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In Vitro Characterization of Ertugliflozin Metabolism by UDP-Glucuronosyltransferase and Cytochrome P450 Enzymes

Autor: Jian Lin, Kimberly Lapham, Ernesto Callegari, Julie Cianfrogna, Christine C. Orozco, Raman Sharma, Mark Niosi, Theunis C. Goosen

Publikováno v: Drug metabolism and disposition: the biological fate of chemicals. 48(12)

Ertugliflozin is primarily cleared through UDP-glucurosyltransferase (UGT)–mediated metabolism (86%) with minor oxidative clearance (12%). In vitro phenotyping involved enzyme kinetic characterization of UGTs or cytochrome P450 enzymes catalyzing f

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c5f829ffbea55140205a3e462fa347f3
https://pubmed.ncbi.nlm.nih.gov/33020067

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6-Chloro-5-[4-(1-Hydroxycyclobutyl)Phenyl]-1H-Indole-3-Carboxylic Acid is a Highly Selective Substrate for Glucuronidation by UGT1A1, Relative toβ-Estradiol

Autor: Kimberly Lapham, Jian Lin, Jonathan J. Novak, Heather Eng, Theunis C. Goosen, Li Di, Amit S. Kalgutkar, Kimberly O. Cameron, Mark Niosi, Christine C. Orozco, Sangwoo Ryu, Keith Riccardi

Publikováno v: Drug Metabolism and Disposition. 46:1836-1846

6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic acid (PF-06409577) is a direct activator of the human β1-containing adenosine monophosphate-activated protein kinase (ΑMPK) isoforms. The clearance mechanism of PF-06409577 in animal

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::8a21e8671f0b104eab298f3d27ba8a2f
https://doi.org/10.1124/dmd.118.083709

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Data Generated by Quantitative Liquid Chromatography-Mass Spectrometry Proteomics Are Only the Start and Not the Endpoint: Optimization of Quantitative Concatemer-Based Measurement of Hepatic Uridine-5′-Diphosphate–Glucuronosyltransferase Enzymes with Reference to Catalytic Activity

Autor: Jill Barber, Zubida M. Al-Majdoub, Jonathan J. Novak, Theunis C. Goosen, Amin Rostami-Hodjegan, Brahim Achour, Alyssa Dantonio, Mark Niosi

Publikováno v: Drug Metabolism and Disposition. 46:805-812

Quantitative proteomic methods require optimization at several stages, including sample preparation, liquid chromatography-tandem mass spectrometry (LC-MS/MS), and data analysis, with the final analysis stage being less widely appreciated by end-user

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d8d20722785c35b1d8852ca7fbab70a4
https://doi.org/10.1124/dmd.117.079475

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A sensitive method for the quantitation of the peptide-based glucagon-like peptide-1 receptor agonist liraglutide in plasma using microfluidics chromatography tandem MS

Autor: Christopher L Holliman, Heather Eng, Amit S. Kalgutkar, Amanda King-Ahmad, Mark Niosi

Publikováno v: Bioanalysis. 10:357-368

Aim: An LC–MS/MS assay for the quantitation of liraglutide, a peptide-based injectable glucagon-like peptide-1 receptor agonist, has been developed as a convenient alternative to the enzyme-linked immunosorbent assay, and used to characterize lirag

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bb113f88700ee23a7c74cd5faf268354
https://doi.org/10.4155/bio-2017-0239

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Quantitative Characterization of Major Hepatic UDP-Glucuronosyltransferase Enzymes in Human Liver Microsomes: Comparison of Two Proteomic Methods and Correlation with Catalytic Activity

Autor: John K. Fallon, Alyssa Dantonio, Theunis C. Goosen, Jill Barber, Philip C. Smith, Amin Rostami-Hodjegan, Mark Niosi, Jonathan J. Novak, Brahim Achour

Publikováno v: Achour, B, Dantonio, A, Niosi, M, Novak, J J, Fallon, J K, Barber, J, Smith, P C, Rostami-Hochaghan, A & Goosen, T C 2017, ' Quantitative Characterization of Major Hepatic UDP-Glucuronosyltransferase Enzymes in Human Liver Microsomes : Comparison of Two Proteomic Methods and Correlation with Catalytic Activity ', Drug Metabolism and Disposition, vol. 45, no. 10, pp. 1102-1112 . https://doi.org/10.1124/dmd.117.076703

Quantitative characterization of UDP-glucuronosyltransferase (UGT) enzymes is valuable in glucuronidation reaction phenotyping, predicting metabolic clearance and drug-drug interactions using extrapolation exercises based on pharmacokinetic modeling.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::339bd84bea6db293e6c6362b447e9601
https://doi.org/10.1124/dmd.117.076703

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Novel Method to Predict In Vivo Liver-to-Plasma Kpuu for OATP Substrates Using Suspension Hepatocytes

Autor: John Litchfield, Jian Lin, Mark Niosi, Wenyi Hua, Sangwoo Ryu, Keith Riccardi, Rachel E. Kosa, Karen Atkinson, Li Di, Zhenhong Li

Publikováno v: Drug Metabolism and Disposition. 45:576-580

The ability to predict human liver-to-plasma unbound partition coefficient (Kpuu) is of great importance to estimate unbound liver concentration, develop PK/PD relationships, predict efficacy and toxicity in the liver, and model the drug-drug interac

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::0ac8dc96e10cce61792059396d3ec19c
https://doi.org/10.1124/dmd.116.074575

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