Metabolic activation of drugs by cytochrome P450 enzymes: Biochemical insights into mechanism-based inactivation by fibroblast growth factor receptor inhibitors and chemical approaches to attenuate reactive metabolite formation

Direct and Sequential Bioactivation of Pemigatinib to Reactive Iminium Ion Intermediates Culminate in Mechanism-Based Inactivation of Cytochrome P450 3A

(2022) Lloyd Wei Tat Tang et al.   DRUG METABOLISM AND DISPOSITION

Metabolic Activation of the Acrylamide Michael Acceptor Warhead in Futibatinib to an Epoxide Intermediate Engenders Covalent Inactivation of Cytochrome P450 3A

(2022) Lloyd Wei Tat Tang et al.   DRUG METABOLISM AND DISPOSITION

The Ascension of Targeted Covalent Inhibitors

(2022) Juswinder Singh   JOURNAL OF MEDICINAL CHEMISTRY

Quantification of the irreversible fibroblast growth factor receptor inhibitor futibatinib by UPLC-MS/MS: Application to the metabolic stability assay in human liver microsomes for the estimation of its in vitro hepatic intrinsic clearance

(2022) Lloyd Wei Tat Tang et al.   JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS

Identification of Infigratinib as a Potent Reversible Inhibitor and Mechanism-Based Inactivator of CYP2J2: Nascent Evidence for a Potential In Vivo Metabolic Drug-Drug Interaction with Rivaroxaban

(2022) Lloyd Wei Tat Tang et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Site-directed deuteration of dronedarone preserves cytochrome P4502J2 activity and mitigates its cardiac adverse effects in canine arrhythmic hearts

(2022) Aneesh V. Karkhanis et al.   Acta Pharmaceutica Sinica B

Mechanism-based Inactivation of Cytochrome P450 3A4 by Benzbromarone

(2021) Lloyd Wei Tat Tang et al.   MOLECULAR PHARMACOLOGY

An exploratory analysis of effects of poyendarone, a deuterated analogue of dronedarone, on the canine model of paroxysmal atrial fibrillation

(2021) Ryuichi Kambayashi et al.   NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY

Mechanism-Based Inactivation of Cytochrome P450 3A4 and 3A5 by the Fibroblast Growth Factor Receptor Inhibitor Erdafitinib

(2021) Lloyd Wei Tat Tang et al.   CHEMICAL RESEARCH IN TOXICOLOGY

Infigratinib is a Reversible Inhibitor and Mechanism-based Inactivator of Cytochrome P450 3A4

(2021) Lloyd Wei Tat Tang et al.   DRUG METABOLISM AND DISPOSITION

Infigratinib: First Approval

(2021) Connie Kang   DRUGS

Evaluation of drug-drug interactions of pemigatinib in healthy participants

(2021) Tao Ji et al.   EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY

Discovery of Pemigatinib: A Potent and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor

(2021) Liangxing Wu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Differential Reversible and Irreversible Interactions between Benzbromarone and Human Cytochrome P450s 3A4 and 3A5

(2021) Lloyd Wei Tat Tang et al.   MOLECULAR PHARMACOLOGY

How the Deuteration of Dronedarone Can Modify Its Cardiovascular Profile: In Vivo Characterization of Electropharmacological Effects of Poyendarone, a Deuterated Analogue of Dronedarone

(2020) Ryuichi Kambayashi et al.   Cardiovascular Toxicology

FOENIX-CCA2: A phase II, open-label, multicenter study of futibatinib in patients (pts) with intrahepatic cholangiocarcinoma (iCCA) harboring FGFR2 gene fusions or other rearrangements.

(2020) Lipika Goyal et al.   JOURNAL OF CLINICAL ONCOLOGY

Pemigatinib for previously treated, locally advanced or metastatic cholangiocarcinoma: a multicentre, open-label, phase 2 study

(2020) Ghassan K Abou-Alfa et al.   LANCET ONCOLOGY

INCB054828 (pemigatinib), a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3, displays activity against genetically defined tumor models

(2020) Phillip C. C. Liu et al.   PLoS One

Fibroblast growth factor receptor (FGFR) inhibitors: A review of a novel therapeutic class

(2020) April Weaver et al.   JOURNAL OF ONCOLOGY PHARMACY PRACTICE

Erdafitinib: First Global Approval

(2019) Anthony Markham   DRUGS

Resistance Mechanisms to Targeted Therapies inROS1+andALK+Non–small Cell Lung Cancer

(2018) Caroline E. McCoach et al.   CLINICAL CANCER RESEARCH

Dronedarone-Induced Cardiac Mitochondrial Dysfunction and Its Mitigation by Epoxyeicosatrienoic Acids

(2018) Aneesh Karkhanis et al.   TOXICOLOGICAL SCIENCES

Review of deutetrabenazine: a novel treatment for chorea associated with Huntington's disease

(2018) Marissa Dean et al.   Drug Design Development and Therapy

A phase Ib study of BGJ398, a pan-FGFR kinase inhibitor in combination with imatinib in patients with advanced gastrointestinal stromal tumor

(2018) Ciara M. Kelly et al.   INVESTIGATIONAL NEW DRUGS

Evaluation of BGJ398, a Fibroblast Growth Factor Receptor 1-3 Kinase Inhibitor, in Patients With Advanced Solid Tumors Harboring Genetic Alterations in Fibroblast Growth Factor Receptors: Results of a Global Phase I, Dose-Escalation and Dose-Expansion Study

(2017) Lucia Nogova et al.   JOURNAL OF CLINICAL ONCOLOGY

Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor

(2017) Timothy P.S. Perera et al.   MOLECULAR CANCER THERAPEUTICS

Multiple modes of inhibition of human cytochrome P450 2J2 by dronedarone, amiodarone and their active metabolites

(2016) Aneesh Karkhanis et al.   BIOCHEMICAL PHARMACOLOGY

Immune Checkpoint Targeting in Cancer Therapy: Toward Combination Strategies with Curative Potential

(2015) Padmanee Sharma et al.   CELL

Targeting FGFR Signaling in Cancer

(2015) M. Touat et al.   CLINICAL CANCER RESEARCH

The FGFR Landscape in Cancer: Analysis of 4,853 Tumors by Next-Generation Sequencing

(2015) T. Helsten et al.   CLINICAL CANCER RESEARCH

Mechanism-based inactivation of CYP450 enzymes: a case study of lapatinib

(2015) Han Kiat Ho et al.   DRUG METABOLISM REVIEWS

Mechanisms of drug-induced liver injury

(2014) Camilla Stephens et al.   Current Opinion in Allergy and Clinical Immunology

Drug resistance to targeted therapies: Déjà vu all over again

(2014) Floris H. Groenendijk et al.   Molecular Oncology

Using Deuterium in Drug Discovery: Leaving the Label in the Drug

(2013) Thomas G. Gant   JOURNAL OF MEDICINAL CHEMISTRY

Crizotinib versus Chemotherapy in Advanced ALK-Positive Lung Cancer

(2013) Alice T. Shaw et al.   NEW ENGLAND JOURNAL OF MEDICINE

Cytochrome P450 enzymes in drug metabolism: Regulation of gene expression, enzyme activities, and impact of genetic variation

(2013) Ulrich M. Zanger et al.   PHARMACOLOGY & THERAPEUTICS

Deuterated Clopidogrel Analogues as a New Generation of Antiplatelet Agents

(2013) Yaoqiu Zhu et al.   ACS Medicinal Chemistry Letters

Enhanced Plasma Concentration by Selective Deuteration of Rofecoxib in Rats

(2012) Frank Schneider et al.   ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH

Clinical perspectives for irreversible tyrosine kinase inhibitors in cancer

(2012) Caterina Carmi et al.   BIOCHEMICAL PHARMACOLOGY

Drug discovery for a new generation of covalent drugs

(2012) Amit S Kalgutkar et al.   Expert Opinion on Drug Discovery

Drug safety evaluation of dronedarone in atrial fibrillation

(2012) Gaetano M De Ferrari et al.   Expert Opinion On Drug Safety

Mechanism-Based Inactivation (MBI) of Cytochrome P450 Enzymes: Structure–Activity Relationships and Discovery Strategies To Mitigate Drug–Drug Interaction Risks

(2012) Suvi T. M. Orr et al.   JOURNAL OF MEDICINAL CHEMISTRY

Survival in BRAF V600–Mutant Advanced Melanoma Treated with Vemurafenib

(2012) Jeffrey A. Sosman et al.   NEW ENGLAND JOURNAL OF MEDICINE

Hallmarks of Cancer: The Next Generation

(2011) Douglas Hanahan et al.   CELL

Improved Survival with Vemurafenib in Melanoma with BRAF V600E Mutation

(2011) Paul B. Chapman et al.   NEW ENGLAND JOURNAL OF MEDICINE

Liver injury caused by drugs: an update

(2011) G Stirnimann et al.   SWISS MEDICAL WEEKLY

Mechanisms of Drug Toxicity and Relevance to Pharmaceutical Development

(2010) F. Peter Guengerich   Drug Metabolism and Pharmacokinetics

Hepatotoxicity and hepatic metabolism of available drugs: current problems and possible solutions in preclinical stages

(2010) Shibashish Giri et al.   Expert Opinion on Drug Metabolism & Toxicology

Metabolites in Safety Testing (MIST): Considerations of Mechanisms of Toxicity with Dose, Abundance, and Duration of Treatment

(2009) Dennis A. Smith et al.   CHEMICAL RESEARCH IN TOXICOLOGY

Structural Alerts, Reactive Metabolites, and Protein Covalent Binding: How Reliable Are These Attributes as Predictors of Drug Toxicity?

(2009) Amit S. Kalgutkar et al.   CHEMISTRY & BIODIVERSITY

Dronedarone

(2009) Chinmay Patel et al.   CIRCULATION

A Benefit-Risk Assessment of Benzbromarone in the Treatment of Gout

(2009) Ming-Han H Lee et al.   DRUG SAFETY

Investigation of the role of the thiazolidinedione ring of troglitazone in inducing hepatotoxicity

(2009) Sudipta Saha et al.   TOXICOLOGY LETTERS

Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation

(2008) Ulrich M. Zanger et al.   ANALYTICAL AND BIOANALYTICAL CHEMISTRY

Cholangiocarcinoma

(2008) Stefania Mosconi et al.   CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY

Increased Mortality after Dronedarone Therapy for Severe Heart Failure

(2008) Lars Køber et al.   NEW ENGLAND JOURNAL OF MEDICINE