Background The signaling protein p38 mitogen-activated protein kinase (MAPK) regulates the tumor cell microenvironment, modulating cell survival, migration, and invasion.
Modeling of prolactin response following dopamine D2 receptor antagonists in rats: can it be translated to clinical dosing?
Prolactin release is a side effect of antipsychotic therapy with dopamine antagonists, observed in rats as well as humans.
A cross-species translational pharmacokinetic-pharmacodynamic evaluation of core bodytemperature reduction by the TRPM8 blocker PF-05105679.
PF-05105679 is a moderately potent TRPM8 blocker which has been evaluated for the treatment of cold pain sensitivity.
Ribociclib Bioavailability Is Not Affected by Gastric pH Changes or Food Intake: In Silico and Clinical Evaluations.
Ribociclib (KISQALI®), a cyclin-dependent kinase 4/6 inhibitor approved for the first-line treatment of HR+/HER2– advanced breast cancer with an aromatase inhibitor, is administered with...
Intrinsic dissolution simulation of highly and poorly soluble drugs for BCS solubility classification
Intrinsic dissolution testing allows characterizing drug substances through its dissolution rate when exposed to a specified surface area in a specific dissolution media.
Combining “Bottom-up” and “Top-down” Approaches to Assess the Impact of Food and Gastric pH on Pictilisib (GDC-0941) Pharmacokinetics
Pictilisib, a weakly basic compound, is an orally administered, potent, and selective pan-inhibitor of phosphatidylinositol 3-kinases for oncology indications.
Investigating Oral Absorption of Carbamazepine in Pediatric Populations
Prediction of the pharmacokinetics of orally administered drugs in children is of importance to optimize the efficacy and safety of pediatricmedicines.
Predictive Biopharmaceutics and Pharmacokinetics: Modeling and Simulation
Scientists have made great discoveries concerning human physiology and gained tremendous knowledge during drug development efforts.
Investigating the state of physiologically based kinetic modelling practices and challenges associated with gaining regulatory acceptance of model applications.
Physiologically based kinetic (PBK) models are used widely throughout a number of working sectors, including academia and industry, to provide insight into the dosimetry related to observed adverse...
Effect of the pulmonary deposition and in vitro permeability on the prediction of plasma levels of inhaled budesonide formulation
The growing interest in the inhalable pharmaceutical products requires advanced approaches to safe and fast product development, such as in silico tools that can be used...
Abstract B083: Population pharmacokinetics and pharmacodynamics for an oral Notch inhibitor, LY3039478, in patients with advanced cancer and healthy volunteers
Background: LY3039478 is an oral Notch inhibitor that prevents release of the Notch Intracellular Domain (NICD) by inhibiting proteolytic activity of the gamma (γ)-secretase complex.
Identification of impurities in macrolides by liquid chromatography–mass spectrometric detection and prediction of retention times of impurities by constructing quantitative structure–retention relationship (QSRR)
Macrolides are multicomponent drugs whose impurity control is always a challenge demanding analysis method with good sensitivity and selectivity.
Industry’s View on Using Quality Control, Biorelevant, and Clinically Relevant Dissolution Tests for Pharmaceutical Development, Registration, and Commercialization.
This article intends to summarize the current views of the IQ Consortium Dissolution Working Group, which comprises various industry companies, on the roles of dissolution testing throughout...
Bio–relevant characterisation of lipidic formulations and prediction of in vivo exposure
Lipidic formulations (LFs) are increasingly utilised for the delivery of poorly–water soluble drugs to improve oral bioavailability.
The solubility-permeability trade-off of progesterone with cyclodextrins under physiological conditions: Experimental observations and computer simulations
This study intended to evaluate the effect of cyclodextrins on the apparent solubility and permeability of lipophilic drugs under physiological conditions and establish in silico model to choose...
Characterization of stress degradation products of amodiaquine dihydrochloride by liquid chromatography with high‐resolution mass spectrometry and prediction of their properties by using ADMET Predictor™
The degradation behavior of amodiaquine dihydrochloride, an antimalarial drug, was investigated in solution as well as solid states.
Development of long-circulating docetaxel loaded poly (3-hydroxybutyrate-co-3-hydroxyvalerate) nanoparticles: optimization, pharmacokinetic, cytotoxicity and in vivo assessments
Long-circulating Nanoparticles (NPs) are promising drug delivery vehicles which target solid tumors via enhanced permeation and retention effect.
In Vitro Evaluation of Absorption Characteristics of Peramivir for Oral Delivery
Peramivir is a novel antiviral agent approved for the treatment of severe influenza.
Pharmacokinetics of Tedizolid in Obese and Nonobese Subjects
Obesity, defined as body mass index (BMI) 30 kg/m2, is a growing problem worldwide; the prevalence is 38% in the US adult population.