The occurrence of idiosyncratic adverse drug reactions during late clinical trials or after a
drug has been released can lead to a severe restriction in its use and even in its withdrawal. …

Purpose: The c-MET receptor tyrosine kinase plays important roles in the formation, progression,
and dissemination of human cancer and presents an attractive therapeutic target. This …

Oxidative metabolism by the cytochromes P450 (CYPs) is the most common metabolic pathway
of drug clearance. Medicinal chemists in drug discovery often synthesize analogs of lead …

An investigation was conducted to follow up on the apparent species-dependent toxicity
reported for 6-(6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-ylthio)quinoline (…

The clinical development of fedratinib, a Janus kinase (JAK2) inhibitor, was terminated after
reports of Wernicke's encephalopathy in myelofibrosis patients. Since Wernicke's …

Biotransformation has a huge impact on the efficacy and safety of drugs. Ultimately the effects
of metabolism can be the lynchpin in the discovery and development cycle of a new drug. …

The synthesis, in vitro properties, and in vivo pharmacokinetics for a series of sulfoximine-substituted
trifluoromethylpyrimidines as inhibitors of proline-rich tyrosine kinase, a target for …

The Proviral Integration site of Moloney murine leukemia virus (PIM) serine/threonine protein
kinases are overexpressed in many hematologic and solid tumor malignancies and play …

The 14 th edition of the Workshop on Recent Issues in Bioanalysis (14 th WRIB) was held
virtually on June 15–29, 2020 with an attendance of over 1000 representatives from …

Epacadostat (EPA, INCB024360) is a first-in-class, orally active, investigational drug
targeting the enzyme indoleamine 2,3-dioxygenase 1 (IDO1). In Phase I studies, EPA has …