Pharmaceutical companies regularly run campaigns to evolve their proprietary chemical libraries which are among their most valuable assets.
Physiologically Based Oral Absorption Modelling to Study Gut-Level Drug Interactions
Physiologically based oral absorption models are in silico tools primarily used to guide formulation development and project the clinical performance of formulation variants.
The Combination of GIS and Biphasic to Better Predict In Vivo Dissolution of BCS Class IIb Drugs, Ketoconazole and Raloxifene
The formulation developments and the in vivo assessment of Biopharmaceutical Classification System (BCS) class II drugs are challenging due to their low solubility and high permeability in the...
Synaptophysin expression on circulating tumor cells in patients with castration resistant prostate cancer undergoing treatment with abiraterone acetate or enzalutamide
Background: With the advent of secondary androgen receptor (AR)-targeted therapies in metastatic castration resistant prostate cancer (PC), nonadenocarcinoma PCs are...
Identification of mechanisms of resistance to treatment with abiraterone acetate or enzalutamide in patients with castration-resistant prostate cancer (CRPC)
Background: Two androgen receptor (AR)-targeted therapies, enzalutamide and abiraterone acetate plus prednisone (abiraterone), have been approved for the treatment...
Refining Liver Safety Risk Assessment: Application of Mechanistic Modeling and Serum Biomarkers to Cimaglermin Alfa (GGF2) Clinical Trials
Cimaglermin alfa (GGF2) is a recombinant human protein growth factor in development for heart failure.
Software based approaches for drug designing and development: A systematic review on commonly used software and its applications.
Drug discovery include drug designing and development, is a multifarious and expensive endeavor, where least number of drugs that pass the clinical trials makes it to market.
Phase 1 and pharmacokinetic study of LY3007113, a p38 MAPK inhibitor, in patients with advanced cancer
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.