Results 171 to 180 of about 78,269 (301)

Does Next Generation Sequencing (NGS)‐Based CYP2D6 Sequencing Improve Genotype–Phenotype Concordance in Tamoxifen‐Treated Patients?

open access: yesClinical Pharmacology &Therapeutics, EarlyView.
CYP2D6 metabolizes about 20% of commonly used drugs, including tamoxifen, a major hormone therapy for breast cancer. Although the relationship between tamoxifen pharmacokinetics and CYP2D6 genotype has been demonstrated, residual variability in drug exposure remains unexplained.
Jeanne Petit   +7 more
wiley   +1 more source

Effects of Fomepizole on Acetaminophen Oxidative Metabolism: A Randomized, Crossover Study in Human Volunteers

open access: yesClinical Pharmacology &Therapeutics, EarlyView.
Acetaminophen overdose can cause liver injury. Hepatotoxicity results from N‐acetyl‐p‐benzoquinone imine (NAPQI), generated via cytochrome P450‐2E1 (CYP2E1). Acetylcysteine is the mainstay of treatment, but efficacy may be reduced with delayed administration or large ingestions.
Sidharth Anand   +6 more
wiley   +1 more source

Combinatorial targeting of G‐protein‐coupled bile acid receptor 1 and cysteinyl leukotriene receptor 1 reveals a mechanistic role for bile acids and leukotrienes in drug‐induced liver injury

open access: yesHepatology, EarlyView., 2022
CHIN117 is a dual cysteinyl leukotriene receptor 1 (CYSLTR1) antagonist and G‐protein‐coupled bile acid receptor 1 (GPBAR1) agonist. In the liver, GPBAR1 and CYSLTR1 are coexpressed by liver sinusoidal endothelial cells (LSECs), HSCs, circulating monocytes/macrophages, and liver resident macrophages (Kupffer cells).
Michele Biagioli   +13 more
wiley   +1 more source

From Executor to Orchestrator: The Pharmacology Scientist in the Age of Agentic AI

open access: yesClinical Pharmacology &Therapeutics, EarlyView.
Drug development productivity has not improved despite five decades of computational advancement, with the probability that a compound entering Phase I achieving regulatory approval remaining near 10%. Each automation wave increased throughput while leaving the interpretive bottleneck intact; scientists continued to formulate questions, evaluate ...
Michael McCoy, Matthew McCoy
wiley   +1 more source

Exploring Cerumen as an Alternative Matrix for Drug Detection and Quantification: Method Development and Application in Clinical Samples

open access: yesDrug Testing and Analysis, EarlyView.
An LC–MS/MS method was developed for the detection of 33 psychoactive medications in cerumen (earwax) and applied to the samples of 60 psychiatric inpatient volunteers. The findings highlighted the utility of cerumen as an innovative biospecimen in clinical toxicological analysis.
Dimitrios Phaedon Kevrekidis   +5 more
wiley   +1 more source

Effects of fenfluramine and sigma‐1‐dependent pharmacological and genetic modulation in a mouse kindling model

open access: yesEpilepsia, EarlyView.
Abstract Objective Sigma‐1 is a chaperone protein that serves as a key homeostatic regulator, implicated in neuronal excitability and seizure control. Positive allosteric modulators offer a use‐dependent means to enhance Sigma‐1 activity, potentially with favorable tolerability compared to direct agonists.
Eva‐Lotta von Rüden   +5 more
wiley   +1 more source

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