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The conduct of in vitro studies to address time-dependent inhibition of drug-metabolizing enzymes: a perspective of the pharmaceutical research and manufacturers of America

Drug metabolism and disposition, 2009-07, Vol.37 (7), p.1355

2009

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AMG 837: a novel GPR40/FFA1 agonist that enhances insulin secretion and lowers glucose levels in rodents

PloS one, 2011-11, Vol.6 (11), p.e27270-e27270

2011

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DNL104, a Centrally Penetrant RIPK1 Inhibitor, Inhibits RIP1 Kinase Phosphorylation in a Randomized Phase I Ascending Dose Study in Healthy Volunteers

Clinical pharmacology and therapeutics, 2020-02, Vol.107 (2), p.406-414

2020

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An inhibitory metabolite leads to dose- and time-dependent pharmacokinetics of (R)-N-{1-[3-(4-ethoxy-phenyl)-4-oxo-3,4-dihydro-pyrido[2,3-d]pyrimidin-2-yl]-ethyl}-N-pyridin-3-yl-methyl-2-(4-trifluoromethoxy-phenyl)-acetamide (AMG 487) in human subjects after multiple dosing

Drug metabolism and disposition, 2009-03, Vol.37 (3), p.502

2009

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Application of Virtual Screening to the Identification of New LpxC Inhibitor Chemotypes, Oxazolidinone and Isoxazoline

Journal of medicinal chemistry, 2018-10, Vol.61 (20), p.9360-9370

2018

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Discovery of the imidazole-derived GPR40 agonist AM-3189

Bioorganic & medicinal chemistry letters, 2016-01, Vol.26 (1), p.15-20

2016

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Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme

Drug metabolism and disposition, 2012-07, Vol.40 (7), p.1429

2012

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SAR and Mode of Action of Novel Non-Nucleoside Inhibitors of Hepatitis C NS5b RNA Polymerase

Journal of medicinal chemistry, 2006-02, Vol.49 (3), p.1034-1046

2006

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Optimization of GPR40 Agonists for Type 2 Diabetes

ACS medicinal chemistry letters, 2014-05, Vol.5 (5), p.517-521

2014

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Bioactivation of a novel 2-methylindole-containing dual chemoattractant receptor-homologous molecule expressed on T-helper type-2 cells/D-prostanoid receptor antagonist leads to mechanism-based CYP3A inactivation: glutathione adduct characterization and prediction of in vivo drug-drug interaction

Drug metabolism and disposition, 2010-05, Vol.38 (5), p.841

2010

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DNL 104, a Centrally Penetrant RIPK 1 Inhibitor, Inhibits RIP 1 Kinase Phosphorylation in a Randomized Phase I Ascending Dose Study in Healthy Volunteers

Clinical pharmacology and therapeutics, 2020-02, Vol.107 (2), p.406-414

2020

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Diphenhydramine disposition in the sheep maternal-placental-fetal unit: gestational age, plasma drug protein binding, and umbilical blood flow effects on clearance

Drug metabolism and disposition, 2000-03, Vol.28 (3), p.279

2000

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Estimation of transplacental and nonplacental diphenhydramine clearances in the fetal lamb: the impact of fetal first-pass hepatic drug uptake

The Journal of pharmacology and experimental therapeutics, 1997-08, Vol.282 (2), p.617

1997

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Diphenhydramine disposition in the sheep maternal–Placental–Fetal unit: Determinants of plasma drug concentrations in the mother and the fetus††Abbreviations: DPHM, diphenhydramine; [2H10]DPHM, deuteriumlabeled diphenhydramine; CLmm, maternal total body clearance; CLff, fetal total body clearance; CLmf, maternal to fetal placental clearance; CLfm, fetal to maternal placental clearance; CLmo, maternal nonplacental clearance; CLfo, fetal nonplacental clearance; Cm, maternal plasma steady-state DPH

Journal of pharmaceutical sciences, 1999-12, Vol.88 (12), p.1259-1265

1999

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Clinical Drug Metabolism

Handbook of Drug Metabolism, 2019, p.551-576

3, 2019

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Intravenous and Oral Propafenone for Treatment of Tachycardia in Infants and Children: Pharmacokinetics and Clinical Response

Journal of clinical pharmacology, 1998-06, Vol.38 (6), p.496-501

1998

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Diphenhydramine disposition in the sheep maternal–Placental–Fetal unit: Determinants of plasma drug concentrations in the mother and the fetus

Journal of pharmaceutical sciences, 1999-12, Vol.88 (12), p.1259-1265

1999

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Simultaneous analysis of diphenylmethoxyacetic acid, a metabolite of diphenhydramine, and its deuterium-labeled stable isotope analog in ovine plasma and urine

Journal of chromatography. B, Biomedical applications, 1995-01, Vol.663 (1), p.67-81

1995

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In Vitro Protein Binding of Propafenone and 5-Hydroxypropafenone in Serum, in Solutions of Isolated Serum Proteins, and to Red Blood Cells

Journal of pharmaceutical sciences, 1992-11, Vol.81 (11), p.1098-1103

1992

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High-grade glioma: ESMO Clinical Practice Guidelines for diagnosis, treatment and follow-up

Annals of oncology, 2014-09, Vol.25 Suppl 3, p.iii93-iii101

2014

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Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors

Bioorganic & medicinal chemistry letters, 2013-05, Vol.23 (9), p.2743-2749

2013

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Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration

Bioorganic & medicinal chemistry letters, 2011-09, Vol.21 (18), p.5521-5527

2011

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Imidazo-pyrazine derivatives as potent CXCR3 antagonists

Bioorganic & medicinal chemistry letters, 2009-09, Vol.19 (17), p.5200-5204

2009

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Optimization of the heterocyclic core of the quinazolinone-derived CXCR3 antagonists

Bioorganic & medicinal chemistry, 2008-01, Vol.18 (2), p.688-693

2008

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The conduct of in vitro studies to address time-dependent inhibition of drug-metabolizing enzymes: a perspective of the pharmaceutical research and manufacturers of America

AMG 837: a novel GPR40/FFA1 agonist that enhances insulin secretion and lowers glucose levels in rodents

DNL104, a Centrally Penetrant RIPK1 Inhibitor, Inhibits RIP1 Kinase Phosphorylation in a Randomized Phase I Ascending Dose Study in Healthy Volunteers

An inhibitory metabolite leads to dose- and time-dependent pharmacokinetics of (R)-N-{1-[3-(4-ethoxy-phenyl)-4-oxo-3,4-dihydro-pyrido[2,3-d]pyrimidin-2-yl]-ethyl}-N-pyridin-3-yl-methyl-2-(4-trifluoromethoxy-phenyl)-acetamide (AMG 487) in human subjects after multiple dosing

Application of Virtual Screening to the Identification of New LpxC Inhibitor Chemotypes, Oxazolidinone and Isoxazoline

Discovery of the imidazole-derived GPR40 agonist AM-3189

Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme

SAR and Mode of Action of Novel Non-Nucleoside Inhibitors of Hepatitis C NS5b RNA Polymerase

Optimization of GPR40 Agonists for Type 2 Diabetes

Bioactivation of a novel 2-methylindole-containing dual chemoattractant receptor-homologous molecule expressed on T-helper type-2 cells/D-prostanoid receptor antagonist leads to mechanism-based CYP3A inactivation: glutathione adduct characterization and prediction of in vivo drug-drug interaction

DNL 104, a Centrally Penetrant RIPK 1 Inhibitor, Inhibits RIP 1 Kinase Phosphorylation in a Randomized Phase I Ascending Dose Study in Healthy Volunteers

Diphenhydramine disposition in the sheep maternal-placental-fetal unit: gestational age, plasma drug protein binding, and umbilical blood flow effects on clearance

Estimation of transplacental and nonplacental diphenhydramine clearances in the fetal lamb: the impact of fetal first-pass hepatic drug uptake

Clinical Drug Metabolism

Intravenous and Oral Propafenone for Treatment of Tachycardia in Infants and Children: Pharmacokinetics and Clinical Response

Diphenhydramine disposition in the sheep maternal–Placental–Fetal unit: Determinants of plasma drug concentrations in the mother and the fetus

Simultaneous analysis of diphenylmethoxyacetic acid, a metabolite of diphenhydramine, and its deuterium-labeled stable isotope analog in ovine plasma and urine

In Vitro Protein Binding of Propafenone and 5-Hydroxypropafenone in Serum, in Solutions of Isolated Serum Proteins, and to Red Blood Cells

High-grade glioma: ESMO Clinical Practice Guidelines for diagnosis, treatment and follow-up

Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors

Selective and Brain-Permeable Polo-like Kinase-2 (Plk-2) Inhibitors That Reduce α-Synuclein Phosphorylation in Rat Brain

Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration

Imidazo-pyrazine derivatives as potent CXCR3 antagonists

Optimization of the heterocyclic core of the quinazolinone-derived CXCR3 antagonists

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