Crizotinib and pazopanib are oral receptor tyrosine kinase inhibitors (TKIs).
Concentration-QT Analysis of Quizartinib in Patients With Relapsed/Refractory AML
FMS-like tyrosine kinase 3 (FLT3) is expressed in hematopoietic progenitor cells, and signaling through FLT3 promotes these cells’ proliferation and differentiation.
Zonal Extracellular Matrix (ECM) Accumulation in Nonalcoholic Steatohepatitis (NASH) Characterized by a Mathematical Model of Fibrosis
Non-alcoholic fatty liver disease (NAFLD) is of growing concern, within developed countries, with recent estimates suggesting up to, 30% of the US population may be affected.
New Approach Methods for Testing Chemicals for Endocrine Disruption Potential
Concern that chemicals in the environment can disrupt the endocrine systems of humans and ecological species (fish, frogs, birds) has driven the development of bioassays to test for endocrine activity.
Preparation of lapatinib ditosylate solid dispersions using solvent rotary evaporation and hot melt extrusion for solubility and dissolution enhancement
The objective of this study was to enhance solubility and dissolution of lapatinib (LB) ditosylate (DT) using solid dispersions (SD) prepared by solvent rotary evaporation (SRE) and hot melt extrusion (HME).
Bioformulative concepts on intracellular organ specific bioavailability
Bioavailability is an ancient but effective terminology by which the entire therapeutic efficacy of a drug directly or indirectly relays.
Role of Physiologically Based Kinetic modelling in addressing environmental chemical mixtures – a review
The role of Physiologically Based Kinetic (PBK) modelling in assessing mixture toxicology has been growing for the last three decades. It has been widely used to investigate and address interactions in mixtures.
Quantitative prediction of oral bioavailability of a lipophilic antineoplastic drug bexarotene administered in lipidic formulation using a combined in vitro lipolysis/microsomal metabolism approach
For performance assessment of the lipid-based drug delivery systems (LBDDS), in vitrolipolysis is commonly applied because traditional dissolution tests do not reflect the complicated in vivo micellar formation and solubilisation processes.
Model-based drug development in pulmonary delivery: Pharmacokinetic analysis of novel drug candidates for treatment of Pseudomonas aeruginosa lung infection
Antibiotic resistance is a major public health threat worldwide. In particular, about 80% of cystic fibrosis patients have chronic Pseudomonas aeruginosa (PA) lung infection resistant to many current antibiotics.
Estimating Predictive Uncertainty for Ensemble Regression Models by Gamma Error Analysis
The Standard Error (SE) of Prediction: a Measure of Individual Uncertainties
Galactosylated chitosan Triptolide nanoparticles for overcoming hepatocellular carcinoma: Enhanced therapeutic efficacy, low toxicity, and validated network regulatory mechanisms
Hepatocellular carcinoma (HCC) is the second leading cause of cancer-related deaths worldwide. Current therapies present significant limitations.
Dibutyltin(IV) Complexes Derived from L-DOPA: Synthesis, Molecular Docking, Cytotoxic and Antifungal Activity
A series of organotin(IV) complexes was herein prepared and characterized. A one-pot synthetic strategy afforded reasonable to high yields, depending on the nature of the ligand.
Bringing physiologically-based pharmacokinetic (PBPK) simulation to early drug discovery and development
Lack of efficacy continues to be a problem in drug development. Piecemeal rules of thumb such as Lipinski’s Rule of Five [1] help avoid compounds likely to be poorly...
Critical Evaluation of 2-Ethylhexyl Acrylate Dermal Carcinogenicity Studies Using Contemporary Criteria
Skin tumors have been observed in C3H/HeJ mice following treatment with high and strongly irritating concentrations of 2-ethylhexyl acrylate (2-EHA).
Simulations Plus Receives New Grant Award from the FDA
Simulations Plus today announced today a new funded cooperative agreement with the FDA to work on the GastroPlus dermal absorption/PBPK (TCAT) model.
The PKPlus Module in GastroPlus® Tutorial
This video shows how to create noncompartment, 1-, 2-, and 3-compartment pharmacokinetic models based on in vivo data using the PKPlus™ module in GastroPlus.
Computer-aided drug discovery of Myc-Max inhibitors as potential therapeutics for prostate cancer
While Myc is an essential regulator of growth in normal cells, it is also frequently associated with cancer progression, therapy-resistance and lethal outcomes in most human cancers.
In silico scaling and prioritization of chemical disposition and chemical toxicity of 15,145 organic chemicals
This report describes the development and beta-test of methods that prioritize and scale in silico predictions of chemical disposition {(CD) intestinal absorption, membrane permeability...
In Silico Study of Pyrazolylaminoquinazoline Toxicity by Lazar, Protox, and Admet Predictor
Pyrazolylaminoquinazoline is obtained from synthetic AZD4547 and can inhibit kinase activity in recombinant fibroblast growth factor receptor (FGFR) in vitro.
Structural and functional pharmacokinetic analogs for physiologically based pharmacokinetic (PBPK) model evaluation
Physiologically based pharmacokinetic (PBPK) models enable simulations of absorption, distribution, metabolism, and elimination of chemicals from the body.