Nirmatrelvir is a protease inhibitor that is essential for virus replication. Nirmatrelvir is indicated for the management of mild to severe cases of COVID-19 in individuals who are 12 years of age or older.
Machine learning driven bioequivalence risk assessment at an early stage of generic drug development
Bioequivalence risk assessment as an extension of quality risk management lacks examples of quantitative approaches to risk assessment at an early stage of generic drug development.
Discovery and Characterization of BAY-184: A New Potent and Selective Acylsulfonamide-Benzofuran In Vivo-Active KAT6AB InhibitorCli
KAT6A and KAT6B genes are two closely related lysine acetyltransferases that transfer an acetyl group from acetyl coenzyme A (AcCoA) to lysine residues of target histone substrates, hence playing a key role in chromatin regulation.
Developing a Screening Strategy to Identify Hepatotoxicity and Drug Interaction Potential of Botanicals
Botanical supplements, herbal remedies, and plant-derived products are used globally. However, botanical dietary supplements are rarely subjected to robust safety testing unless there are adverse reports in post-market surveillance.
Landscape of regulatory quantitative systems pharmacology submissions to the U.S. Food and Drug Administration: An update report
The number of quantitative systems pharmacology (QSP) submissions to the U.S. Food and Drug Administration has continued to increase over the past decade.
Bioequivalence Requirements for Orally Inhaled and Nasal Drug Products and Use of Novel Physiologically Based Biopharmaceutics Modeling Approaches for Assessing In Vivo Performance
Orally inhaled and nasal drug products (OINDPs) are complex due to the interplay between the device, formulation, and patient characteristics.
Justification of widened dissolution specifications of an extended-release product using physiologically based biopharmaceutics modeling
Drug products meeting the dissolution specifications is crucial in order to ensure consistent clinical performance.
Preclinical Assessment of the PI3Kα Selective Inhibitor Inavolisib and Prediction of Its Pharmacokinetics and Efficacious Dose in Human
Small molecule inhibitors of the PI3K pathway have been extensively investigated as potential anticancer agents. Among the effectors in this pathway
A critical review on approaches to generate and validate virtual population for physiologically based pharmacokinetic models: Methodologies, case studies and way forward
In silico modeling and simulation techniques such as physiologically based pharmacokinetic (PBPK) and physiologically based biopharmaceutics modeling (PBBM) have demonstrated various applications in drug discovery and development.
PBBM Considerations for Base Models, Model Validation, and Application Steps: Workshop Summary Report
The proceedings from the 30th August 2023 (Day 2) of the workshop “Physiologically Based Biopharmaceutics Models (PBBM) Best Practices for Drug Product Quality: Regulatory and Industry Perspectives” are provided herein.
Preparation and Evaluation of Nanolipid Carriers of Bedaquiline- In vitro Evaluation and in silico Prediction
Bedaquiline, a potent antitubercular drug used in the treatment of multidrug-resistant strains, suffers from low oral bioavailability, a slow onset of therapeutic action, and side effects.
Synthesis, Absolute Configuration, Biological Profile and Antiproliferative Activity of New 3,5-Disubstituted Hydantoins
Hydantoins, a class of five-membered heterocyclic compounds, exhibit diverse biological activities.
Advancing the Harmonization of Biopredictive Methodologies through the Product Quality Research Institute (PQRI) Consortium: Biopredictive Dissolution of Dipyridamole Tablets
Biorelevant dissolution and its concept have been widely accepted and further developed to meaningfully predict the bioperformance of oral drug products.
Effect of Data Quality and Data Quantity on the Estimation of Intrinsic Solubility: Analysis Based on a Single-Source Data Set
Aqueous solubility is one of the most important physicochemical properties of drug molecules and a major driving force for oral drug absorption.
Phase I Clinical Trial of NH130 and the Prediction of its Pharmacokinetics Using Physiologically Based Pharmacokinetic Modeling
Parkinson’s disease psychosis (PDP) is a common and distressing complication of Parkinson’s disease (PD), characterized by hallucinations and delusions.
In Silico Dose Adjustment of Zolpidem in Females Using Physiologically Based Pharmacokinetic Modeling and Simulations
Zolpidem (ZPD) is a non-benzodiazepine sedative indicated for the treatment of insomnia.
CFD-PK model for nasal suspension sprays: Validation with human adult in vivo data for triamcinolone acetonide
The objectives of this study were to expand and implement a Computational Fluid Dynamics (CFD)-Dissolution, Absorption and Clearance (DAC)-Pharmacokinetics (PK) multi-physics modeling framework for simulating the transport of suspension-based nasal corticosteroid sprays.
Application of Virtual Drug Study to New Drug Research and Development: Challenges and Opportunity
In recent years, virtual drug study, as an emerging research strategy, has become increasingly important in guiding and promoting new drug research and development.
PBPK Modeling of Lamotrigine and Efavirenz during Pregnancy: Implications for Personalized Dosing and Drug-Drug Interaction Management
This study aimed to model the pharmacokinetics of lamotrigine (LTG) and efavirenz (EFV) in pregnant women using physiologically based pharmacokinetic (PBPK) and pregnancy-specific PBPK (p-PBPK) models.
Understanding the mechanisms of food effect on omaveloxolone pharmacokinetics through physiologically based biopharmaceutics modeling
Omaveloxolone is a nuclear factor (erythroid-derived 2)-like 2 activator approved in the United States and the European Union for the treatment of patients with Friedreich ataxia aged ≥16 years, with a recommended dosage of 150 mg orally once daily on an empty stomach.