Investigations into the role of bioactivation in the pathogenesis of xenobiotic-induced toxicity
have been a major area of research since the link between reactive metabolites and …

Evaluation and optimization of drug metabolism and pharmacokinetic data plays an important
role in drug discovery and development and several reliable in vitro ADME models are …

Recent clinical trials using immunotherapy have demonstrated its potential to control cancer
by disinhibiting the immune system. Immune checkpoint blocking (ICB) antibodies against …

N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide (14, PHA-543,613), a
novel agonist of the α7 neuronal nicotinic acetylcholine receptor (α7 nAChR), has been …

In vitro covalent binding assessments of drugs have been useful in providing retrospective
insights into the association between drug metabolism and a resulting toxicological response. …

Optimization of isoquinolinone PI3K inhibitors led to the discovery of a potent inhibitor of
PI3K-γ (26 or IPI-549) with >100-fold selectivity over other lipid and protein kinases. IPI-549 …

The therapeutic benefits of the antidepressant nefazodone have been hampered by several
cases of acute hepatotoxicity/liver failure. Although the mechanism of hepatotoxicity remains …

ROS1 tyrosine kinase inhibitors (TKI) have been approved (crizotinib and entrectinib) or
explored (lorlatinib, taletrectinib, and repotrectinib) for the treatment of ROS1 fusion–positive …

An in vitro reactive intermediate screening assay, incorporating the use of the close analog
of glutathione, glutathione ethyl ester (GSH-EE) as a conjugating agent, was developed to …

We report herein, facile metabolite identification workflow on the anti-depressant
nefazodone, which is derived from accurate mass measurements based on a single run/experimental …