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.
Challenges in translational drug research in neuropathic and inflammatory pain: the prerequisites for a new paradigm
Despite an improved understanding of the molecular mechanisms of nociception, existing analgesic drugs remain limited in terms of efficacy in chronic conditions, such as neuropathic pain.
Computer Simulation in Pharmacokinetic and Pharmacodynamic Studies
Computer simulation in the field of Pharmacokinetic and Pharmacodynamics or in silica model is need of the hour in the biomedical field.
Modeling Tolerance Development for the Effect on Heart Rate of the Selective S1P1 Receptor Modulator Ponesimod
Ponesimod is a selective sphingosine-1-phosphate-1 (S1P1 ) receptor modulator currently under investigation for the treatment of multiple sclerosis.
Looking to the future of drug-induced liver injury: an interview with Paul B Watkins
Paul Watkins talks to Francesca Lake, Head of Open Access Publishing: Paul is The Howard Q Ferguson Professor in the Eshelman School of Pharmacy at The University of North Carolina at Chapel Hill (UNC, NC, USA), and an expert in drug safety and drug-induced liver injury (DILI).
Population Pharmacokinetic Evaluation and Missed-Dose Simulations for Eslicarbazepine Acetate Monotherapy in Patients With Partial-Onset Seizures
Given the potential consequences of antiepileptic therapy nonadherence, missed-dose scenarios of 12- to 48-hour dose delays (4-hour intervals) for eslicarbazepine acetate monotherapy...
In vitro and in vivo evaluation of gastro-retentive carvedilol loaded chitosan beads using GastroPlus™
The objective of present investigation was to develop gastro-retentive controlled release system of carvedilol using biological macromolecule, chitosan. 32 full factorial design was adopted for...
Population Pharmacokinetic and Pharmacodynamic Modeling of LY2510924 in Patients with Advanced Cancer.
The objectives of this study were to characterize the pharmacokinetics (PK) of LY2510924, a potent peptide antagonist of the CXCR4 receptor, after subcutaneous administration in patients with...
Discovery of Resistance Pathways to Fibroblast Growth Factor Receptor inhibition in Bladder Cancer
Background Aberrant fibroblast growth factor receptor (FGFR) signaling drives the growth of many bladder cancers. NVP-BGJ398 is a small molecule with potent inhibitory...
Biorelevant Dissolution Models for a Weak Base To Facilitate Formulation Development and Overcome Reduced Bioavailability Caused by Hypochlordyria or Achlorhydria.
In this study, two dissolution models were developed to achieve in vitro–in vivo relationship for immediate release formulations of Compound-A, a poorly soluble weak base with pH-dependent...
Synthesis, antioxidant, antifungal, molecular docking and ADMET studies of some thiazolyl hydrazones
Some thiazolyl hydrazones were synthesized by one pot reaction of thiophene-2-carbaldehyde or 2, 4-dichlorobenzaldehyde, thiosemicarbazide and various phenacyl bromides which were preliminarily...