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A Comparison of Total and Plasma Membrane Abundance of Transporters in Suspended, Plated, Sandwich-Cultured Human Hepatocytes vs. 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 Jan 8. pii: dmd.118.084988. doi: 10.1124/dmd.118.084988. [Epub ahead of print]


Improving Confidence in the Determination of Free Fraction for Highly Bound Drugs Using Bidirectional Equilibrium Dialysis.

Chen YC, Kenny JR, Wright M, Hop CECA, Yan Z.

J Pharm Sci. 2018 Oct 14. pii: S0022-3549(18)30610-5. doi: 10.1016/j.xphs.2018.10.011. [Epub ahead of print]


Correction to: Strategies of Drug Transporter Quantitation by LC-MS: Importance of Peptide Selection and Digestion Efficiency.

Chen B, Liu L, Ho H, Chen Y, Yang Z, Liang X, Payandeh J, Dean B, Hop CECA, Deng Y.

AAPS J. 2018 Jun 6;20(4):75. doi: 10.1208/s12248-018-0236-3.


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.


Prediction of the Pharmacokinetics of Pravastatin as an OATP Substrate Using Plateable Human Hepatocytes With Human Plasma Data and PBPK Modeling.

Mao J, Doshi U, Wright M, Hop CECA, Li AP, Chen Y.

CPT Pharmacometrics Syst Pharmacol. 2018 Apr;7(4):251-258. doi: 10.1002/psp4.12283. Epub 2018 Feb 13.


Immolation of p-Aminobenzyl Ether Linker and Payload Potency and Stability Determine the Cell-Killing Activity of Antibody-Drug Conjugates with Phenol-Containing Payloads.

Zhang D, Le H, Cruz-Chuh JD, Bobba S, Guo J, Staben L, Zhang C, Ma Y, Kozak KR, Lewis Phillips GD, Vollmar BS, Sadowsky JD, Vandlen R, Wei B, Su D, Fan P, Dragovich PS, Khojasteh SC, Hop CECA, Pillow TH.

Bioconjug Chem. 2018 Feb 21;29(2):267-274. doi: 10.1021/acs.bioconjchem.7b00576. Epub 2018 Feb 7.


Intratumoral Payload Concentration Correlates with the Activity of Antibody-Drug Conjugates.

Zhang D, Yu SF, Khojasteh SC, Ma Y, Pillow TH, Sadowsky JD, Su D, Kozak KR, Xu K, Polson AG, Dragovich PS, Hop CECA.

Mol Cancer Ther. 2018 Mar;17(3):677-685. doi: 10.1158/1535-7163.MCT-17-0697. Epub 2018 Jan 18.


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.


Strategy for CYP3A Induction Risk Assessment from Preclinical Signal to Human: a Case Example of a Late-Stage Discovery Compound.

Mao J, Fan P, Wong S, Wang J, Ismaili MHA, Dean B, Hop CECA, Wright M, Chen Y.

Pharm Res. 2017 Nov;34(11):2403-2414. doi: 10.1007/s11095-017-2246-8. Epub 2017 Aug 16.


Mixed Matrix Method Provides A Reliable Metabolite Exposure Comparison for Assessment of Metabolites in Safety Testing (MIST).

Takahashi RH, Khojasteh C, Wright M, Hop CECA, Ma S.

Drug Metab Lett. 2017 Nov 17;11(1):21-28. doi: 10.2174/1872312811666170710193229.


Strategies of Drug Transporter Quantitation by LC-MS: Importance of Peptide Selection and Digestion Efficiency.

Chen B, Liu L, Ho H, Chen Y, Yang Z, Liang X, Payandeh J, Dean B, Hop CECA, Deng Y.

AAPS J. 2017 Sep;19(5):1469-1478. doi: 10.1208/s12248-017-0106-4. Epub 2017 Jun 6. Erratum in: AAPS J. 2018 Jun 6;20(4):75.


Novel Mechanism of Decyanation of GDC-0425 by Cytochrome P450.

Takahashi RH, Halladay JS, Siu M, Chen Y, Hop CE, Khojasteh SC, Ma S.

Drug Metab Dispos. 2017 May;45(5):430-440. doi: 10.1124/dmd.116.074336. Epub 2017 Feb 10.


Linker Immolation Determines Cell Killing Activity of Disulfide-Linked Pyrrolobenzodiazepine Antibody-Drug Conjugates.

Zhang D, Pillow TH, Ma Y, Cruz-Chuh JD, Kozak KR, Sadowsky JD, Lewis Phillips GD, Guo J, Darwish M, Fan P, Chen J, He C, Wang T, Yao H, Xu Z, Chen J, Wai J, Pei Z, Hop CE, Khojasteh SC, Dragovich PS.

ACS Med Chem Lett. 2016 Aug 26;7(11):988-993. eCollection 2016 Nov 10.


Antibody Drug Conjugates Differentiate Uptake and DNA Alkylation of Pyrrolobenzodiazepines in Tumors from Organs of Xenograft Mice.

Ma Y, Khojasteh SC, Hop CE, Erickson HK, Polson A, Pillow TH, Yu SF, Wang H, Dragovich PS, Zhang D.

Drug Metab Dispos. 2016 Dec;44(12):1958-1962. Epub 2016 Sep 28.


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.

Drug Metab Dispos. 2016 Nov;44(11):1752-1758. Epub 2016 Aug 19.


Corrigendum to "Simultaneous determination of itraconazole, hydroxy itraconazole, keto itraconazole and N-desalkyl itraconazole concentration in human plasma using liquid chromatography with tandem mass spectrometry" [J. Chromatogr. B 1020 (2016) 111-119].

Liang X, Van Parys M, Ding X, Zeng N, Bi L, Dorshorst D, McKnight J, Milanowski D, Mao J, Chen Y, Ware JA, Dean B, Hop CECA, Deng Y.

J Chromatogr B Analyt Technol Biomed Life Sci. 2016 Sep 1;1029-1030:239. doi: 10.1016/j.jchromb.2016.06.023. Epub 2016 Jul 16. No abstract available.


Chemical Structure and Concentration of Intratumor Catabolites Determine Efficacy of Antibody Drug Conjugates.

Zhang D, Yu SF, Ma Y, Xu K, Dragovich PS, Pillow TH, Liu L, Del Rosario G, He J, Pei Z, Sadowsky JD, Erickson HK, Hop CE, Khojasteh SC.

Drug Metab Dispos. 2016 Sep;44(9):1517-23. doi: 10.1124/dmd.116.070631. Epub 2016 Jul 14.


An Automated High-Throughput Metabolic Stability Assay Using an Integrated High-Resolution Accurate Mass Method and Automated Data Analysis Software.

Shah P, Kerns E, Nguyen DT, Obach RS, Wang AQ, Zakharov A, McKew J, Simeonov A, Hop CE, Xu X.

Drug Metab Dispos. 2016 Oct;44(10):1653-61. doi: 10.1124/dmd.116.072017. Epub 2016 Jul 14.


A clinical drug-drug interaction study to evaluate the effect of a proton-pump inhibitor, a combined P-glycoprotein/cytochrome 450 enzyme (CYP)3A4 inhibitor, and a CYP2C9 inhibitor on the pharmacokinetics of vismodegib.

Malhi V, Colburn D, Williams SJ, Hop CE, Dresser MJ, Chandra P, Graham RA.

Cancer Chemother Pharmacol. 2016 Jul;78(1):41-9. doi: 10.1007/s00280-016-3020-z. Epub 2016 May 6.


Elucidating the Mechanism of Tofacitinib Oxidative Decyanation.

Le H, Fan PW, Wong S, Ma S, Driscoll JP, Hop CE, Cyrus Khojasteh S.

Drug Metab Lett. 2016;10(2):136-43.


Absorption, metabolism and excretion of cobimetinib, an oral MEK inhibitor, in rats and dogs.

Takahashi RH, Ma S, Yue Q, Kim-Kang H, Yi Y, Ly J, Boggs JW, Fettes A, McClory A, Deng Y, Hop CE, Khojasteh SC, Choo EF.

Xenobiotica. 2017 Jan;47(1):50-65. doi: 10.3109/00498254.2016.1157645. Epub 2016 Apr 8.


Simultaneous determination of itraconazole, hydroxy itraconazole, keto itraconazole and N-desalkyl itraconazole concentration in human plasma using liquid chromatography with tandem mass spectrometry.

Liang X, Van Parys M, Ding X, Zeng N, Bi L, Dorshort D, McKnight J, Milanowski D, Mao J, Chen Y, Ware JA, Dean B, Hop CE, Deng Y.

J Chromatogr B Analyt Technol Biomed Life Sci. 2016 May 1;1020:111-9. doi: 10.1016/j.jchromb.2016.03.039. Epub 2016 Mar 26. Erratum in: J Chromatogr B Analyt Technol Biomed Life Sci. 2016 Sep 1;1029-1030:239.


Evaluation of Time Dependent Inhibition Assays for Marketed Oncology Drugs: Comparison of Human Hepatocytes and Liver Microsomes in the Presence and Absence of Human Plasma.

Mao J, Tay S, Khojasteh CS, Chen Y, Hop CE, Kenny JR.

Pharm Res. 2016 May;33(5):1204-19. doi: 10.1007/s11095-016-1865-9. Epub 2016 Feb 11.


Surrogate analyte approach for quantitation of endogenous NAD(+) in human acidified blood samples using liquid chromatography coupled with electrospray ionization tandem mass spectrometry.

Liu L, Cui Z, Deng Y, Dean B, Hop CE, Liang X.

J Chromatogr B Analyt Technol Biomed Life Sci. 2016 Feb 1;1011:69-76. doi: 10.1016/j.jchromb.2015.12.040. Epub 2015 Dec 24.


Development of a Physiologically Based Pharmacokinetic Model for Itraconazole Pharmacokinetics and Drug-Drug Interaction Prediction.

Chen Y, Ma F, Lu T, Budha N, Jin JY, Kenny JR, Wong H, Hop CE, Mao J.

Clin Pharmacokinet. 2016 Jun;55(6):735-49. doi: 10.1007/s40262-015-0352-5.


Absorption, Metabolism, Excretion, and the Contribution of Intestinal Metabolism to the Oral Disposition of [14C]Cobimetinib, a MEK Inhibitor, in Humans.

Takahashi RH, Choo EF, Ma S, Wong S, Halladay J, Deng Y, Rooney I, Gates M, Hop CE, Khojasteh SC, Dresser MJ, Musib L.

Drug Metab Dispos. 2016 Jan;44(1):28-39. doi: 10.1124/dmd.115.066282. Epub 2015 Oct 8.


A novel reaction mediated by human aldehyde oxidase: amide hydrolysis of GDC-0834.

Sodhi JK, Wong S, Kirkpatrick DS, Liu L, Khojasteh SC, Hop CE, Barr JT, Jones JP, Halladay JS.

Drug Metab Dispos. 2015 Jun;43(6):908-15. doi: 10.1124/dmd.114.061804. Epub 2015 Apr 6.


Prediction of drug distribution in subcutaneous xenografts of human tumor cell lines and healthy tissues in mouse: application of the tissue composition-based model to antineoplastic drugs.

Poulin P, Chen YH, Ding X, Gould SE, Hop CE, Messick K, Oeh J, Liederer BM.

J Pharm Sci. 2015 Apr;104(4):1508-21. doi: 10.1002/jps.24336. Epub 2015 Jan 14.


Interspecies variability in expression of hepatobiliary transporters across human, dog, monkey, and rat as determined by quantitative proteomics.

Wang L, Prasad B, Salphati L, Chu X, Gupta A, Hop CE, Evers R, Unadkat JD.

Drug Metab Dispos. 2015 Mar;43(3):367-74. doi: 10.1124/dmd.114.061580. Epub 2014 Dec 22.


Quantitative transporter proteomics by liquid chromatography with tandem mass spectrometry: addressing methodologic issues of plasma membrane isolation and expression-activity relationship.

Kumar V, Prasad B, Patilea G, Gupta A, Salphati L, Evers R, Hop CE, Unadkat JD.

Drug Metab Dispos. 2015 Feb;43(2):284-8. doi: 10.1124/dmd.114.061614. Epub 2014 Dec 8.


Physiologically based pharmacokinetic modeling to predict drug-drug interactions involving inhibitory metabolite: a case study of amiodarone.

Chen Y, Mao J, Hop CE.

Drug Metab Dispos. 2015 Feb;43(2):182-9. doi: 10.1124/dmd.114.059311. Epub 2014 Oct 16.


Rational use of plasma protein and tissue binding data in drug design.

Liu X, Wright M, Hop CE.

J Med Chem. 2014 Oct 23;57(20):8238-48. doi: 10.1021/jm5007935. Epub 2014 Aug 6. Review.


Measuring NAD(+) levels in mouse blood and tissue samples via a surrogate matrix approach using LC-MS/MS.

Liang X, Yang L, Qin AR, Ly J, Liederer BM, Messick K, Ma S, Zak M, Dragovich PS, Dean BJ, Hop CE, Deng Y.

Bioanalysis. 2014 Jun;6(11):1445-57. doi: 10.4155/bio.14.8. Erratum in: Bioanalysis. 2014;6(13):1870.


Dose-dependent exposure and metabolism of GNE-892, a β-secretase inhibitor, in monkeys: contributions by P450, AO, and P-gp.

Takahashi R, Ma S, Yue Q, Kim-Kang H, Yi Y, Lyssikatos JP, Regal K, Hunt KW, Kallan NC, Siu M, Hop CE, Liu X, Khojasteh SC.

Eur J Drug Metab Pharmacokinet. 2015 Jun;40(2):171-85. doi: 10.1007/s13318-014-0198-5. Epub 2014 Apr 3.


Elucidating the mechanism of cytochrome P450-mediated pyrimidine ring conversion to pyrazole metabolites with the BACE1 inhibitor GNE-892 in rats.

Takahashi R, Ma S, Deese A, Yue Q, Kim-Kang H, Yi Y, Siu M, Hunt KW, Kallan NC, Hop CE, Liu X, Khojasteh SC.

Drug Metab Dispos. 2014 May;42(5):890-8. doi: 10.1124/dmd.114.057141. Epub 2014 Mar 4.


1-Aminobenzotriazole coincubated with (S)-warfarin results in potent inactivation of CYP2C9.

Sodhi JK, Ford KA, Mukadam S, Wong S, Hop CE, Khojasteh SC, Halladay JS.

Drug Metab Dispos. 2014 May;42(5):813-7. doi: 10.1124/dmd.113.055913. Epub 2014 Feb 18.


Assessment of the hepatic CYP reductase null mouse model and its potential application in drug discovery.

Boggs JW, Hop CE, McNamara E, Deng Y, Messick K, West K, Choo EF.

Mol Pharm. 2014 Mar 3;11(3):1062-8. doi: 10.1021/mp400556x. Epub 2014 Jan 29.


Investigations into the mechanisms of pyridine ring cleavage in vismodegib.

Khojasteh SC, Yue Q, Ma S, Castanedo G, Chen JZ, Lyssikatos J, Mulder T, Takahashi R, Ly J, Messick K, Jia W, Liu L, Hop CE, Wong H.

Drug Metab Dispos. 2014 Mar;42(3):343-51. doi: 10.1124/dmd.113.055715. Epub 2014 Jan 3.


Interindividual variability in hepatic organic anion-transporting polypeptides and P-glycoprotein (ABCB1) protein expression: quantification by liquid chromatography tandem mass spectroscopy and influence of genotype, age, and sex.

Prasad B, Evers R, Gupta A, Hop CE, Salphati L, Shukla S, Ambudkar SV, Unadkat JD.

Drug Metab Dispos. 2014 Jan;42(1):78-88. doi: 10.1124/dmd.113.053819. Epub 2013 Oct 11.


Learning and confirming with preclinical studies: modeling and simulation in the discovery of GDC-0917, an inhibitor of apoptosis proteins antagonist.

Wong H, Gould SE, Budha N, Darbonne WC, Kadel EE 3rd, La H, Alicke B, Halladay JS, Erickson R, Portera C, Tolcher AW, Infante JR, Mamounas M, Flygare JA, Hop CE, Fairbrother WJ.

Drug Metab Dispos. 2013 Dec;41(12):2104-13. doi: 10.1124/dmd.113.053926. Epub 2013 Sep 16.


Mechanistic pharmacokinetic-pharmacodynamic modeling of BACE1 inhibition in monkeys: development of a predictive model for amyloid precursor protein processing.

Liu X, Wong H, Scearce-Levie K, Watts RJ, Coraggio M, Shin YG, Peng K, Wildsmith KR, Atwal JK, Mango J, Schauer SP, Regal K, Hunt KW, Thomas AA, Siu M, Lyssikatos J, Deshmukh G, Hop CE.

Drug Metab Dispos. 2013 Jul;41(7):1319-28. doi: 10.1124/dmd.112.050864. Epub 2013 Apr 12.


Correlation of tissue-plasma partition coefficients between normal tissues and subcutaneous xenografts of human tumor cell lines in mouse as a prediction tool of drug penetration in tumors.

Poulin P, Hop CE, Salphati L, Liederer BM.

J Pharm Sci. 2013 Apr;102(4):1355-69. doi: 10.1002/jps.23452. Epub 2013 Jan 18.


High-throughput liquid chromatography/mass spectrometry method for the quantitation of small molecules using accurate mass technologies in supporting discovery drug screening.

Ding X, Ghobarah H, Zhang X, Jaochico A, Liu X, Deshmukh G, Liederer BM, Hop CE, Dean B.

Rapid Commun Mass Spectrom. 2013 Feb 15;27(3):401-8. doi: 10.1002/rcm.6461.


Evaluation of metabolism and disposition of GDC-0152 in rats using 14C labeling strategy at two different positions: a novel formation of hippuric acid from 4-phenyl-5-amino-1,2,3-thiadiazole.

Yue Q, Mulder T, Rudewicz PJ, Solon E, Budha N, Ware JA, Lyssikatos J, Hop CE, Wong H, Khojasteh SC.

Drug Metab Dispos. 2013 Feb;41(2):508-17. doi: 10.1124/dmd.112.047019. Epub 2012 Dec 4.


Comparative assessment of In Vitro-In Vivo extrapolation methods used for predicting hepatic metabolic clearance of drugs.

Poulin P, Hop CE, Ho Q, Halladay JS, Haddad S, Kenny JR.

J Pharm Sci. 2012 Nov;101(11):4308-26. doi: 10.1002/jps.23288. Epub 2012 Aug 13.


Dogs are more sensitive to antagonists of inhibitor of apoptosis proteins than rats and humans: a translational toxicokinetic/toxicodynamic analysis.

Wong H, Budha NR, West K, Blackwood E, Ware JA, Yu R, Darbonne WC, Gould SE, Steigerwalt R, Erickson R, Hop CE, LoRusso P, Eckhardt SG, Wagner A, Chan IT, Mamounas M, Flygare JA, Fairbrother WJ.

Toxicol Sci. 2012 Nov;130(1):205-13. doi: 10.1093/toxsci/kfs235. Epub 2012 Jul 28.


Radiolabeled mass-balance excretion and metabolism studies in laboratory animals: a commentary on why they are still necessary.

White RE, Evans DC, Hop CE, Moore DJ, Prakash C, Surapaneni S, Tse FL.

Xenobiotica. 2013 Feb;43(2):219-25; discussion 226-7. doi: 10.3109/00498254.2012.706724. Epub 2012 Jul 18.


Validation and application of a liquid chromatography-tandem mass spectrometric method for the determination of GDC-0879 and its metabolite in dog plasma using solid phase extraction.

Chou B, Adler RS, Meng M, Percey S, Dean B, Hop CE, Shin YG.

J Pharm Biomed Anal. 2012 Nov;70:354-61. doi: 10.1016/j.jpba.2012.05.029. Epub 2012 Jun 1.


Antitumor activity of targeted and cytotoxic agents in murine subcutaneous tumor models correlates with clinical response.

Wong H, Choo EF, Alicke B, Ding X, La H, McNamara E, Theil FP, Tibbitts J, Friedman LS, Hop CE, Gould SE.

Clin Cancer Res. 2012 Jul 15;18(14):3846-55. doi: 10.1158/1078-0432.CCR-12-0738. Epub 2012 May 30.

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