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...
Population Pharmacokinetics (PK) and Exposure-Efficacy Analyses of Nivolumab in Subjects with Advanced Hepatocellular Carcinoma (HCC)
Nivolumab is a fully human immunoglobulin G4 (IgG4) monoclonal antibody (mAb) that selectively binds to the programmed death-1 (PD-1) membrane receptor. PD-1 is a negative regulatory molecule expressed...
Population Pharmacokinetics and Exposure-Response Analyses for Abatacept in Juvenile Idiopathic Arthritis
Polyarticular-course juvenile idiopathic arthritis (pJIA) is the most common chronic rheumatic disorder in children and one of the leading causes of childhood-acquired disability. Treatment with biologic...
Systemization of Time-to-Event Analyses for Pharmacometric Applications
In addition to the values of efficacy and safety endpoints, the timing of such endpoints relative to the start of treatment is often of interest. A commonly used statistical methodology for analyzing such...
Ceftolozane/Tazobactam Dose Selection for Pediatric Patients (Birth to <18 years)
Ceftolozane/tazobactam is a combination of the novel cephalosporin, ceftolozane, and the beta-lactamase inhibitor, tazobactam. It is approved for the treatment of complicated urinary tract infections (cUTI)...
Prospective Liver Safety Comparison of Two Treatments for Autosomal-Dominant Polycystic Kidney Disease (ADPKD) Using Quantitative Systems Toxicology Modeling
The main objective of this research was to prospectively compare the potential for lixivaptan to cause liver toxicity to a comparator drug in the same class, tolvaptan, which has produced off-target liver signals in clinical trials.
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.
Simulations Plus Reports Preliminary Revenues for Fourth Quarter and Fiscal Year 2017
Company Reports Record Fourth-Quarter and Full-Year Revenues
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.
Understanding dermal drug disposition using TCAT™ – a novel PBPK model
Scientists from GlaxoSmithKline and Simulations Plus have collaborated to develop a mathematical model, Transdermal Compartmental Absorption & Transit (TCAT™), that allows better understanding of drug penetration through the skin while accounting for the formulation characteristics, evaporation and precipitation effects that influence dermal delivery.
Sarcomatoid Renal Cell Carcinoma: The Apple Doesn’t Fall Far from the Tree
The most comprehensive sequencing effort of sarcomatoid renal cell carcinoma (sRCC) to date reinforces the notion that the sarcomatoid component is closely related to the...