Alfin D. N. Vaz

TL;DR: The pharmacokinetic characterization of tofacitinib has been consistent with its clinical experience in drug-drug interaction studies, and Cytochrome P450 (P450) profiling indicated that tofacItinib was mainly metabolized by CYP3A4, with a smaller contribution from CYP2C19.

TL;DR: The data suggest that ertugliflozin is well absorbed in humans, and eliminated largely via glucuronidation, suggestive of moderate metabolic elimination in humans.

TL;DR: To gain from the application of deuteration as a strategy to alter drug pharmacokinetics, these studies demonstrate the importance of understanding the systemic clearance mechanism and knowing the identity of the metabolic enzymes involved, the extent to which they contribute to metabolic clearance, and the degree to which metabolism contributes to the systemic cleared.

TL;DR: Members of this series of LpxC inhibitors have improved solubility and free fraction when compared to compounds in the previously described biphenyl methylsulfone hydroxamate series, and they maintain superior Gram-negative antibacterial activity to comparator agents.

TL;DR: Findings are consistent with bioactivation sequences involving aromatic hydroxylation of the 3-chlorophenyl-ring in trazodone followed by the two-electron oxidation of this metabolite to a reactive quinone-imine intermediate and oxidation of the pyridinone ring to an electrophilic epoxide.