Currently, there are >11,000 synthetic turf athletic fields in the United States and >13,000 in Europe. Concerns have been raised about exposure to carcinogenic chemicals resulting from...
Population pharmacokinetics and exposure – safety analyses of nivolumab in patients with relapsed or refractory classical hodgkin lymphoma
Nivolumab, a fully human immunoglobulin G4 monoclonal anti-programmed death-1 antibody, has demonstrated clinical benefits in multiple tumors, including classical Hodgkin lymphoma.
Machine Learning: What, Why, and How?
Since the beginning of computers era, an enormous amount of data generated seems to be ever-increasing and could be of great use with efficient learning techniques.
Tannic Acid Solution: A Better Fixative Solution Than Formalin for Elastin and Collagen—Toxic and Morphological Assessment.
Formaldehyde is commonly used worldwide, even though it is classified as carcinogenic to humans by the International Agency for Research on Cancer.
Design, synthesis, structural characterization and in vitro evaluation of new 1,4-disubstituted-1,2,3-triazole derivatives against glioblastoma cells
A new series of 1,4-disubstituted-1,2,3-triazole derivatives were synthesized through the copper-catalyzed azide-alkyne 1,3-dipolar cycloaddition (Click chemistry) and their inhibitory activities were...
The Irrelevance of in vitro Dissolution in Setting Product Specifications for Drugs like Dextromethorphan that are Subject to Lysosomal Trapping
The purpose of the current study was to develop a physiologically-based pharmacokinetic (PBPK) model for dextromethorphan (DEX) and its metabolites in extensive (EM) and poor metabolizers (PM).
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.
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.
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).
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...
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.
Virtual screening using covalent docking to find activators for G245S mutant p53
TP53 is the most mutated gene in all cancers. The mutant protein also accumulates in cells. The high frequency of p53 mutations makes the protein a promising target for anti-cancer therapy.
In Vivo Predictive Dissolution and Simulation Workshop Report: Facilitating the Development of Oral Drug Formulation and the Prediction of Oral Bioperformance
A 2-day workshop entitled “In Vivo Predictive Dissolution and Simulation” was held September 11–12, 2017 in Washington, DC, focused on the selection of applications, methodologies, and...