat JD. PubMed
Drug Metab Dispos. 2019;47:350-357. A comparison of total and plasma membrane abundance of transporters in suspended, plated, Sandwich-Cultured Human Hepatocytes versus human liver tissue using quantitative targeted proteomics and cell surface biotinylation. Kumar V, Salphati L, Hop CECA, Xiao G, Lai Y, Mathias A, Chu X, Humphreys WG, Liao M, Heyward S, Unadkat JD. 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
Clin Pharmacol Ther. 2018;104:916-932. Can Bile Salt Export Pump inhibition testing in drug discovery and development reduce liver injury risk? An International Transporter Consortium perspective. Kenna JG, Taskar KS, Battista C, Bourdet DL, Brouwer KLR, Brouwer KR, Dai D, Funk C, Hafey MJ, Lai Y, Maher J, Pak YA, Pedersen JM, Polli JW, Rodrigues AD, Watkins PB, Yang K, Yucha RW; International Transporter Consortium. PubMed
Pharmaceutics. 2018;10:125. In vitro stimulation of Multidrug Resistance-Associated Protein 2 function is not reproduced in vivo in rats. Gilibili RR, Kurawattimath V, Murali BV, Lai Y, Mariappan TT, Shen H, Chatterjee S. PubMed
Drug Metab Dispos. 2018;46:1075-1082. Further studies to support the use of Coproporphyrin I and III as novel clinical biomarkers for evaluating the potential for Organic Anion Transporting Polypeptide 1B1 and OATP1B3 inhibition. Shen H, Christopher L, Lai Y, Gong J, Kandoussi H, Garonzik S, Perera V, Garimella T, Humphreys WG. PubMed
Bioanalysis. 2018;10:633-644. UHPLC-MS/MS bioanalysis of human plasma coproporphyrins as potential biomarkers for organic anion-transporting polypeptide-mediated drug interactions. Kandoussi H, Zeng J, Shah K, Paterson P, Santockyte R, Kadiyala P, Shen H, Shipkova P, Langish R, Burrrell R, Easter J, Mariannino T, Marathe P, Lai Y, Zhang Y, Pillutla R. PubMed
Drug Metab Dispos. 2018;46:561-566. Drug transporters in xenobiotic Ddsposition and pharmacokinetic prediction. Mao Q, Lai Y, Wang J. PubMed
Clin Pharmacol Ther. 2018;104:564-574. Gaining mechanistic insight into Coproporphyrin I as endogenous biomarker for OATP1B-mediated Drug-Drug Interactions using population pharmacokinetic modeling and simulation. Barnett S, Ogungbenro K, Ménochet K, Shen H, Lai Y, Humphreys WG, Galetin A. PubMed
Drug Metab Dispos. 2018;46:178-188. Discovery and validation of Pyridoxic acid and Homovanillic acid as novel endogenous plasma biomarkers of Organic Anion Transporter (OAT) 1 and OAT3 in Cynomolgus monkeys. Shen H, Nelson DM, Oliveira RV, Zhang Y, Mcnaney CA, Gu X, Chen W, Su C, Reily MD, Shipkova PA, Gan J, Lai Y, Marathe P, Humphreys WG. PubMed
Drug Metab Dispos. 2018;46:189-196. Transporter expression in noncancerous and cancerous liver tissue from donors with hepatocellular carcinoma and chronic hepatitis C infection quantified by LC-MS/MS proteomics. Billington S, Ray AS, Salphati L, Xiao G, Chu X, Humphreys WG, Liao M, Lee CA, Mathias A, Hop CECA, Rowbottom C, Evers R, Lai Y, Kelly EJ, Prasad B, Unadkat JD. PubMed
AAPS J. 2017;19:1878-1889. Physiologically based pharmacokinetic modeling of transporter-mediated hepatic clearance and liver partitioning of OATP and OCT substrates in Cynomolgus monkeys. Morse BL, MacGuire JG, Marino AM, Zhao Y, Fox M, Zhang Y, Shen H, Griffith Humphreys W, Marathe P, Lai Y. PubMed
J Pharmacol Exp Ther. 2017;362:385-394. Bile salt homeostasis in normal and Bsep gene knockout rats with single and repeated doses of Troglitazone. Cheng Y, Chen S, Freeden C, Chen W, Zhang Y, Abraham P, Nelson DM, Humphreys WG, Gan J, Lai Y. PubMed
Drug Metab Dispos. 2017;45:908-919. Comparative evaluation of plasma bile acids, Dehydroepiandrosterone Sulfate, Hexadecanedioate, and Tetradecanedioate with Coproporphyrins I and III as markers of OATP inhibition in healthy subjects. Shen H, Chen W, Drexler DM, Mandlekar S, Holenarsipur VK, Shields EE, Langish R, Sidik K, Gan J, Humphreys WG, Marathe P, Lai Y. PubMed
Adv Drug Deliv Rev. 2017;116:92-99. Molecular properties associated with transporter-mediated drug disposition. Varma MV, Lai Y, El-Kattan AF. PubMed
Drug Metab Dispos. 2017;45:604-611. Coproporphyrin-I: A fluorescent, Endogenous optimal probe substrate for ABCC2 (MRP2) suitable for vesicle-based MRP2 inhibition assay. Gilibili RR, Chatterjee S, Bagul P, Mosure KW, Murali BV, Mariappan TT, Mandlekar S, Lai Y. PubMed
J Pharmacol Exp Ther. 2017;360:341-342. Tenofovir Disoproxil Fumarate is not an inhibitor of human Organic Cation Transporter 1. Shen H, Li W, Humphreys WG, Lai Y. PubMed
Drug Metab Dispos. 2017;45:228-236. Organic Anion Transporter 2: An enigmatic human Solute Carrier. Shen H, Lai Y, Rodrigues AD. PubMed
Drug Metab Dispos. 2016;44:1752-1758. Transporter expression in liver tissue from subjects with alcoholic or hepatitis C cirrhosis quantified by targeted quantitative proteomics. Wang L, Collins C, Kelly EJ, Chu X, Ray AS, Salphati L, Xiao G, Lee C, Lai Y, Liao M, Mathias A, Evers R, Humphreys W, Hop CE, Kumer SC, Unadkat JD. PubMed
J Pharmacol Exp Ther. 2016;358:397-404. Coproporphyrins in plasma and urine can be appropriate clinical biomarkers to recapitulate Drug-Drug Interactions mediated by Organic Anion Transporting Polypeptide inhibition. Lai Y, Mandlekar S, Shen H, Holenarsipur VK, Langish R, Rajanna P, Murugesan S, Gaud N, Selvam S, Date O, Cheng Y, Shipkova P, Dai J, Humphreys WG, Marathe P. PubMed
Biopharm Drug Dispos. 2016;37:276-86. Biliary excretion of pravastatin and taurocholate in rats with bile salt export pump (Bsep) impairment. Cheng Y, Freeden C, Zhang Y, Abraham P, Shen H, Wescott D, Humphreys WG, Gan J, Lai Y. PubMed
Mol Pharm. 2016;13:1206-16. Disruption of BSEP function in HepaRG Cells alters bile acid disposition and is a susceptive factor to Drug-induced cholestatic injury. Qiu X, Zhang Y, Liu T, Shen H, Xiao Y, Bourner MJ, Pratt JR, Thompson DC, Marathe P, Humphreys WG, Lai Y. PubMed
J Pharmacol Exp Ther. 2016;357:382-93. Coproporphyrins I and III as functional markers of OATP1B activity: In vitro and in vivo evaluation in preclinical species. Shen H, Dai J, Liu T, Cheng Y, Chen W, Freeden C, Zhang Y, Humphreys WG, Marathe P, Lai Y. PubMed
Chem Res Toxicol. 2016;29:545-63. Involvement of drug transporters in organ toxicity: The fundamental basis of drug discovery and development. Cheng Y, El-Kattan A, Zhang Y, Ray AS, Lai Y. PubMed
Drug Metab Dispos. 2016;44:505-16. Mechanistic modeling of Pitavastatin disposition in Sandwich-Cultured Human Hepatocytes: A proteomics-informed bottom-up approach. Vildhede A, Mateus A, Khan EK, Lai Y, Karlgren M, Artursson P, Kjellsson MC. PubMed
Drug Metab Dispos. 2016;44:320-8. Diclofenac and its Acyl Glucuronide: Determination of in vivo exposure in human subjects and characterization as human drug transporter substrates in vitro. Zhang Y, Han YH, Putluru SP, Matta MK, Kole P, Mandlekar S, Furlong MT, Liu T, Iyer RA, Marathe P, Yang Z, Lai Y, Rodrigues AD. PubMed
Drug Metab Dispos. 2016;44:238-49. Cynomolgus monkey as a clinically relevant model to study transport involving renal Organic Cation Transporters: In vitro and in vivo evaluation. Shen H, Liu T, Jiang H, Titsch C, Taylor K, Kandoussi H, Qiu X, Chen C, Sukrutharaj S, Kuit K, Mintier G, Krishnamurthy P, Fancher RM, Zeng J, Rodrigues AD, Marathe P, Lai Y. PubMed
Mol Pharm. 2015;12:3943-52. Hepatic disposition of Gemfibrozil and its major metabolite Gemfibrozil 1-O-β-Glucuronide. Kimoto E, Li R, Scialis RJ, Lai Y, Varma MV. PubMed
Drug Metab Dispos. 2015;43:1788-94. Rosuvastatin liver partitioning in Cynomolgus monkeys: Measurement in vivo and prediction using in vitro Monkey hepatocyte uptake. Morse BL, Cai H, MacGuire JG, Fox M, Zhang L, Zhang Y, Gu X, Shen H, Dierks EA, Su H, Luk CE, Marathe P, Shu YZ, Humphreys WG, Lai Y. PubMed
Drug Metab Dispos. 2015;43:984-93. Characterization of Organic Anion Transporter 2 (SLC22A7): A highly efficient transporter for Creatinine and species-dependent renal tubular expression. Shen H, Liu T, Morse BL, Zhao Y, Zhang Y, Qiu X, Chen C, Lewin AC, Wang XT, Liu G, Christopher LJ, Marathe P, Lai Y. PubMed
Mol Pharm. 2014;11:3547-55. Protein abundance of clinically relevant multidrug transporters along the entire length of the human intestine. Drozdzik M, Gröer C, Penski J, Lapczuk J, Ostrowski M, Lai Y, Prasad B, Unadkat JD, Siegmund W, Oswald S. PubMed
AAPS J. 2014;16:802-9. Permeability comparison between hepatocyte and low efflux MDCKII cell monolayer. Li R, Bi YA, Lai Y, Sugano K, Steyn SJ, Trapa PE, Di L. PubMed
AAPS J. 2014;16:714-26. Quantitative targeted proteomics for membrane transporter proteins: method and application. Qiu X, Zhang H, Lai Y. PubMed
Drug Metab Dispos. 2014;42:1210-8. Hepatic uptake of atorvastatin: influence of variability in transporter expression on uptake clearance and drug-drug interactions. Vildhede A, Karlgren M, Svedberg EK, Wisniewski JR, Lai Y, Norén A, Artursson P. PubMed
Drug Metab Lett. 2013;7:15-22. Inhibition of hepatobiliary transporters by a novel kinase inhibitor contributes to hepatotoxicity in beagle dogs. Daniels JS, Lai Y, South S, Chiang PC, Walker D, Feng B, Mireles R, Whiteley LO, McKenzie JW, Stevens J, Mourey R, Anderson D, Davis Ii JW. PubMed
Drug Metab Dispos. 2014;42:566-74. Drug-induced perturbations of the bile acid pool, cholestasis, and hepatotoxicity: mechanistic considerations beyond the direct inhibition of the bile salt export pump. Rodrigues AD, Lai Y, Cvijic ME, Elkin LL, Zvyaga T, Soars MG. PubMed
Biopharm Drug Dispos. 2013;34:452-61. Quantitative assessment of the contribution of sodium-dependent taurocholate co-transporting polypeptide (NTCP) to the hepatic uptake of rosuvastatin, pitavastatin and fluvastatin. Bi YA, Qiu X, Rotter CJ, Kimoto E, Piotrowski M, Varma MV, Ei-Kattan AF, Lai Y. PubMed
Curr Pharm Des. 2014;20:1577-94. Beyond the ITC White Paper: emerging sciences in drug transporters and opportunities for drug development. Lai Y, Hsiao P. PubMed
J Pharm Sci. 2013;102:3252-63. Absolute measurement of species differences in sodium taurocholate cotransporting polypeptide (NTCP/Ntcp) and its modulation in cultured hepatocytes. Qiu X, Bi YA, Balogh LM, Lai Y. PubMed
Drug Metab Dispos. 2013;41:966-74. Quantitative prediction of repaglinide-rifampicin complex drug interactions using dynamic and static mechanistic models: delineating differential CYP3A4 induction and OATP1B1 inhibition potential of rifampicin. Varma MV, Lin J, Bi YA, Rotter CJ, Fahmi OA, Lam JL, El-Kattan AF, Goosen TC, Lai Y. PubMed
Expert Opin Drug Metab Toxicol. 2013;9:459-72. Model-based approaches to predict drug-drug interactions associated with hepatic uptake transporters: preclinical, clinical and beyond. Barton HA, Lai Y, Goosen TC, Jones HM, El-Kattan AF, Gosset JR, Lin J, Varma MV. PubMed
Pharm Res. 2013;30:1188-99. Mechanistic modeling to predict the transporter- and enzyme-mediated drug-drug interactions of repaglinide. Varma MV, Lai Y, Kimoto E, Goosen TC, El-Kattan AF, Kumar V. PubMed
J Pharm Sci. 2013;102:787-93. Interindividual variability in the hepatic expression of the human breast cancer resistance protein (BCRP/ABCG2): effect of age, sex, and genotype. Prasad B, Lai Y, Lin Y, Unadkat JD. PubMed
Hepatology. 2013;57:1530-41. Bile salt export pump is dysregulated with altered farnesoid X receptor isoform expression in patients with hepatocellular carcinoma. Chen Y, Song X, Valanejad L, Vasilenko A, More V, Qiu X, Chen W, Lai Y, Slitt A, Stoner M, Yan B, Deng R. PubMed
Mol Pharm. 2012;9:3535-42. Characterization of organic anion transporting polypeptide (OATP) expression and its functional contribution to the uptake of substrates in human hepatocytes. Kimoto E, Yoshida K, Balogh LM, Bi YA, Maeda K, El-Kattan A, Sugiyama Y, Lai Y. PubMed
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