Identification of novel TACE inhibitors compatible with topical application

Identification of novel TACE inhibitors compatible with topical application

Publication: Bioorg Med Chem Lett.
Software: ADMET Predictor®

Targeting the Tumor Necrosis Factor α signalling with antibodies has led to a revolution in the treatment of psoriasis. Locally inhibiting Tumor Necrosis Factor α Converting Enzyme...

Evolution of Circulating Tumor DNA Profile from First-line to Subsequent Therapy in Metastatic Renal Cell Carcinoma

Evolution of Circulating Tumor DNA Profile from First-line to Subsequent Therapy in Metastatic Renal Cell Carcinoma

Publication: Eur Urol

Background: Treatment of metastatic renal cell carcinoma (mRCC) typically entails mechanistically distinct agents across the first- and second-line setting.

Prediction of Losartan Active Carboxylic Acid Metabolite Exposure Following Losartan Administration Using Static and Physiologically-Based Pharmacokinetic Models.

Prediction of Losartan Active Carboxylic Acid Metabolite Exposure Following Losartan Administration Using Static and Physiologically-Based Pharmacokinetic Models.

Publication: J Pharm Sci
Software: GastroPlus®

The aim of this study was to evaluate a strategy based on static and dynamic physiologically based pharmacokinetic (PBPK) modeling for the prediction of metabolite and parent drug area under...

Development and qualification of physiologically based pharmacokinetic models for drugs with atypical distribution behavior: A desipramine case study.

Development and qualification of physiologically based pharmacokinetic models for drugs with atypical distribution behavior: A desipramine case study.

Publication: CPT Pharmacometrics Syst Pharmacol
Software: GastroPlus®
Division: PBPK

Desipramine is a secondary tricyclic amine, which is primarily metabolized by cytochrome 2D6. It shows a high volume of distribution (Vss) (10–50 L/kg) due to its high lipophilicity, unspecific phospholipid binding, and lysosomal trapping.

Food effect: The combined effect of media pH and viscosity on the gastrointestinal absorption of ciprofloxacin tablet

Food effect: The combined effect of media pH and viscosity on the gastrointestinal absorption of ciprofloxacin tablet

Publication: Eur J Pharm Sci
Software: GastroPlus®

The clinical implications of food-drug interactions may have to be taken seriously into account with oral drugs administration in order to minimize variations in drug bioavailability. 

Influence of different proton pump inhibitors on the pharmacokinetics of voriconazole

Influence of different proton pump inhibitors on the pharmacokinetics of voriconazole

Authors: Qi F, Zhu L, Li N, Ge T, Xu G, Liao S
Publication: Int J Antimicrob Agents
Software: GastroPlus®

This study aimed to determine the influence of proton pump inhibitors (PPIs) on the pharmacokinetics of voriconazole and to characterise potential drug-drug interactions (DDIs)...

In vitro dissolution models for the prediction of in vivo performance of an oral mesoporous silica formulation

In vitro dissolution models for the prediction of in vivo performance of an oral mesoporous silica formulation

Publication: J Control Release

Drug release from mesoporous silica systems has been widely investigated in vitro using USP Type II (paddle) dissolution apparatus.

Lead Antimalarial Identification Using in silico Prediction Methods and Simulation

Lead Antimalarial Identification Using in silico Prediction Methods and Simulation

Conference: ASCPT

With increasing resistance to currently available antimalarials, new compounds with activity against resistant parasites are needed. Novel compounds were designed and first-in-human (FIH) simulations...

Mechanistic prediction of food effects for Compound A tablet using PBPK model

Mechanistic prediction of food effects for Compound A tablet using PBPK model

Publication: Saudi J Biol Sci
Software: GastroPlus®
Division: PBPK

Physiologically based pharmacokinetic (PBPK) modeling has been extensively used to study the factors of effect drug absorption, distribution, metabolize and extraction progress in human.

QSP Modeling of Liver AMPK Activation Using NAFLDsym Is Predicted to Reduce Steatosis in NAFLD Patients

QSP Modeling of Liver AMPK Activation Using NAFLDsym Is Predicted to Reduce Steatosis in NAFLD Patients

Conference: ASCPT
Software: NAFLDsym®

Non-alcoholic fatty liver disease (NAFLD) currently has few available treatment options. Bringing effective treatments rapidly to market is paramount.