Pulmonary diseases, such as asthma and chronic obstructive pulmonary disease (COPD) are complex human airway diseases that affect millions of people worldwide.
From Lab-to-Clinic with Model Informed Formulation Development: a Case Study of Hydroxyzine SR Tablets
Model Informed Formulation Development (MIFD) uses physiologically based pharmacokinetic (PBPK) modelling and other in silico tools to facilitate new product development.
Quantitative Systems Toxicology Modeling of Acetaminophen Pharmacokinetics and Hepatic Biomarkers After Overdoses of Extended-Release and Immediate-Release Formulations in Adults With Chronic Alcohol Use or Low Glutathione
Acetaminophen (APAP), an over-the-counter analgesic and antipyretic, can cause hepatotoxicity when ingested in large overdoses.
Beyond the Linear Model in Concentration-QT Analysis
This work introduces several extensions for concentration-QT modeling in a pharmacometric context.
A Well-Characterized Mechanistic Model for Exploring Known or Hypothesized T cell Mediated Drug Induced Liver Injury: Current Capabilities and Challenges for Future Predictivity
Drug-induced liver injury (DILI) is an adverse event whose emergence can slow or halt drug development programs.
Model Integrated Evidence Approach for Rational and Safe Formulation Development: case of alfuzosin prolonged-release tablets
The model integrated evidence (MIE) approach aims to utilize simulation tools like physiologically based biopharmaceutic model (PBBM) or physiologically based pharmacokinetic (PBPK) model for the development of new drugs and generic formulations.
Role of Physiologically Based Biopharmaceutics Modeling in Predicting and Circumventing the Drug-Drug Interactions of Tyrosine Kinase Inhibitors with Acid-Reducing Agents
Tyrosine kinase inhibitors (TKIs) are molecular targeting agents used to treat various types of cancer. During the treatment with TKIs, acid-reducing agents (ARAs) are prescribed to prevent gastric mucosal damage.
Evaluation of Violacein Metabolic Stability and Metabolite Identification in Human, Mouse, and Rat Liver Microsomes
Malaria significantly impacts the health of populations living in poverty and vulnerable conditions. Resistance to current antimalarial drugs remains a major challenge and highlights the urgent need for novel, effective, and safer therapies.
An Ocular Exposure Prediction for Topical Atropine in Human Using Physiologically Based Pharmacokinetic Modeling
Developing a mathematical model to predict the distribution and bioavailability of atropine in human eyes is an insight approach for clinical practice.
Establishing Clinically Relevant Specifications for Carbamazepine Tablets Using Physiologically Based Pharmacokinetic Modeling
The purpose of this study was to establish a clinically relevant specification for carbamazepine (CBZ) tablets, a classic narrow therapeutic index drug (NTID), within the Chinese population.
Structural Modification of Aceclofenac to Design Enhanced COX-2 Inhibitors: A Medicinal and Toxicological Study
Aceclofenac (ACF) is a nonsteroidal anti-inflammatory drug (NSAID), prescribed for treating pain and inflammation.
Microfluidic Device Successfully Replaces Traditional Models of Pregnancy Associated Drug Pharmacokinetic Studies
Pregnant and lactating people remain therapeutic orphans as they are often excluded from clinical trials, remaining one of the most therapeutically vulnerable.
Predicting and Confirming Bioequivalence of Alpelisib Oral Granules and Tablets for Patients With PIK3CA-Related Disorders
Alpelisib, an oral α-specific phosphoinositide 3-kinase (PI3K) inhibitor, has been shown to be safe and effective for some patients with gain-of-function mutation in the PIK3CA oncogene
ADME profile of AP-238 – opioid designer drug (CAS: 140924-11-4): first application of multi-in silico approach methodology for comprehensive prediction of ADME profile (absorption, distribution, metabolism and excretion) important for clinical toxicology and forensic purposes
AP-238 is a recently emerged opioid designer drug from the cinnamylpiperazine class, raising increasing concern in forensic and clinical toxicology due to its potential for abuse and limited ADME (absorption, distribution, metabolism, and excretion) profile.
Extrapolation of Midazolam Disposition in Neonates Using Physiological-Based Pharmacokinetic/Pharmacodynamic Modeling
There is a shortage of data in clinical studies of neonatal populations, which often utilize extrapolation strategies and model simulation techniques to support drug development and clinical applications.
Utilizing Physiologically Based Pharmacokinetic Models to Support Rational Medication in Chinese Elderly Population
China is undergoing a pronounced shift towards an aging society, wherein the elderly constitute a prominent demographic relying significantly on medications.
Design and Development of Sulfenylated 5-Aminopyrazoles as Inhibitors of Acetylcholinesterase and Butyrylcholinesterase: Exploring the Implication for Aβ1–42 Aggregation Inhibition in Alzheimer’s Disease
Current therapeutic regimens approved to treat Alzheimer's disease (AD) provide symptomatic relief by replenishing the acetylcholine levels in the brain by inhibiting AChE.
Formulation Strategy of BCS-II Drugs by Coupling Mechanistic In-Vitro and Nonclinical In-Vivo Data with PBPK: Fundamentals of Absorption-Dissolution to Parameterization of Modelling and Simulation
BCS class II candidates pose challenges in drug development due to their low solubility and permeability.
Rat-to-Human PBPK Model of U-47700: Unveiling Pharmacokinetic Risks of a Synthetic Opioid Through Interspecies Extrapolation
U-47700, a synthetic μ-opioid receptor agonist and emerging new psychoactive substance, poses critical public health risks due to its high abuse liability and fatal overdose potential.
From In Vivo Predictive Dissolution to Virtual Bioequivalence: A GastroPlus®-Driven Framework for Generic Candesartan Cilexetil Tablets
Candesartan cilexetil, a Biopharmaceutics Classification System (BCS) II prodrug, demonstrates compromised bioavailability attributable to its limited aqueous solubility coupled with P-glycoprotein (P-gp)-mediated efflux and hepatic first-pass metabolism, thereby introducing complexities in generic drug bioequivalence assessments.