Background: The replacement of traditional in vivo bioequivalence studies by in vitro dissolution assays, based on the biopharmaceutical classification system (BCS), has...
Pediatric dose selection for fremanezumab (AJOVY) phase 3 migraine study using pharmacokinetic data from a pediatric phase 1 study and a population pharmacokinetic modeling and simulation approach
Previous examination of the relationship between fremanezumab exposures and baseline body weight supports a weight cutoff of 45 kg of pediatric dose selection, with the approved adult dose of 225 mg monthly being appropriate or patients weighing >= 45 kg
Biopharmaceutical characterization of rebamipide: The role of mucus binding in regional-dependent intestinal permeability
In this study, we aimed to elucidate biopharmaceutical characteristics of the anti-ulcer drug rebamipide, with special emphasis on the...
Computational Methods Used in Phytocompound-Based Drug Discovery
Phytocompounds are gaining popularity, due to lesser toxicity, greater bioavailability and high chemodiversity.
In silico models for genotoxicity and drug regulation
Whereas in the past, (Q)SAR methods have been largely used to support the design of new drugs, in the last few decades...
Application of synthetic membranes in establishing bio-predictive IVPT for testosterone transdermal gel
The current study investigated the use of synthetic membranes in developing a bio-predictive in vitro permeation testing (IVPT) method for 1.62% testosterone gel.
Evaluation of the effect of synthetic compounds derived from azidothymidine on MDA-MB-231 type breast cancer cells
The present study aimed to investigate the effect of AZT derivates containing tellurium (Te) on human breast cancer cell lines and the mechanisms...
Mechanistic Investigations Support Liver Safety of Ubrogepant
Small-molecule calcitonin gene–related peptide (CGRP) receptor antagonists have demonstrated therapeutic potential for the treatment of migraine.
In Vitro-In Silico Evaluation of Apremilast Solid Dispersions Prepared via Corotating Twin Screw Extruder
The purpose of this study was to employ the Hot melt extrusion technique (HME) to prepare amorphous solid dispersions (ASDs) of Apremilast, a BCS class IV drug.
The GastroPlus® Additional Dosage Routes Seminar Series Discussion Panel
Ask Us Anything panel discussion
Developing HME-Based Drug Products Using Emerging Science: a Fast-Track Roadmap from Concept to Clinical Batch
This paper presents a rational workflow for developing enabling formulations, such as amorphous solid dispersions, via hot-melt...
DILIsym: Quantitative systems toxicology impacting drug development
DILIsym®, a quantitative systems toxicology model developed over the last decade by the drug-induced liver injury (DILI)-sim Initiative, has provided novel...
Application of the Gastrointestinal Simulator (GIS) Coupled with In Silico Modeling to Measure the Impact of Coca-Cola® on the Luminal and Systemic Behavior of Loratadine (BCS Class 2b)
In the present work, we explored if Coca-Cola® had a beneficial impact on the systemic outcome of the weakly basic drug loratadine...
The AHR1-ARNT1 dimerization pair is a major regulator of the response to natural ligands, but not to TCDD, in the chicken
The activation of the aryl hydrocarbon receptor (AHR) occurs through the binding of dioxin-like compounds (DLCs) or natural ligands.
The application of machine learning techniques to innovative antibacterial discovery and development
After the initial wave of antibiotic discovery, few novel classes of antibiotics have emerged, with the latest dating back to the 1980’s.
Development and evaluation of a high throughput inhalation model for organic chemicals
Currently it is difficult to prospectively estimate human toxicokinetics (particularly for novel chemicals) in a high-throughput manner.
Computational Approaches in Drug Designing and Their Applications
Computational approaches have tremendous potential to speed up the process of drug discovery.
Predicted effect of ticagrelor on the pharmacokinetics of dabigatran etexilate using physiologically based pharmacokinetic modeling
Dabigatran etexilate (DABE) is a direct oral anticoagulant (DOAC) and may be combined with ticagrelor, a P2Y12 inhibitor...
In Vitro and In Vivo Efficacy of AZD3965 and Alpha-Cyano-4-Hydroxycinnamic Acid in the Murine 4T1 Breast Tumor Model
Monocarboxylate transporter 1 (MCT1) represents a potential therapeutic target in cancer.
Quantitative structure–activity relationships of xanthen-3-one and xanthen-1,8-dione derivatives and design of new compounds with enhanced antiproliferative activity on HeLa cervical cancer cells
Xanthene derivatives have become a group of molecules of great importance in discovering of new anticancer drugs.