Understanding Interindividual Variability in the Drug Interaction of a Highly Extracted CYP1A2 Substrate Tizanidine: Application of a Permeability-Limited Multicompartment Liver Model in a Population Based Physiologically Based Pharmacokinetic Framework

Understanding Interindividual Variability in the Drug Interaction of a Highly Extracted CYP1A2 Substrate Tizanidine: Application of a Permeability-Limited Multicompartment Liver Model in a Population Based Physiologically Based Pharmacokinetic Framework

Authors: Zhang M, Fisher C, Gardner I, Pan X, Kilford P, Bois FY, Jamei M
Publication: Drug Metab Dispos
Keywords: drug interaction, drug pharmacokinetics, hepatic metabolism, liver model, PBPK modeling
Division: PBPK

Tizanidine, a centrally acting skeletal muscle relaxant, is predominantly metabolized by CYP1A2 and undergoes extensive hepatic first-pass metabolism after oral administration.

Simulation of febuxostat pharmacokinetics in healthy subjects and patients with impaired kidney function using physiologically based pharmacokinetic modeling

Simulation of febuxostat pharmacokinetics in healthy subjects and patients with impaired kidney function using physiologically based pharmacokinetic modeling

Authors: Xu Y, Chen J, Ruan Z
Publication: Biopharm Drug Dispos
Keywords: biopharmaceutics, disease model, gastroplus, pbbm, PBPK modeling, physiologically based pharmacokinetics, renal impairment, virtual populations
Software: GastroPlus®

Febuxostat is recommended by the American College of Rheumatology Gout Management Guidelines as a first-line therapy for lowering the level of urate in patients with gout.

Impact of Composition and Morphology of Ketoconazole-Loaded Solid Lipid Nanoparticles on Intestinal Permeation and Gastroplus-Based Prediction Studies

Impact of Composition and Morphology of Ketoconazole-Loaded Solid Lipid Nanoparticles on Intestinal Permeation and Gastroplus-Based Prediction Studies

Authors: Aljurbui SJ, Hussain A, Yusuf M, Ramzan M, Afzal O, Almohaywi B, Yasmin S, Altamimi ASA
Publication: ACS Omega
Keywords: gastroplus, mechanistic absorption model, pbbm, physiologically based biopharmaceutics modeling
Software: GastroPlus®

Ketoconazole (KTZ) is a potential oral antifungal agent to control systemic and local infections.

Machine Learning guided early drug discovery of small molecules

Machine Learning guided early drug discovery of small molecules

Authors: Pillai N, Dasgupta A, Sudsakorn S, Fretland J, Mavroudisa PD
Publication: Drug Discov Today
Keywords: Candidate selection, drug discovery, machine learning, Molecular screening, Small molecules
Software: ADMET Predictor®

Machine learning (ML) approaches have been widely adopted within the early stages of the drug discovery process, particularly within the context of small-molecule drug...

Absence of association between abatacept exposure levels and initial infection in patients with RA: a post hoc analysis of the randomized, placebo-controlled AVERT-2 study

Absence of association between abatacept exposure levels and initial infection in patients with RA: a post hoc analysis of the randomized, placebo-controlled AVERT-2 study

Authors: Emery P, Fleischmann R, Wong R, Lozenski K, Tanaka Y, Bykerk V, Bingham CO, Huizinga TWJ, Citera G, Elbez Y, Perera V, Murthy B, Fellows Maxwell K, Passarell JA, Hedrich W, Williams D
Conference: EULAR
Keywords: abatacept, AVERT-2, RA, rheumatoid arthritis
Division: Clinical Pharmacology and Pharmacometrics (CPP)

Infections are the most commonly reported AEs in patients with RA treated with immunosuppressive therapies, and