Publications by authors named "Amit Kalgutkar"

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Effect of Varying Degrees of Hepatic Impairment on the Pharmacokinetics of Ervogastat, a Diacylglycerol Acyltransferase 2 (DGAT2) Inhibitor, and Clesacostat, an Acetyl-CoA Carboxylase (ACC) Inhibitor.
Manoli Vourvahis, Arthur J Bergman, Adam G Ogden, Jim Hughes, James R Gosset, Amit S Kalgutkar

J Clin Pharmacol· December 2025

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Studies addressing potential bioactivation and genotoxicity liabilities of the -nitroso derivative of the antidepressant paroxetine.
Carley J S Heck, Heather Eng, Jennifer R Cheung, Joseph Tillotson, Krista L Dobo, Amit S Kalgutkar

Xenobiotica· October 2025

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Discovery of Nirmatrelvir (PF-07321332): A Potent, Orally Active Inhibitor of the Severe Acute Respiratory Syndrome Coronavirus 2 (SARS CoV-2) Main Protease.
Jamison B Tuttle, Christophe Allais, Charlotte M N Allerton, Annaliesa S Anderson, Joel T Arcari, Amit S Kalgutkar

J Med Chem· April 2025

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Discovery of First Branched-Chain Ketoacid Dehydrogenase Kinase (BDK) Inhibitor Clinical Candidate PF-07328948.
Kevin J Filipski, Luis A Martinez-Alsina, Matthew R Reese, Edelweiss Evrard, Leanne M Buzon, Amit S Kalgutkar

J Med Chem· February 2025

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A Second-Generation Oral SARS-CoV-2 Main Protease Inhibitor Clinical Candidate for the Treatment of COVID-19.
Charlotte M N Allerton, Joel T Arcari, Lisa M Aschenbrenner, Melissa Avery, Bruce M Bechle, Amit S Kalgutkar

J Med Chem· August 2024

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Bioactivation and reactivity research advances - 2023 year in review.
Shuai Wang, Upendra A Argikar, Maria Chatzopoulou, Sungjoon Cho, Rachel D Crouch, Amit S Kalgutkar

Drug Metab Rev· August 2024

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Biotransformation research advances - 2023 year in review.
S Cyrus Khojasteh, Upendra A Argikar, Maria Chatzopoulou, Lionel Cheruzel, Sungjoon Cho, Amit S Kalgutkar

Drug Metab Rev· August 2024

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A Kinetic Model for Assessing Potential Nitrosamine Carcinogenicity.
Shu Yu, J Christopher McWilliams, Olivier Dirat, Krista L Dobo, Amit S Kalgutkar

Chem Res Toxicol· August 2024

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Discovery of SARS-CoV-2 papain-like protease (PL) inhibitors with efficacy in a murine infection model.
Michelle R Garnsey, Matthew C Robinson, Luong T Nguyen, Rhonda Cardin, Joseph Tillotson, Amit S Kalgutkar

Sci Adv· August 2024

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Development of a sensitive LC-MS/MS assay to support human microdose study for an oral agonist of the GLP-1 receptor.
Eugene P Kadar, Heather Eng, Amit S Kalgutkar, Christopher L Holliman, Gregory S Steeno

Bioanalysis· June 2024

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Mechanisms of Nitrosamine Mutagenicity and Their Relationship to Rodent Carcinogenic Potency.
David J Snodin, Alejandra Trejo-Martin, David J Ponting, Graham F Smith, Andreas Czich, Amit S Kalgutkar

Chem Res Toxicol· February 2024

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Bioactivation and reactivity research advances - 2022 year in review‡.
Shuai Wang, Upendra A Argikar, Lionel Cheruzel, Sungjoon Cho, Rachel D Crouch, Amit S Kalgutkar

Drug Metab Rev· November 2023

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Biotransformation research advances - 2022 year in review.
S Cyrus Khojasteh, Upendra A Argikar, Lionel Cheruzel, Sungjoon Cho, Rachel D Crouch, Amit S Kalgutkar

Drug Metab Rev· November 2023

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Small molecule branched-chain ketoacid dehydrogenase kinase (BDK) inhibitors with opposing effects on BDK protein levels.
Rachel J Roth Flach, Eliza Bollinger, Allan R Reyes, Brigitte Laforest, Bethany L Kormos, Amit S Kalgutkar

Nat Commun· August 2023

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Mitigating a Bioactivation Liability with an Azetidine-Based Inhibitor of Diacylglycerol Acyltransferase 2 (DGAT2) En Route to the Discovery of the Clinical Candidate Ervogastat.
Raman Sharma, Matthew S Dowling, Kentaro Futatsugi, Amit S Kalgutkar

Chem Res Toxicol· June 2023

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Species differences in plasma protein binding of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease inhibitor nirmatrelvir.
Siennah R Greenfield, Heather Eng, Qingyi Yang, Chunyang Guo, Laura Byrnes, Amit S Kalgutkar

Xenobiotica· January 2023

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Metabolism and Excretion of Nirmatrelvir in Humans Using Quantitative Fluorine Nuclear Magnetic Resonance Spectroscopy: A Novel Approach for Accelerating Drug Development.
Ravi Shankar P Singh, Gregory S Walker, Eugene P Kadar, Loretta M Cox, Heather Eng, Amit S Kalgutkar

Clin Pharmacol Ther· December 2022

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Strategies for Assessing Acceptable Intakes for Novel -Nitrosamines Derived from Active Pharmaceutical Ingredients.
David J Ponting, Krista L Dobo, Michelle O Kenyon, Amit S Kalgutkar

J Med Chem· December 2022

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Discovery of Ervogastat (PF-06865571): A Potent and Selective Inhibitor of Diacylglycerol Acyltransferase 2 for the Treatment of Non-alcoholic Steatohepatitis.
Kentaro Futatsugi, Shawn Cabral, Daniel W Kung, Kim Huard, Esther Lee, Amit S Kalgutkar

J Med Chem· November 2022

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Comprehensive Nonclinical Safety Assessment of Nirmatrelvir Supporting Timely Development of the SARS-COV-2 Antiviral Therapeutic, Paxlovid™.
Jean G Sathish, Siddhartha Bhatt, Jamie K DaSilva, Declan Flynn, Stephen Jenkinson, Amit S Kalgutkar

Int J Toxicol· August 2022

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Biotransformation novel advances - 2021 year in review.
S Cyrus Khojasteh, Upendra A Argikar, Sungjoon Cho, Rachel Crouch, Carley J S Heck, Amit S Kalgutkar

Drug Metab Rev· August 2022

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Yan Weng, Kari R Fonseca, Yi-An Bi, Sumathy Mathialagan, Keith Riccardi, Amit S Kalgutkar

Drug Metab Dispos· July 2022

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A Small-Molecule Oral Agonist of the Human Glucagon-like Peptide-1 Receptor.
David A Griffith, David J Edmonds, Jean-Philippe Fortin, Amit S Kalgutkar, J Brent Kuzmiski

J Med Chem· June 2022

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Practical and Science-Based Strategy for Establishing Acceptable Intakes for Drug Product -Nitrosamine Impurities.
Krista L Dobo, Michelle O Kenyon, Olivier Dirat, Maria Engel, Andrew Fleetwood, Amit S Kalgutkar

Chem Res Toxicol· March 2022

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Pharmacokinetics, mass balance, metabolism, and excretion of the liver-targeted acetyl-CoA carboxylase inhibitor PF-05221304 (clesacostat) in humans.
Tim F Ryder, Arthur Bergman, Amanda King-Ahmad, Neeta B Amin, Manjinder S Lall, Amit S Kalgutkar

Xenobiotica· March 2022

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