Costs, scientific and ethical concerns related to animal tests for regulatory decision-makinghave stimulated the development of alternative methods.
Challenges with Multi-Objective QSAR in Drug Discovery
The complexity in the drug discovery pipeline, in combination with the exponential growth of experimental and computational data, the technological achievements, and the access to large data sets, has led…
Photolytic and Photocatalytic Transformation of an Antipsychotic Drug Asenapine: Comparison of Kinetics, Identification of Transformation Products, and in silico Estimation of Their Properties
The photolytic and photocatalytic transformation of an antipsychotic drug asenapine with the use of H2O2 and TiO2 was studied. A method employing irradiation with a simulated full solar spectrum in the…
Concentration Profiles of Carvedilol: A Comparison Between In Vitro Transfer Model and Dissolution Testing
The study aims to investigate the transfer behavior of the weakly basic BCS class II model drug carvedilol from the stomach to the small intestine and compare the concentration profiles of carvedilol that...
Design, Synthesis, and Evaluation of Novel L-phenylglycine Derivatives as Potential PPARγ Lead Compounds
In accordance with the structural characteristics of thiazolidinedione drugs and highly bioactive tyrosine derivatives, we tentatively designed the l-phenylglycine derivatives TM1and TM2 based on basic…
Utility of physiologically based pharmacokinetic (PBPK) modeling in oncology drug development and its accuracy: a systematic review
Physiologically based pharmacokinetic (PBPK) modeling, a mathematical modeling approach which uses a pharmacokinetic model to mimick human physiology to predict drug...
Inquiry of Literature Evidence for Induced Fit of Cytochrome P450 2C9 for Warfarin, Phenprocoumon, Flurbiprofen and Clopidogrel: A Critical Review
Cytochrome P450 oxygenases (CYP for short) are liver microsomal enzymes with a prosthetic hem(e) group that catalyze various types of hepatic biotransformation reactions including aromatic and...
Biopharmaceutical considerations in paediatrics with a view to the evaluation of orally administered drug products – a PEARRL review
In this review, the current biopharmaceutical approaches for evaluation of oral formulation performance in paediatrics are discussed.
Population Pharmacokinetics and Exposure-Response Analyses of Eslicarbazepine Acetate Efficacy and Safety in Monotherapy of Partial-Onset Seizures.
Eslicarbazepine acetate (ESL) is a once-daily oral antiepileptic drug (AED) indicated for partial-onset seizures (POS). ESL pharmacokinetics (PK) and exposure-response analyses were supported by...
The role of peroxisome proliferator-activated receptor gamma in prostate cancer
Despite great progress in the detection and treatment of prostate cancer, this disease remains an incredible health and economic burden. Although androgen receptor (AR)...
Ethanolic Extract of Pomegranate (Punica Granatum L) Peel: Acute Toxicity Tests on Zebrafish (Danio rerio) Embryos and its Toxicity Prediction by in silico
Antibiotic resistance causes many serious health problems that have emerged both in developed and developing countries. One of many examples of the antibiotic problem is resistance to Mycobacterium…
Food for thought: formulating away the food effect – a PEARRL review
Co‐ingestion of oral dosage forms with meals can cause substantial changes in bioavailability relative to the fasted state. Food‐mediated effects on bioavailability can have significant consequences...
In vitro methods to assess drug precipitation in the fasted small intestine – a PEARRL review
Drug precipitation in vivo poses a significant challenge for the pharmaceutical industry.
Pharmacokinetic/Pharmacodynamic Model of CW002, an Investigational Intermediate Neuromuscular Blocking Agent, in Healthy Volunteers
CW002 is an investigational non-depolarizing, neuromuscular blocking agent with a rapid onset and intermediate duration of
Computational Toxicology Methods in Chemical Library Design and High-Throughput Screening Hit Validation
The discovery of molecular toxicity in a clinical drug candidate can have a significant impact on both the cost and timeline of the drug discovery process.
Development of a Clinically Relevant Dissolution Method for Metaxalone Immediate Release Formulations Based on an IVIVC Model
The aim of the present work was to classify metaxalone according to the Biopharmaceutics Classification System (BCS), to develop a clinically relevant dissolution method that can be used to predict...
Brief overview of solubility methods: Recent trends in equilibrium solubility measurement and predictive models
Solubility is a crucial physicochemical parameter affecting the whole process of drug discovery and development.
Pathway-based predictive approaches for non-animal assessment of acute inhalation toxicity
New approaches are needed to assess the effects of inhaled substances on human health.
Antibacterial and antibiofilm activities of Prangos acaulis Bornm. extract against Streptococcus mutans: an in silico and in vitro study
Streptococcus mutans is a principal pathogenic agent in biofilm formation on the teeth surfaces and subsequently development of dental caries and plaque.
Advanced Chemometric Modeling Approaches for the Design of Multitarget Drugs Against Neurodegenerative Diseases
Neurodegenerative diseases (ND), a major worldwide health problem, present a multifactorial nature.