Mechanistic Investigation of the Androgen Receptor DNA-Binding Domain Inhibitor Pyrvinium

Mechanistic Investigation of the Androgen Receptor DNA-Binding Domain Inhibitor Pyrvinium

Publication: ACS Omega

Pyrvinium was identified as the first small molecule inhibitor of the androgen receptor (AR) DNA-binding domain (DBD). It was also among the first small molecules shown to...

Model-Informed Drug Discovery and Development: Current Industry Good Practice and Regulatory Expectations and Future Perspectives

Model-Informed Drug Discovery and Development: Current Industry Good Practice and Regulatory Expectations and Future Perspectives

Publication: CPT Pharmacometrics Syst Pharmacol

Good practices around model-informed drug discovery and development (MID3) aim to improve the implementation, standardization, and

DILIsym 8A New Features for Predicting & Understand Drug-Induced Liver Injury

DILIsym 8A New Features for Predicting & Understand Drug-Induced Liver Injury

Authors: Howell BA
Software: DILIsym®

So how can DILIsym help my organization? Predict DILI liabilities beforehand and save $$$, Choose the lead candidate most likely to succeed from a DILI standpoint, Communicate with regulators on safety issues with information they have requested from others numerous times and from a platform they license (FDA) & keep patients safer.

The in vivo predictive dissolution for immediate release dosage of donepezil and danazol, BCS class IIc drugs, with the GIS and the USP II with biphasic dissolution apparatus

The in vivo predictive dissolution for immediate release dosage of donepezil and danazol, BCS class IIc drugs, with the GIS and the USP II with biphasic dissolution apparatus

Publication: J Drug Deliv Sci Technol
Software: GastroPlus®

The formulation developments and the in vivo assessment of Biopharmaceutical Classification System (BCS) class II drugs are challenging due to their low solubility and high permeability in the human gastrointestinal (GI) tract.

Dissolution Testing in Drug Product Development: Workshop Summary Report

Dissolution Testing in Drug Product Development: Workshop Summary Report

Publication: AAPS J

This publication summarizes the proceedings and key outcomes of the first day (“Day 1”) of the 3-day workshop on “Dissolution and Translational Modeling Strategies Enabling Patient-Centric Product Development.”

Physiologically Based Pharmacokinetic/ Pharmacodynamic Model for Caffeine Disposition in Pregnancy

Physiologically Based Pharmacokinetic/ Pharmacodynamic Model for Caffeine Disposition in Pregnancy

Publication: Mol Pharm
Software: GastroPlus®

Caffeine is the most consumed active stimulant. About 80% of pregnant women consume caffeine orally on daily basis. Many reports indicated consumption of >200 mg caffeine during pregnancy could increase the likelihood of miscarriage.

EDEn–Electroceutical Design Environment: Ion Channel Tissue Expression Database with Small Molecule Modulators

EDEn–Electroceutical Design Environment: Ion Channel Tissue Expression Database with Small Molecule Modulators

Publication: iScience
Software: ADMET Predictor®

The emerging field of bioelectricity has revealed numerous new roles for ion channels beyond the nervous system, which can be exploited for applications in regenerative medicine.

PBPK Absorption Modeling: Establishing the In Vitro–In Vivo Link—Industry Perspective

PBPK Absorption Modeling: Establishing the In Vitro–In Vivo Link—Industry Perspective

Publication: AAPS J
Software: GastroPlus®

The establishment of an in vitro–in vivo correlation (IVIVC) is considered the gold standard to establish in vivo relevance of a dissolution method and to utilize dissolution data in the context of regulatory bioequivalence questions...

Molecular Determinants of Cell Permeability Beyond the Rule of 5

Molecular Determinants of Cell Permeability Beyond the Rule of 5

Authors: Matsson P, Lawless M
Software: ADMET Predictor®
Division: PBPK

Molecules that violate conventional guidelines for druglikeness—such as the Rule-of-5—are of increasing interest as chemical probes and drugs for intractable pharmacological targets.