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Lysosomal P-gp-MDR1 Confers Drug Resistance of Brentuximab Vedotin and Its Cytotoxic Payload Monomethyl Auristatin E in Tumor Cells.

Liu-Kreyche P, Shen H, Marino AM, Iyer RA, Humphreys WG, Lai Y.

Front Pharmacol. 2019 Jul 17;10:749. doi: 10.3389/fphar.2019.00749. eCollection 2019.


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.

Clin Transl Sci. 2019 Jul;12(4):388-399. doi: 10.1111/cts.12625. Epub 2019 Apr 13.


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.

Clin Pharmacol Ther. 2019 Jul;106(1):228-237. doi: 10.1002/cpt.1373. Epub 2019 Mar 18.


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.

Drug Metab Dispos. 2019 Apr;47(4):350-357. doi: 10.1124/dmd.118.084988. Epub 2019 Jan 8.


Evidence for the Validity of Pyridoxic Acid (PDA) as a Plasma-Based Endogenous Probe for OAT1 and OAT3 Function in Healthy Subjects.

Shen H, Holenarsipur VK, Mariappan TT, Drexler DM, Cantone JL, Rajanna P, Singh Gautam S, Zhang Y, Gan J, Shipkova PA, Marathe P, Humphreys WG.

J Pharmacol Exp Ther. 2019 Jan;368(1):136-145. doi: 10.1124/jpet.118.252643. Epub 2018 Oct 25.


Comprehensive Evaluation of the Utility of 20 Endogenous Molecules as Biomarkers of OATP1B Inhibition Compared with Rosuvastatin and Coproporphyrin I.

Barnett S, Ogungbenro K, Ménochet K, Shen H, Humphreys WG, Galetin A.

J Pharmacol Exp Ther. 2019 Jan;368(1):125-135. doi: 10.1124/jpet.118.253062. Epub 2018 Oct 12.


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.

Drug Metab Dispos. 2018 Aug;46(8):1075-1082. doi: 10.1124/dmd.118.081125. Epub 2018 May 18.


Comparative untargeted proteomic analysis of ADME proteins and tumor antigens for tumor cell lines.

Gu X, Xiao Q, Ruan Q, Shu Y, Dongre A, Iyer R, Humphreys WG, Lai Y.

Acta Pharm Sin B. 2018 Mar;8(2):252-260. doi: 10.1016/j.apsb.2017.10.002. Epub 2017 Nov 4.


Abundance of Phase 1 and 2 Drug-Metabolizing Enzymes in Alcoholic and Hepatitis C Cirrhotic Livers: A Quantitative Targeted Proteomics Study.

Prasad B, Bhatt DK, Johnson K, Chapa R, Chu X, Salphati L, Xiao G, Lee C, Hop CECA, Mathias A, Lai Y, Liao M, Humphreys WG, Kumer SC, Unadkat JD.

Drug Metab Dispos. 2018 Jul;46(7):943-952. doi: 10.1124/dmd.118.080523. Epub 2018 Apr 25.


A Decade in the MIST: Learnings from Investigations of Drug Metabolites in Drug Development under the "Metabolites in Safety Testing" Regulatory Guidance.

Schadt S, Bister B, Chowdhury SK, Funk C, Hop CECA, Humphreys WG, Igarashi F, James AD, Kagan M, Khojasteh SC, Nedderman ANR, Prakash C, Runge F, Scheible H, Spracklin DK, Swart P, Tse S, Yuan J, Obach RS.

Drug Metab Dispos. 2018 Jun;46(6):865-878. doi: 10.1124/dmd.117.079848. Epub 2018 Feb 27. Review.


Physiologically-based pharmacokinetic modelling of a CYP2C19 substrate, BMS-823778, utilizing pharmacogenetic data.

Gong J, Iacono L, Iyer RA, Humphreys WG, Zheng M.

Br J Clin Pharmacol. 2018 Jun;84(6):1335-1345. doi: 10.1111/bcp.13565. Epub 2018 Apr 10.


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.

Clin Pharmacol Ther. 2018 Sep;104(3):564-574. doi: 10.1002/cpt.983. Epub 2018 Jan 17.


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.

Drug Metab Dispos. 2018 Feb;46(2):178-188. doi: 10.1124/dmd.117.077586. Epub 2017 Nov 21.


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.

Drug Metab Dispos. 2018 Feb;46(2):189-196. doi: 10.1124/dmd.117.077289. Epub 2017 Nov 14.


Clinical significance of CYP2C19 polymorphisms on the metabolism and pharmacokinetics of 11β-hydroxysteroid dehydrogenase type-1 inhibitor BMS-823778.

Cheng Y, Wang L, Iacono L, Zhang D, Chen W, Gong J, Humphreys WG, Gan J.

Br J Clin Pharmacol. 2018 Jan;84(1):130-141. doi: 10.1111/bcp.13421. Epub 2017 Oct 4.


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.

J Pharmacol Exp Ther. 2017 Sep;362(3):385-394. doi: 10.1124/jpet.117.242370. Epub 2017 Jun 23.


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.

Drug Metab Dispos. 2017 Aug;45(8):908-919. doi: 10.1124/dmd.117.075531. Epub 2017 Jun 2.


Tenofovir Disoproxil Fumarate Is Not an Inhibitor of Human Organic Cation Transporter 1.

Shen H, Li W, Humphreys WG, Lai Y.

J Pharmacol Exp Ther. 2017 Feb;360(2):341-342. doi: 10.1124/jpet.116.238337. No abstract available.


In Vitro Metabolite Formation in Human Hepatocytes and Cardiomyocytes and Metabolism and Tissue Distribution in Monkeys of the 2'-C-Methylguanosine Prodrug BMS-986094.

Li W, Trouba KJ, Ma L, Kwagh J, Storck C, Zhu Y, Flint O, Humphreys WG, Wang J, Liu A, Wang B, Graziano MJ, Davies MH, Sanderson TP.

Int J Toxicol. 2017 Jan 1:1091581816683642. doi: 10.1177/1091581816683642. [Epub ahead of print]


Drug-Protein Adducts: Chemistry, Mechanisms of Toxicity, and Methods of Characterization.

Gan J, Zhang H, Humphreys WG.

Chem Res Toxicol. 2016 Dec 19;29(12):2040-2057. Epub 2016 Dec 5. Review.


Tissue distribution and tumor uptake of folate receptor-targeted epothilone folate conjugate, BMS-753493, in CD2F1 mice after systemic administration.

Shen H, Wang L, Chen W, Menard K, Hong Y, Tian Y, Bonacorsi SJ, Humphreys WG, Lee FY, Gan J.

Acta Pharm Sin B. 2016 Sep;6(5):460-467. Epub 2016 Aug 11.


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.

J Pharmacol Exp Ther. 2016 Sep;358(3):397-404. doi: 10.1124/jpet.116.234914. Epub 2016 Jun 17.


Application of Static Models to Predict Midazolam Clinical Interactions in the Presence of Single or Multiple Hepatitis C Virus Drugs.

Cheng Y, Ma L, Chang SY, Humphreys WG, Li W.

Drug Metab Dispos. 2016 Aug;44(8):1372-80. doi: 10.1124/dmd.116.070409. Epub 2016 May 25.


Toxicology Strategies for Drug Discovery - Present and Future: Introduction.

Humphreys WG, Will Y, Guengerich FP.

Chem Res Toxicol. 2016 Apr 18;29(4):437. doi: 10.1021/acs.chemrestox.6b00049. No abstract available.


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.

Biopharm Drug Dispos. 2016 Jul;37(5):276-86. doi: 10.1002/bdd.2011.


Biotransformation of Daclatasvir In Vitro and in Nonclinical Species: Formation of the Main Metabolite by Pyrrolidine δ-Oxidation and Rearrangement.

Li W, Zhao W, Liu X, Huang X, Lopez OD, Leet JE, Fancher RM, Nguyen V, Goodrich J, Easter J, Hong Y, Caceres-Cortes J, Chang SY, Ma L, Belema M, Hamann LG, Gao M, Zhu M, Shu YZ, Humphreys WG, Johnson BM.

Drug Metab Dispos. 2016 Jun;44(6):809-20. doi: 10.1124/dmd.115.068866. Epub 2016 Mar 30.


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.

Mol Pharm. 2016 Apr 4;13(4):1206-16. doi: 10.1021/acs.molpharmaceut.5b00659. Epub 2016 Mar 8.


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.

J Pharmacol Exp Ther. 2016 May;357(2):382-93. doi: 10.1124/jpet.116.232066. Epub 2016 Feb 23.


Label-Free Bottom-Up Proteomic Workflow for Simultaneously Assessing the Target Specificity of Covalent Drug Candidates and Their Off-Target Reactivity to Selected Proteins.

Yang Y, Shu YZ, Humphreys WG.

Chem Res Toxicol. 2016 Jan 19;29(1):109-16. doi: 10.1021/acs.chemrestox.5b00460. Epub 2015 Dec 29.


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.

Drug Metab Dispos. 2015 Nov;43(11):1788-94. doi: 10.1124/dmd.115.065946. Epub 2015 Sep 4.


Correction to "Synthesis of Biologically Active Piperidine Metabolites of Clopidogrel: Determination of Structure and Analyte Development".

Shaw SA, Balasubramanian B, Bonacorsi S, Caceres Cortes J, Cao K, Chen BC, Dai J, Decicco C, Goswami A, Guo Z, Hanson R, Humphreys WG, Lam PY, Li W, Mathur A, Maxwell BD, Michaudel Q, Peng L, Pudzianowski A, Qiu F, Su S, Sun D, Tymiak AA, Vokits BP, Wang B, Wexler R, Wu DR, Zhang Y, Zhao R, Baran PS.

J Org Chem. 2015 Sep 18;80(18):9370. doi: 10.1021/acs.joc.5b02011. Epub 2015 Sep 2. No abstract available.


Integration of Physiologically-Based Pharmacokinetic Modeling into Early Clinical Development: An Investigation of the Pharmacokinetic Nonlinearity.

Zhou L, Gan J, Yoshitsugu H, Gu X, Lutz JD, Masson E, Humphreys WG.

CPT Pharmacometrics Syst Pharmacol. 2015 May;4(5):286-94. doi: 10.1002/psp4.35. Epub 2015 Apr 29.


Characterization of ADME properties of [(14)C]asunaprevir (BMS-650032) in humans.

Gong J, Eley T, He B, Arora V, Philip T, Jiang H, Easter J, Humphreys WG, Iyer RA, Li W.

Xenobiotica. 2016;46(1):52-64. doi: 10.3109/00498254.2015.1048487. Epub 2015 Jul 7.


Synthesis of Biologically Active Piperidine Metabolites of Clopidogrel: Determination of Structure and Analyte Development.

Shaw SA, Balasubramanian B, Bonacorsi S, Cortes JC, Cao K, Chen BC, Dai J, Decicco C, Goswami A, Guo Z, Hanson R, Humphreys WG, Lam PY, Li W, Mathur A, Maxwell BD, Michaudel Q, Peng L, Pudzianowski A, Qiu F, Su S, Sun D, Tymiak AA, Vokits BP, Wang B, Wexler R, Wu DR, Zhang Y, Zhao R, Baran PS.

J Org Chem. 2015 Jul 17;80(14):7019-32. doi: 10.1021/acs.joc.5b00632. Epub 2015 Jul 7. Erratum in: J Org Chem. 2015 Sep 18;80(18):9370.


Contribution of metabolites to P450 inhibition-based drug-drug interactions: scholarship from the drug metabolism leadership group of the innovation and quality consortium metabolite group.

Yu H, Balani SK, Chen W, Cui D, He L, Humphreys WG, Mao J, Lai WG, Lee AJ, Lim HK, MacLauchlin C, Prakash C, Surapaneni S, Tse S, Upthagrove A, Walsky RL, Wen B, Zeng Z.

Drug Metab Dispos. 2015 Apr;43(4):620-30. doi: 10.1124/dmd.114.059345. Epub 2015 Feb 5.


Identification of human liver microsomal proteins adducted by a reactive metabolite using shotgun proteomics.

Yang Y, Xiao Q, Humphreys WG, Dongre A, Shu YZ.

Chem Res Toxicol. 2014 Sep 15;27(9):1537-46. doi: 10.1021/tx500181p. Epub 2014 Aug 19.


Quantitative analysis of polyethylene glycol (PEG) and PEGylated proteins in animal tissues by LC-MS/MS coupled with in-source CID.

Gong J, Gu X, Achanzar WE, Chadwick KD, Gan J, Brock BJ, Kishnani NS, Humphreys WG, Iyer RA.

Anal Chem. 2014 Aug 5;86(15):7642-9. doi: 10.1021/ac501507g. Epub 2014 Jul 8.


Investigating the enteroenteric recirculation of apixaban, a factor Xa inhibitor: administration of activated charcoal to bile duct-cannulated rats and dogs receiving an intravenous dose and use of drug transporter knockout rats.

Zhang D, Frost CE, He K, Rodrigues AD, Wang X, Wang L, Goosen TC, Humphreys WG.

Drug Metab Dispos. 2013 Apr;41(4):906-15. doi: 10.1124/dmd.112.050575. Epub 2013 Feb 5.


Characterization of efflux transporters involved in distribution and disposition of apixaban.

Zhang D, He K, Herbst JJ, Kolb J, Shou W, Wang L, Balimane PV, Han YH, Gan J, Frost CE, Humphreys WG.

Drug Metab Dispos. 2013 Apr;41(4):827-35. doi: 10.1124/dmd.112.050260. Epub 2013 Feb 4.


The influence of kidney function on dapagliflozin exposure, metabolism and pharmacodynamics in healthy subjects and in patients with type 2 diabetes mellitus.

Kasichayanula S, Liu X, Pe Benito M, Yao M, Pfister M, LaCreta FP, Humphreys WG, Boulton DW.

Br J Clin Pharmacol. 2013 Sep;76(3):432-44. doi: 10.1111/bcp.12056.


Bioactivation of 2-(alkylthio)-1,3,4-thiadiazoles and 2-(alkylthio)-1,3-benzothiazoles.

Yang Y, Qiu F, Josephs JL, Humphreys WG, Shu YZ.

Chem Res Toxicol. 2012 Dec 17;25(12):2770-9. doi: 10.1021/tx3003998. Epub 2012 Nov 30.


Metabolic chiral inversion of brivanib and its relevance to safety and pharmacology.

Gong J, Gan J, Masson E, Syed S, Xia YQ, Williams D, Pursley J, Jemal M, Humphreys WG, Iyer RA.

Drug Metab Dispos. 2012 Dec;40(12):2374-80. doi: 10.1124/dmd.112.047340. Epub 2012 Sep 14.


Overcoming bioanalytical challenges in an Onglyza(®) intravenous [(14)C]microdose absolute bioavailability study with accelerator MS.

Xu XS, Dueker SR, Christopher LJ, Lohstroh PN, Keung CF, Cao KK, Bonacorsi SJ, Cojocaru L, Shen JX, Humphreys WG, Stouffer B, Arnold ME.

Bioanalysis. 2012 Aug;4(15):1855-70. doi: 10.4155/bio.12.171.


A semi-automated method for the integrated evaluation of half-life and metabolic soft spots of discovery compounds.

Grubb MF, Humphreys WG, Josephs JL.

Bioanalysis. 2012 Jul;4(14):1747-61. doi: 10.4155/BIO.12.134.


Characterization of the in vitro and in vivo metabolism and disposition and cytochrome P450 inhibition/induction profile of saxagliptin in human.

Su H, Boulton DW, Barros A Jr, Wang L, Cao K, Bonacorsi SJ Jr, Iyer RA, Humphreys WG, Christopher LJ.

Drug Metab Dispos. 2012 Jul;40(7):1345-56. doi: 10.1124/dmd.112.045450. Epub 2012 Apr 10.


Integrated quantitative and qualitative workflow for in vivo bioanalytical support in drug discovery using hybrid Q-TOF-MS.

Ranasinghe A, Ramanathan R, Jemal M, D'Arienzo CJ, Humphreys WG, Olah TV.

Bioanalysis. 2012 Mar;4(5):511-28. doi: 10.4155/bio.12.13.


Liquid chromatography and tandem mass spectrometry method for the quantitative determination of saxagliptin and its major pharmacologically active 5-monohydroxy metabolite in human plasma: method validation and overcoming specific and non-specific binding at low concentrations.

Xu XS, Demers R, Gu H, Christopher LJ, Su H, Cojocaru L, Boulton DW, Kirby M, Stouffer B, Humphreys WG, Arnold ME.

J Chromatogr B Analyt Technol Biomed Life Sci. 2012 Mar 15;889-890:77-86. doi: 10.1016/j.jchromb.2012.01.033. Epub 2012 Feb 6.


Cytochrome P450 11A1 bioactivation of a kinase inhibitor in rats: use of radioprofiling, modulation of metabolism, and adrenocortical cell lines to evaluate adrenal toxicity.

Zhang D, Flint O, Wang L, Gupta A, Westhouse RA, Zhao W, Raghavan N, Caceres-Cortes J, Marathe P, Shen G, Zhang Y, Allentoff A, Josephs J, Gan J, Borzilleri R, Humphreys WG.

Chem Res Toxicol. 2012 Mar 19;25(3):556-71. doi: 10.1021/tx200524d. Epub 2012 Mar 2.


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