Metabolic Profiling and Detoxification of Eupalinolide A and B in Human Liver Microsomal Systems

Metabolic Profiling and Detoxification of Eupalinolide A and B in Human Liver Microsomal Systems

Publication: Toxics
Software: ADMET Predictor®

Eupalinolide A (EA, Z-configuration) and Eupalinolide B (EB, E-configuration) are cis-trans isomeric sesquiterpenoid monomers isolated from Eupatorium lindleyanum DC. (Asteraceae).

Automated Concentration-QT data preparation, model selection and reporting in R

Automated Concentration-QT data preparation, model selection and reporting in R

Conference: International Society of Pharmacometrics
Software: Monolix®

Since the publication of the ICH E14 guidance in 2015, QT interval prolongation as-sessment can be carried out with a concentration-QTc modeling approach as part of single- or mul-tiple- dose escalation studies, instead of conducting a thorough QT/QTc study.

Pharmacokinetic Studies and Synergistic Antitumor Effects of Cannabichromene and Cannabidiol in Drug-Resistant Breast Cancers

Pharmacokinetic Studies and Synergistic Antitumor Effects of Cannabichromene and Cannabidiol in Drug-Resistant Breast Cancers

Publication: Drug Delivery and Translational Research
Software: GastroPlus®

Triple-negative breast cancer (TNBC) is highly aggressive with limited treatment options, and resistance to doxorubicin (DOX) further compromises outcomes.

Design, Synthesis, and Pharmacological Evaluation of Metabolically Stable Apelin Receptor Antagonists with Improved In Vivo Exposure and Efficacy in Ovarian Cancer

Design, Synthesis, and Pharmacological Evaluation of Metabolically Stable Apelin Receptor Antagonists with Improved In Vivo Exposure and Efficacy in Ovarian Cancer

Publication: J Med Chem
Software: ADMET Predictor®

The apelin receptor (APJ) has emerged as a potential novel therapeutic target in cancer due to its role in regulating cell proliferation, angiogenesis, and metastasis.

Novel Descriptors and Models for More Accurate ADME Predictions of Beyond Rule of Five Molecules

Novel Descriptors and Models for More Accurate ADME Predictions of Beyond Rule of Five Molecules

Publication: ChemRxiv

This study addresses the critical need for improved physicochemical descriptors and predictive models tailored to beyond Rule of Five (bRo5) compounds, including PROTACs and cyclic peptides. B

Development of a Pregnancy-Specific Physiologically Based Pharmacokinetics (PBPK) Model for Aspirin

Development of a Pregnancy-Specific Physiologically Based Pharmacokinetics (PBPK) Model for Aspirin

Publication: CPT Pharmacometrics Syst Pharmacol
Software: GastroPlus®

Aspirin is one of the most commonly used medications in pregnancy, particularly for the prevention of hypertensive disorders.

Quantitative Systems Toxicology Modeling with DILIsym to Support Phase 3 Dose Selection for Fezolinetant

Quantitative Systems Toxicology Modeling with DILIsym to Support Phase 3 Dose Selection for Fezolinetant

Publication: Clin Pharmacol Ther
Software: DILIsym®

Fezolinetant is a first-in-class, selective, non-hormonal, neurokinin 3 receptor antagonist that is approved for the treatment of moderate to severe vasomotor symptoms due to menopause.

Unveiling Anticancer Potential of Imidazo-Pyridine/Pyrazine-Fused bicyclic Heterocycles: Insights From in silico and in vitro Studies

Unveiling Anticancer Potential of Imidazo-Pyridine/Pyrazine-Fused bicyclic Heterocycles: Insights From in silico and in vitro Studies

Publication: In Silico Research in Biomedicine

Cancer is a significant global health challenge and the second leading cause of death worldwide, responsible for millions of fatalities annually.

Physiologically Based Pharmacokinetic Model for Clinical Translation and Prediction of Drug Interaction of the Major Kratom Alkaloid, Mitragynine

Physiologically Based Pharmacokinetic Model for Clinical Translation and Prediction of Drug Interaction of the Major Kratom Alkaloid, Mitragynine

Publication: ACS Pharmacology & Translational Science
Software: GastroPlus®

The opioid crisis presents a significant public health issue and underscores the urgency of developing effective treatments for opioid use disorder (OUD).

Oral Pro‑Transferosome Tablets of Carica papaya Leaf Extract: Box–Behnken Optimization and In Silico Mechanistic Insights for Dengue‑Associated Thrombocytopenia

Oral Pro‑Transferosome Tablets of Carica papaya Leaf Extract: Box–Behnken Optimization and In Silico Mechanistic Insights for Dengue‑Associated Thrombocytopenia

Publication: J Pharma Innovation
Software: GastroPlus®

Carica papaya L. leaf extract has long been recognized for its therapeutic potential in dengue-associated thrombocytopenia through enhancement of platelet production and inhibition of dengue viral proteases.

Comprehensive PBPK Evaluation of Phenytoin and Indomethacin: Dose, Age, Pregnancy and Drug–Drug Interaction Insights

Comprehensive PBPK Evaluation of Phenytoin and Indomethacin: Dose, Age, Pregnancy and Drug–Drug Interaction Insights

Publication: International Journal of Translational Medicine
Software: GastroPlus®

Understanding the pharmacokinetics (PK) of antiepileptic and anti-inflammatory drugs under different physiological conditions is essential for optimizing therapy.

Model-Based Meta-Analysis With MonolixSuite: A Tutorial for Longitudinal Categorical and Continuous Data

Model-Based Meta-Analysis With MonolixSuite: A Tutorial for Longitudinal Categorical and Continuous Data

Publication: CPT Pharmacometrics Syst Pharmacol
Software: Monolix®

Model-based meta-analysis (MBMA) informs key drug development decisions by integrating data, published or unpublished, from multiple studies.