A Preclinical Bioavailability Strategy for Decisions on Clinical Drug Formulation Development: an In Depth Analysis

A Preclinical Bioavailability Strategy for Decisions on Clinical Drug Formulation Development: an In Depth Analysis

Publication: Mol Pharm
Software: GastroPlus®

The aim of the presented retrospective analysis was to verify whether a previously proposed Janssen Biopharmaceutical Classification System (BCS)-like decision tree, based on preclinical bioavailability...

Synthesis and Molecular Drug Efficacy of Indoline‐based Dihydroxy‐thiocarbamides: Inflammation Regulatory Property Unveiled over COX‐2 Inhibition, Molecular Docking, and Cytotoxicity Prospects

Synthesis and Molecular Drug Efficacy of Indoline‐based Dihydroxy‐thiocarbamides: Inflammation Regulatory Property Unveiled over COX‐2 Inhibition, Molecular Docking, and Cytotoxicity Prospects

Publication: J Heterocycl Chem

In this study, substituted indoline‐based dihydroxy‐carbamides (5a–i) were synthesized and evaluated as the cyclooxygenase‐2 (COX‐2) inhibitors to testify their inflammatory regulations through COX‐2 inhibition.

β-CD-Catalyzed Multicomponent Domino Reaction: Synthesis, Characterization, in silico Molecular Docking and Biological Evaluation of pyrano[2,3-d]-pyrimidinone Derivatives

β-CD-Catalyzed Multicomponent Domino Reaction: Synthesis, Characterization, in silico Molecular Docking and Biological Evaluation of pyrano[2,3-d]-pyrimidinone Derivatives

Publication: Res Chem Intermed
Software: ADMET Predictor®

Simple and green synthetic procedures constitute an important goal in organic synthesis. The combination of multicomponent reactions (MCRs) and unconventional solvents has become a new research…

State-of-the-Art Review on Physiologically Based Pharmacokinetic Modeling in Pediatric Drug Development

State-of-the-Art Review on Physiologically Based Pharmacokinetic Modeling in Pediatric Drug Development

Publication: Clin Pharmacokinet
Software: GastroPlus®

Physiologically based pharmacokinetic modeling and simulation is an important tool for predicting the pharmacokinetics, pharmacodynamics, and safety of drugs in pediatrics.

Frangulosid as a Novel Hepatitis B Virus DNA Polymerase Inhibitor: A Virtual Screening Study

Frangulosid as a Novel Hepatitis B Virus DNA Polymerase Inhibitor: A Virtual Screening Study

Authors: Nosrati M, Shakeran Z
Publication: In Silico Pharmacol

Hepatitis B virus (HBV) infects more than 400 million humans Worldwide. Currently, development of new anti-HBV agents is focused on inhibiting of HBV DNA polymerase activity. The natural components of…

Discovery PBPK: How to Estimate the Expected Accuracy of ISIVB and IVIVB for New Chemical Entities

Discovery PBPK: How to Estimate the Expected Accuracy of ISIVB and IVIVB for New Chemical Entities

Authors: Bolger MB
Conference: Asia Pacific ISSX
Division: Simulations Plus

PBPK modeling and simulation can be successfully used in the lead optimization phase of drug discovery. Using CLloc, accurate bioavailability can be predicted for new compounds in a chemical series.

Development of Positron Emission Tomography Radiotracers for the GABA Transporter 1

Development of Positron Emission Tomography Radiotracers for the GABA Transporter 1

Publication: ACS Chem Neurosci
Software: ADMET Predictor®

in vivo positron emission tomography (PET) imaging of the γ-aminobutyric acid (GABA) receptor complex has been accomplished using radiolabeled benzodiazepine derivatives, but development of specific…

Predicting mammalian metabolism and toxicity of pesticides in silico

Predicting mammalian metabolism and toxicity of pesticides in silico

Authors: Clark RD
Publication: Pest Manag Sci
Software: ADMET Predictor®
Division: Simulations Plus

Pesticides must be effective to be commercially viable but they must also be reasonably safe for those who manufacture them, apply them, or consume the food they are used to produce.

The OECD Principles for (Q)SAR Models in the Context of Knowledge Discovery in Databases (KDD)

The OECD Principles for (Q)SAR Models in the Context of Knowledge Discovery in Databases (KDD)

Publication: Adv Protein Chem Struct Biol
Software: ADMET Predictor®

The steps followed in the knowledge discovery in databases (KDD) process are well documented and are widely used in different areas where exploration of data is used for decision making. In turn, while…

In vitro/in silico approach in the development of simvastatin-loaded self-microemulsifying drug delivery systems.

In vitro/in silico approach in the development of simvastatin-loaded self-microemulsifying drug delivery systems.

Publication: Drug Dev Ind Pharm
Software: GastroPlus®

The aims of this study were to formulate simvastatin (SV)-loaded self-microemulsifying drug delivery systems (SMEDDS), and explore the potential of these drug delivery systems to improve...