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
Bariatric surgery introduces significant changes in the gastrointestinal tract, which may affect oral drug absorption/bioavailability.
Evaluation of Drug–Drug Interactions Between Clarithromycin and Direct Oral Anticoagulants Using Physiologically Based Pharmacokinetic Models
This study assessed the pharmacokinetic (PK) interactions between clarithromycin (a P-glycoprotein [P-gp] inhibitor) and four direct oral anticoagulants (DOACs) (P-gp substrates) using physiologically based PK (PBPK) models to elucidate the influence of P-gp in the interaction between them.
Discovery of Penicillic Acid as a Chemical Probe Against Tau Aggregation in Alzheimer’s Disease
Alzheimer's Disease (AD) is a neurodegenerative disorder proven to be caused by the aggregation of protein tau into fibrils, resulting in neuronal death.
Physiologically-Based Pharmacokinetic Modeling of Trofinetide in Moderate Renal Impairment for Phase 1 Clinical Study Dose Selection with Model Validation
Trofinetide, the first approved treatment for Rett syndrome (RTT), is primarily excreted unchanged in the urine; therefore, it is important to assess the extent to which the exposure is affected in patients with renal impairment.
Hansen parameters and GastroPlus assisted optimized topical elastic liposomes to treat breast cancer using a novel isatin derivative
Breast cancer treatment is a global health challenge using conventional toxic chemotherapeutic agents.
Demonstrating Discriminatory Power of a Dissolution Method Using DDDPlus: Case Study of an ExtendedRelease Formulation and Use in Regulatory Justifications
Dissolution testing is an important attribute that provides insight into in vivo performance, batch-tobatch uniformity and consistent clinical quality.
Identification, Characterization, and in silico ADMET Prediction of Nirmatrelvir and its Degradation Products Using HPLC-PDA and LC-QTOF-MS/MS
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.