Results 61 to 70 of about 3,220 (195)

From PK/PD to QSP: Understanding the Dynamic Effect of Cholesterol-Lowering Drugs on Atherosclerosis Progression and Stratified Medicine [PDF]

, 2016
Current computational and mathematical tools are demonstrating the high value of using systems modeling approaches (e.g. Quantitative Systems Pharmacology) to understand the effect of a given compound on the biological and physiological mechanisms ...
Diaz-Zuccarini, V, Pichardo-Almarza, C
core  

Simulated rat intestinal fluid improves oral exposure prediction for poorly soluble compounds over a wide dose range [PDF]

, 2016
Solubility can be the absorption limiting factor for drug candidates and is therefore a very important input parameter for oral exposure prediction of compounds with limited solubility.
Bernard Faller, Frank H. Seiler, Jörg Berghausen, Nathalie Gobeau   +3 more
core   +3 more sources

Population pharmacokinetic modelling of amoxicillin in human breast milk—A contribution from the ConcePTION project

British Journal of Clinical Pharmacology, EarlyView.
Aims Amoxicillin, a widely used β‐lactam antibiotic, requires improved pharmacokinetic characterization during breastfeeding. This study used a population pharmacokinetic (PopPK) approach to model amoxicillin concentrations in breast milk, identify variability sources and estimate infant exposure, applying worst‐case scenarios.
Sarah Baklouti, Virginie Rigourd, Alice Panchaud, Hedvig Nordeng, Karel Allegaert, Pieter Annaert, Miao‐Chan Huang, Anaelle Monfort, Monia Guidi, Peggy Gandia   +9 more
wiley   +1 more source

Design, modelling, and pharmacokinetic prediction of novel BRD4-targeting PROTACs

In Silico Research in Biomedicine
Background: Proteolysis Targeting Chimeras (PROTACs) represent an emerging modality for targeted protein degradation, yet their development is often constrained by suboptimal physicochemical and pharmacokinetic properties.
Bharath BR, S. Jahnavi, Nadeem Khan
doaj   +1 more source

Application of Pharmacokinetics Modelling to Predict Human Exposure of a Cationic Liposomal Subunit Antigen Vaccine System

Pharmaceutics, 2017
The pharmacokinetics of a liposomal subunit antigen vaccine system composed of the cationic lipid dimethyldioctadecylammonium bromide (DDA) and the immunostimulatory agent trehalose 6,6-dibehenate (TDB) (8:1 molar ratio) combined with the Ag85B-ESAT-6 ...
Raj K. S. Badhan, Swapnil Khadke, Yvonne Perrie   +2 more
doaj   +1 more source

Simulating Intestinal Transporter and Enzyme Activity in a Physiologically Based Pharmacokinetic Model for Tenofovir Disoproxil Fumarate [PDF]

, 2017
Tenofovir disoproxil fumarate (TDF), a prodrug of tenofovir, has oral bioavailability (25%) limited by intestinal transport (P-glycoprotein), and intestinal degradation (carboxylesterase). However, the influence of luminal pancreatic enzymes is not fully
Domanico, P, Hobson, J, Moss, DM, Owen, A, Rajoli, RKR, Randolph, R, Rannard, S, Seonghee, P, Siccardi, M, Watkinson, M, Wring, S   +10 more
core   +1 more source

Assessing transporter‐mediated rifampin–linezolid interaction using physiologically‐based pharmacokinetic modelling

British Journal of Clinical Pharmacology, EarlyView.
Abstract Aims The study aims to develop a physiologically‐based pharmacokinetic (PBPK) model to quantitatively evaluate the role of ATP‐binding cassette sub‐family B member 1 (ABCB1) and ATP‐binding cassette super‐family G member 2 (ABCG2) in the drug–drug interaction (DDI) between rifampin and linezolid and to predict the impact of high‐dose rifampin ...
Hoang Dat Nguyen, Vinh Hoa Pham, Richard M. Hoglund, Joel Tarning, Junjie Ding   +4 more
wiley   +1 more source

Beyond the label: Rethinking off‐label drug use in paediatrics. Towards a scientifically grounded and safer future for paediatric pharmacotherapy

British Journal of Clinical Pharmacology, EarlyView.
Abstract Despite regulatory progress being made in the past two decades, off‐label drug use in paediatrics remains pervasive, with prevalence estimated between 3% and 97% of prescriptions across different clinical settings. Off‐label use—defined as prescribing outside the conditions described in the Summary of Product Characteristics (SmPC)—is often ...
Tjitske M. van der Zanden, Miriam G. Mooij, Matthijs de Hoog, Saskia N. de Wildt   +3 more
wiley   +1 more source

Clinical assessment of mocravimod as a victim of drug–drug interactions via CYP3A4 metabolism and transporters

Clinical Pharmacology in Drug Development, EarlyView.
Abstract Mocravimod, a novel immunomodulator targeting sphingosine‐1‐phosphate receptor (S1PR), is being developed as a maintenance treatment for patients with acute myeloid leukemia undergoing allogeneic hematopoietic cell transplantation. Preclinical data suggested that cytochrome (CYP) 3A4 is the primary enzyme involved in mocravimod metabolism.
Dymphy R. Huntjens, Stephan Oehen, Elisabeth Kueenburg   +2 more
wiley   +1 more source

Physiologically Based Pharmacokinetic Modelling of UGT Substrate Drugs Lamotrigine and Raltegravir during Pregnancy

Future Pharmacology
Pregnancy is associated with various physiological changes that can significantly impact the disposition of drugs. To further the insight into how pregnancy affects the pharmacokinetics of drugs at different stages, clinical studies can be simulated ...
Monika Berezowska, Paola Coppola, Venkatesh Pilla Reddy, Pradeep Sharma   +3 more
doaj   +1 more source