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Biotransformation and bioactivation reactions - 2017 literature highlights *.

Khojasteh SC, Miller GP, Mitra K, Rietjens IMCM.

Drug Metab Rev. 2018 Jun 28:1-35. doi: 10.1080/03602532.2018.1473875. [Epub ahead of print]


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.


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.


Dicloxacillin induces CYP2C19, CYP2C9 and CYP3A4 in vivo and in vitro.

Stage TB, Graff M, Wong S, Rasmussen LL, Nielsen F, Pottegård A, Brøsen K, Kroetz DL, Khojasteh SC, Damkier P.

Br J Clin Pharmacol. 2018 Mar;84(3):510-519. doi: 10.1111/bcp.13467. Epub 2018 Jan 10.


CYP1A1-Mediated Intramolecular Rearrangement of Aminoazepane in GDC-0339.

Takahashi RH, Wang X, Segraves NL, Wang J, Chang JH, Khojasteh SC, Ma S.

Drug Metab Dispos. 2017 Oct;45(10):1084-1092. doi: 10.1124/dmd.117.076786. Epub 2017 Aug 8.


Inhibitory Effects of Trapping Agents of Sulfur Drug Reactive Intermediates against Major Human Cytochrome P450 Isoforms.

Sodhi JK, Delarosa EM, Halladay JS, Driscoll JP, Mulder T, Dansette PM, Khojasteh SC.

Int J Mol Sci. 2017 Jul 20;18(7). pii: E1553. doi: 10.3390/ijms18071553.


Glucuronides as Potential Anionic Substrates of Human Cytochrome P450 2C8 (CYP2C8).

Ma Y, Fu Y, Khojasteh SC, Dalvie D, Zhang D.

J Med Chem. 2017 Nov 9;60(21):8691-8705. doi: 10.1021/acs.jmedchem.7b00510. Epub 2017 Jun 27. Review.


Biotransformation and bioactivation reactions - 2016 literature highlights.

Khojasteh SC, Rietjens IMCM, Dalvie D, Miller G.

Drug Metab Rev. 2017 Aug;49(3):285-317. doi: 10.1080/03602532.2017.1326498. Epub 2017 May 31. Review.


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.


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.


Going Beyond Common Drug Metabolizing Enzymes: Case Studies of Biotransformation Involving Aldehyde Oxidase, γ-Glutamyl Transpeptidase, Cathepsin B, Flavin-Containing Monooxygenase, and ADP-Ribosyltransferase.

Fan PW, Zhang D, Halladay JS, Driscoll JP, Khojasteh SC.

Drug Metab Dispos. 2016 Aug;44(8):1253-61. doi: 10.1124/dmd.116.070169. Epub 2016 Apr 26. Review.


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.


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.


Elucidating the Mechanisms of Formation for Two Unusual Cytochrome P450-Mediated Fused Ring Metabolites of GDC-0623, a MAPK/ERK Kinase Inhibitor.

Takahashi RH, Ma S, Robinson SJ, Yue Q, Choo EF, Khojasteh SC.

Drug Metab Dispos. 2015 Dec;43(12):1929-33. doi: 10.1124/dmd.115.067181. Epub 2015 Oct 5.


Bioanalytical approaches for characterizing catabolism of antibody-drug conjugates.

Saad OM, Shen BQ, Xu K, Khojasteh SC, Girish S, Kaur S.

Bioanalysis. 2015;7(13):1583-604. doi: 10.4155/bio.15.87.


Non-Clinical Disposition and Metabolism of DM1, a Component of Trastuzumab Emtansine (T-DM1), in Sprague Dawley Rats.

Shen BQ, Bumbaca D, Yue Q, Saad O, Tibbitts J, Khojasteh SC, Girish S.

Drug Metab Lett. 2015;9(2):119-31.


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.


A probabilistic method to report predictions from a human liver microsomes stability QSAR model: a practical tool for drug discovery.

Aliagas I, Gobbi A, Heffron T, Lee ML, Ortwine DF, Zak M, Khojasteh SC.

J Comput Aided Mol Des. 2015 Apr;29(4):327-38. doi: 10.1007/s10822-015-9838-3. Epub 2015 Feb 24.


Practical permeability-based hepatic clearance classification system (HepCCS) in drug discovery.

Fan PW, Song Y, Berezhkovskiy LM, Cheong J, Plise EG, Khojasteh SC.

Future Med Chem. 2014;6(18):1995-2012. doi: 10.4155/fmc.14.141.


A decades-long investigation of acute metabolism-based hepatotoxicity by herbal constituents: a case study of pennyroyal oil.

Gordon P, Khojasteh SC.

Drug Metab Rev. 2015 Feb;47(1):12-20. doi: 10.3109/03602532.2014.990032. Epub 2014 Dec 16. Review.


Mechanistic studies of the cationic binding pocket of CYP2C9 in vitro and in silico: metabolism of nonionizable analogs of tienilic acid.

Tay S, Le H, Ford KA, Nelson SD, Khojasteh SC, Rademacher PM.

Drug Metab Dispos. 2014 Nov;42(11):1955-63. doi: 10.1124/dmd.114.059022. Epub 2014 Sep 3.


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.


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.


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.


Characterization of rat liver proteins adducted by reactive metabolites of menthofuran.

Khojasteh SC, Hartley DP, Ford KA, Uppal H, Oishi S, Nelson SD.

Chem Res Toxicol. 2012 Nov 19;25(11):2301-9. doi: 10.1021/tx300144d. Epub 2012 Nov 6.


Elucidation of the mechanism of ribose conjugation in a pyrazole-containing compound in rodent liver.

Le H, Ford KA, Khojasteh SC, Fan PW.

Xenobiotica. 2013 Mar;43(3):236-45. doi: 10.3109/00498254.2012.715211. Epub 2012 Aug 30.


An 'all-inclusive' 96-well cytochrome P450 induction method: measuring enzyme activity, mRNA levels, protein levels, and cytotoxicity from one well using cryopreserved human hepatocytes.

Halladay JS, Wong S, Khojasteh SC, Grepper S.

J Pharmacol Toxicol Methods. 2012 Nov-Dec;66(3):270-5. doi: 10.1016/j.vascn.2012.07.004. Epub 2012 Jul 15.


Catabolic fate and pharmacokinetic characterization of trastuzumab emtansine (T-DM1): an emphasis on preclinical and clinical catabolism.

Shen BQ, Bumbaca D, Saad O, Yue Q, Pastuskovas CV, Khojasteh SC, Tibbitts J, Kaur S, Wang B, Chu YW, LoRusso PM, Girish S.

Curr Drug Metab. 2012 Sep 1;13(7):901-10.


Drug-drug interaction potential of marketed oncology drugs: in vitro assessment of time-dependent cytochrome P450 inhibition, reactive metabolite formation and drug-drug interaction prediction.

Kenny JR, Mukadam S, Zhang C, Tay S, Collins C, Galetin A, Khojasteh SC.

Pharm Res. 2012 Jul;29(7):1960-76. doi: 10.1007/s11095-012-0724-6. Epub 2012 Mar 14.


Evaluation of time-dependent cytochrome p450 inhibition in a high-throughput, automated assay: introducing a novel area under the curve shift approach.

Mukadam S, Tay S, Tran D, Wang L, Delarosa EM, Khojasteh SC, Halladay JS, Kenny JR.

Drug Metab Lett. 2012 Mar;6(1):43-53.


Novel mechanism for dehalogenation and glutathione conjugation of dihalogenated anilines in human liver microsomes: evidence for ipso glutathione addition.

Zhang C, Kenny JR, Le H, Deese A, Ford KA, Lightning LK, Fan PW, Driscoll JP, Halladay JS, Hop CE, Khojasteh SC.

Chem Res Toxicol. 2011 Oct 17;24(10):1668-77. doi: 10.1021/tx2002228. Epub 2011 Sep 25.


High-throughput, 384-well, LC-MS/MS CYP inhibition assay using automation, cassette-analysis technique, and streamlined data analysis.

Halladay JS, Delarosa EM, Tran D, Wang L, Wong S, Khojasteh SC.

Drug Metab Lett. 2011 Aug;5(3):220-30.


High-Throughput, 384-Well, LC-MS/MS CYP Inhibition Assay Using Automation, Cassette-Analysis Technique, and Streamlined Data Analysi.

Halladay JS, Delarosa EM, Tran D, Wang L, Wong S, Khojasteh SC.

Drug Metab Lett. 2011 Aug 9. [Epub ahead of print]


Significant species difference in amide hydrolysis of GDC-0834, a novel potent and selective Bruton's tyrosine kinase inhibitor.

Liu L, Halladay JS, Shin Y, Wong S, Coraggio M, La H, Baumgardner M, Le H, Gopaul S, Boggs J, Kuebler P, Davis JC Jr, Liao XC, Lubach JW, Deese A, Sowell CG, Currie KS, Young WB, Khojasteh SC, Hop CE, Wong H.

Drug Metab Dispos. 2011 Oct;39(10):1840-9. doi: 10.1124/dmd.111.040840. Epub 2011 Jul 8.


Absorption, distribution, metabolism, and excretion of [¹⁴C]GDC-0449 (vismodegib), an orally active hedgehog pathway inhibitor, in rats and dogs: a unique metabolic pathway via pyridine ring opening.

Yue Q, Chen YH, Mulder T, Deese A, Takahashi R, Rudewicz PJ, Reynolds M, Solon E, Hop CE, Wong H, Khojasteh SC.

Drug Metab Dispos. 2011 Jun;39(6):952-65. doi: 10.1124/dmd.110.037374. Epub 2011 Mar 1.


Chemical inhibitors of cytochrome P450 isoforms in human liver microsomes: a re-evaluation of P450 isoform selectivity.

Khojasteh SC, Prabhu S, Kenny JR, Halladay JS, Lu AY.

Eur J Drug Metab Pharmacokinet. 2011 Mar;36(1):1-16. doi: 10.1007/s13318-011-0024-2. Epub 2011 Feb 19. Review.


Metabolism and toxicity of menthofuran in rat liver slices and in rats.

Khojasteh SC, Oishi S, Nelson SD.

Chem Res Toxicol. 2010 Nov 15;23(11):1824-32. doi: 10.1021/tx100268g. Epub 2010 Oct 14.


Interplay of dissolution, solubility, and nonsink permeation determines the oral absorption of the Hedgehog pathway inhibitor GDC-0449 in dogs: an investigation using preclinical studies and physiologically based pharmacokinetic modeling.

Wong H, Theil FP, Cui Y, Marsters JC Jr, Khojasteh SC, Vernillet L, La H, Song X, Wang H, Morinello EJ, Deng Y, Hop CE.

Drug Metab Dispos. 2010 Jul;38(7):1029-38. doi: 10.1124/dmd.110.032680. Epub 2010 Apr 20.


Preclinical assessment of the absorption, distribution, metabolism and excretion of GDC-0449 (2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide), an orally bioavailable systemic Hedgehog signalling pathway inhibitor.

Wong H, Chen JZ, Chou B, Halladay JS, Kenny JR, La H, Marsters JC Jr, Plise E, Rudewicz PJ, Robarge K, Shin Y, Wong S, Zhang C, Khojasteh SC.

Xenobiotica. 2009 Nov;39(11):850-61. doi: 10.3109/00498250903180289.


On the prediction of hepatic clearance using the diluted plasma in metabolic stability assay.

Berezhkovskiy LM, Khojasteh SC, Halladay JS, Hop CE.

J Pharm Sci. 2009 Jun;98(6):1922-7. doi: 10.1002/jps.21582.


Preclinical absorption, distribution, metabolism and excretion (ADME) characterization of ICAM1988, an LFA-1/ICAM antagonist, and its prodrug.

Khojasteh SC, Leipold DD, Lai F, La H, Baumgardner MJ, Desino KE, Gudmundsson OS, Bloedow DC, Bodary SC, Reynolds ME, Gadek TR, Kenkare-Mitra S.

Xenobiotica. 2008 Mar;38(3):340-52. doi: 10.1080/00498250701813248 .


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