Fremanezumab, a fully humanized IgG2Δa/kappa monoclonal antibody, selectively targets the calcitonin-gene-related peptide (CGRP) and
Administration in fed state but not controlled release in the colon increases oral bioavailability of DF030263, a promising drug candidate for chronic lymphocytic leukemia
For treatment of chronic cancers, the oral administration route is preferred as it provides numerous advantages over other delivery routes.
Pharmacokinetic/pharmacodynamic modeling of drug interactions at the P2Y12 receptor between selatogrel and oral P2Y12 antagonists
Selatogrel is a potent and reversible P2Y12 receptor antagonist developed for subcutaneous self‐administration by patients with suspected acute myocardial infarction.
Scaffold-Hopping Strategy on a Series of Proteasome Inhibitors Led to a Preclinical Candidate for the Treatment of Visceral Leishmaniasis
There is an urgent need for new treatments for visceral leishmaniasis (VL), a parasitic infection which impacts heavily large areas of East Africa, Asia, and South America
Evaluating the impact of physiological properties of the gastrointestinal tract on drug in vivo performance using Physiologically Based Biopharmaceutics Modeling and virtual clinical trials
The physiological properties of the gastrointestinal tract, such as pH, fluid volume, bile salt concentration, and gastrointestinal transit time, are highly variable in vivo.
High-Fat Breakfast Increases Bioavailability of Albendazole Compared to Low-Fat Breakfast: Single-Dose Study in Healthy Subjects
Albendazole is a benzimidazole carbamate drug with anthelmintic and antiprotozoal activity against intestinal and tissue parasites. It has been described that the administration with meals increases albendazole absorption.
A novel in silico method to predict drug PK profile in human and its application to build the PBPK model of Hydroxychloroquine for COVID-19 treatment
The first part of this study is to develop a novel protocol to predict the pharmacokinetic profiles of a target drug based on the Physiologically based pharmacokinetic (PBPK) model of a structurally similar template drug by combining predictions from two software for PBPK modeling, the SimCYP simulator and ADMET Predictor.
Development of an In Vivo Predictive Dissolution Methodology of Topiroxostat Immediate-Release Tablet Using In Silico Simulation
The main objective of this study was to develop an in vivo predictive dissolution (IVPD) model for topiroxostat immediate-release (IR) formulation...
Decomposition Profile Data Analysis for Deep Understanding of Multiple Effects of Natural Products
It is difficult to understand the entire effect of a natural product because such products generally have multiple effects.
Concentration-QTc Analysis of Quizartinib in Patients with Relapsed/Refractory Acute Myeloid Leukemia
This analysis evaluated the relationship between concentrations of quizartinib and its active metabolite AC886 and QT interval corrected using Fridericia's formula (QTcF) in patients with...
Clinical pharmacokinetic study of latrepirdine via in silico sublingual administration
In recent decades, numerous in silico methodologies have been developed focused on the study of pharmacodynamic, pharmacokinetics and toxicological properties of drugs.
Molecular modeling for potential cathepsin L inhibitor identification as new anti-photoaging agents from tropical medicinal plants
Ultraviolet exposure can cause photoaging toward the human skin which is begun by the inflammation on the exposure area, also resulting in activation of a degradative enzyme cathepsin L.
Basic of machine learning and deep learning in imaging for medical physicists
The manuscript aims at providing an overview of the published algorithms/automation tool for artificial intelligence applied to imaging for Healthcare.
PK/PD modeling of a clazosentan thorough QT study with hysteresis in concentration-QT and RR-QT
Clazosentan's potential QT liability was investigated in a thorough QT study in which clazosentan was administered intravenously as a continuous infusion of 20 mg/h immediately followed by 60 mg/h.
Prediction of fraction unbound in plasma in children in data-limited scenarios for human health risk assessment
In human health risk assessment, pediatric physiologically-based pharmacokinetic modeling has been used to predict chemical-specific toxicokinetic adjustment factors.
The emerging plasticity of SARS-CoV-2
Viruses evolve as a result of mutation (misincorporations, insertions or deletions, and recombination) and natural selection for favorable traits such as more efficient viral replication, transmission, and evasion of host defenses.
Characterization of stress degradation products of nintedanib by UPLC, UHPLC-Q-TOF/MS/MS and NMR: Evidence of a degradation product with a structure alert for mutagenicity
Nintedanib is an anti-cancer drug used for the treatment of idiopathic pulmonary fibrosis and non-small cell lung cancer.
Experimental Solubility, Thermodynamic/Computational Validations, and GastroPlus-Based In Silico Prediction for Subcutaneous Delivery of Rifampicin
We focused to explore a suitable solvent for rifampicin (RIF) recommended for subcutaneous (sub-Q) delivery [ethylene glycol (EG), propylene glycol...
Extemporaneous Compounding and Physiological Modeling of Amlodipine/Valsartan Suspension
In case of absent liquid dosage form, crushing a tablet or dispersing a capsule would be the most convenient option for using these drugs in patients with dysphagia difficulties.
Next generation risk assessment of human exposure to anti-androgens using newly defined comparator compound values
Next Generation Risk Assessment (NGRA) can use the so-called Dietary Comparator Ratio (DCR) to evaluate the safety of a defined exposure...