In vivo Performance of Amorphous Solid Dispersions Based on Water-Insoluble Versus Water-Soluble Carriers: Fenofibrate Case Study

In vivo Performance of Amorphous Solid Dispersions Based on Water-Insoluble Versus Water-Soluble Carriers: Fenofibrate Case Study

Publication: Int J Pharm
Software: GastroPlus®
Division: PBPK

The objective of this study is to address the unanswered question whether sustained supersaturation generated from amorphous solid dispersions (ASDs) formulated in insoluble hydrogel carriers will result in better bioavailability over that of spring-and-parachute type of dissolution profiles of ASDs formulated in water-soluble carriers

Dosage Optimization Using Physiologically Based Pharmacokinetic Modeling for Pediatric Patients with Renal Impairment: A Case Study of Meropenem

Dosage Optimization Using Physiologically Based Pharmacokinetic Modeling for Pediatric Patients with Renal Impairment: A Case Study of Meropenem

Publication: AAPS PharmSciTech
Software: GastroPlus®
Division: PBPK

The pharmacokinetics of renally eliminated antibiotics can be influenced by changes associated with renal function and development in a growing subject. Little is known about the effects of renal insufficiency on the pharmacokinetics of meropenem in pediatric subjects.

Association Between Abatacept Exposure Levels and Infection Occurrence in Patients with Rheumatoid Arthritis: Post Hoc Analysis of the AVERT-2 Study

Association Between Abatacept Exposure Levels and Infection Occurrence in Patients with Rheumatoid Arthritis: Post Hoc Analysis of the AVERT-2 Study

Publication: The Journal of Rheumatology
Therapeutic Areas: Rheumatology

 To determine if higher serum exposure during subcutaneous (SC) abatacept treatment was associated with an increased infection risk in adult patients with early rheumatoid arthritis (RA).

Improving Individualized Salbutamol Treatment: A Population Pharmacokinetic Model for Oral Salbutamol in Virtual Patients

Improving Individualized Salbutamol Treatment: A Population Pharmacokinetic Model for Oral Salbutamol in Virtual Patients

Authors: Marques L, Vale N
Publication: Pharmaceutics
Software: GastroPlus®
Division: PBPK

Salbutamol, a short-acting β2-agonist used in asthma treatment, is available in multiple formulations, including inhalers, nebulizers, oral tablets, and intravenous, intramuscular, and subcutaneous routes.

Characterization of Preclinical Radio ADME Properties of ARV-471 for Predicting Human PK Using PBPK Modeling

Characterization of Preclinical Radio ADME Properties of ARV-471 for Predicting Human PK Using PBPK Modeling

Publication: J Pharm Analysis
Software: GastroPlus®
Division: PBPK

Proteolysis-targeting chimeras (PROTACs) represent a promising class of drugs that can target disease-causing proteins more effectively than traditional small molecule inhibitors can, potentially revolutionizing drug discovery and treatment strategies.

Advancing Systemic Toxicity Risk Assessment: Evaluation of a NAM-based Toolbox Approach

Advancing Systemic Toxicity Risk Assessment: Evaluation of a NAM-based Toolbox Approach

Publication: Toxicol Sci
Software: GastroPlus®
Division: PBPK

For many years, a method that allowed systemic toxicity safety assessments to be conducted without generating new animal test data, seemed out of reach.

Establishment of Biopredictive Dissolution and Bioequivalence Safe Space Using the Physiologically Based Biopharmaceutics Modeling for Tacrolimus Extended-Release Capsules

Establishment of Biopredictive Dissolution and Bioequivalence Safe Space Using the Physiologically Based Biopharmaceutics Modeling for Tacrolimus Extended-Release Capsules

Publication: AAPS PharmSciTech
Software: GastroPlus®
Division: PBPK

A slight variation in in vivo exposure for tacrolimus extended-release (ER) capsules, which have a narrow therapeutic index (NTI), significantly affects the pharmacodynamics of the drug. Generic drug bioequivalence (BE) standards are stricter, necessitating accurate assessment of the rate and extent of drug release.

Advancements in Ocular Modelling and Simulations: Key Considerations and Case Studies

Advancements in Ocular Modelling and Simulations: Key Considerations and Case Studies

Authors: Khan MS, Murthy A, Ahmed T
Publication: AAPS PharmSciTech
Software: GastroPlus®
Division: PBPK

This review paper discusses the key aspects of ocular biopharmaceutics, with emphasis on the crucial role played by ocular compartmental modelling and simulation in deciphering physiological conditions related to various eye diseases.

Predicting Pharmacokinetics of Active Constituents in Spatholobi caulis by Using Physiologically Based Pharmacokinetic Models

Predicting Pharmacokinetics of Active Constituents in Spatholobi caulis by Using Physiologically Based Pharmacokinetic Models

Publication: Pharmaceuticals
Software: GastroPlus®
Division: PBPK

Spatholobi Caulis (SPC) is a medicinal plant that mainly grows in China and Southeast Asian countries and commonly used in clinics; the pharmacokinetic characteristics in humans need to be determined.

Hydrogel for Sustained Delivery of Therapeutic Agents

Hydrogel for Sustained Delivery of Therapeutic Agents

Publication: Gels
Software: GastroPlus®
Division: PBPK

In recent years, hydrogels have emerged as a highly promising platform for the sustained delivery of therapeutic agents, addressing critical challenges in drug delivery systems, from controlled release to biocompatibility.

Synthesis and Structure–Activity Relationship of Thiourea Derivatives Against Leishmania Amazonensis

Synthesis and Structure–Activity Relationship of Thiourea Derivatives Against Leishmania Amazonensis

Publication: Pharmaceuticals
Software: ADMET Predictor®
Division: Cheminformatics

 Leishmaniasis, caused by Leishmania protozoa and transmitted by vectors, presents varied clinical manifestations based on parasite species and host immunity. The lack of effective vaccines or treatments has prompted research into new therapies, including thiourea derivatives, which have demonstrated antiprotozoal activities.

Advancing understanding of human variability through toxicokinetic modeling, in vitro-in vivo extrapolation, and new approach methodologies

Advancing understanding of human variability through toxicokinetic modeling, in vitro-in vivo extrapolation, and new approach methodologies

Publication: Hum Genomics
Software: ADMET Predictor®
Division: Cheminformatics

The merging of physiology and toxicokinetics, or pharmacokinetics, with computational modeling to characterize dosimetry has led to major advances for both the chemical and pharmaceutical research arenas.

A review of quantitative structure-activity relationship: The development and current status of data sets, molecular descriptors and mathematical models

A review of quantitative structure-activity relationship: The development and current status of data sets, molecular descriptors and mathematical models

Authors: Li J, Zhao T, Yang Q, Du S, Xu L
Publication: Chemometr Intell Lab Syst
Software: ADMET Predictor®
Division: Cheminformatics

Developing Quantitative Structure-Activity Relationship (QSAR) models applicable to general molecules is of great significance for molecular design in many disciplines.

Investigation of the Anti-asthmatic Activity of Solidagenone, In Vitro Toxicity Versus In Silico Studies

Investigation of the Anti-asthmatic Activity of Solidagenone, In Vitro Toxicity Versus In Silico Studies

Publication: Revista Brasileira de Farmacognosia
Software: ADMET Predictor®
Division: Cheminformatics

Solidagenone, a labdane diterpene isolated from inflorescences of Solidago chilensis Meyen, Asteraceae, was investigated for its anti-inflammatory and anti-asthmatic action.

Erectile Dysfunction Therapy of Bariatric Patients: Tadalafil Biopharmaceutics and Pharmacokinetics Before vs. After Gastric Sleeve/Bypass

Erectile Dysfunction Therapy of Bariatric Patients: Tadalafil Biopharmaceutics and Pharmacokinetics Before vs. After Gastric Sleeve/Bypass

Publication: AAPS J
Software: GastroPlus®
Division: PBPK

Bariatric surgery introduces significant changes in the gastrointestinal tract, which may affect oral drug absorption/bioavailability.