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.
A Baseline Analysis of Regulatory Review Timelines for ANVISA: 2013-2016
Background: The Brazilian health regulatory agency (Agência Nacional de Vigilância Sanitária, ANVISA) has embarked on transformational initiatives to fulfill its mandate to...
Biological Activity of Halogen-Containing Derivatives of N-Substituted Quinone Imines
The different halogen-containing derivatives of N-substituted quinone imines have been synthesized by the halogenation and...
The GastroPlus® Additional Dosage Routes Seminar Series Ocular with Maxime Le Merdy
The Ocular Compartmental Absorption & Transit (OCAT™) model represents the eye as a collection of the following compartments...
Vesicular elastic liposomes for transdermal delivery of rifampicin: In-vitro, in-vivo and in silico GastroPlus™ prediction studies
This study investigated enhanced bioavailability and sustained delivery of transdermally delivered rifampicin (RIF) in elastic liposomes...
Cerebrospinal fluid penetration of targeted therapeutics in pediatric brain tumor patients
Treatment with small-molecule inhibitors, guided by precision medicine has improved patient outcomes in multiple cancer types.
The GastroPlus® Additional Dosage Routes Seminar Series IM with Viera Lukacova
The intramuscular (IM) drug delivery model represents the site of injection as a single compartment. Within this compartment...