Determination of Susceptibility Breakpoints for the Novel Oxazolidinone Tedizolid

Determination of Susceptibility Breakpoints for the Novel Oxazolidinone Tedizolid

Conference: ECCMID

Tedizolid is a novel oxazolidinone antibacterial with potent in vitro activity against a wide range of Gram-positive pathogens, such as Staphylococcus aureus (including methicillin-resistant S. aureus)...

Run Record for Model Development

Run Record for Model Development

The EMA and FDA recommend including a run record in your technical report to describe any major decisions and should include an overview of the steps taken during model development. KIWI 1.3, available in May 2015, will reduce the time taken to perform this task to just minutes.

Elucidation of the Multiple Activities of Abiraterone by a Synthetic Chemistry Approach

Elucidation of the Multiple Activities of Abiraterone by a Synthetic Chemistry Approach

Publication: Clin and Experimental Pharma

Objective: Novel agents to treat metastatic prostate cancer include a class of drugs which function primarily by inhibiting the action of the CYP17 enzyme, which results...

The importance of critical micellar concentration for the prediction of solubility enhancement in biorelevant media

The importance of critical micellar concentration for the prediction of solubility enhancement in biorelevant media

Publication: Mol Pharm
Software: ADMET Predictor®

This study evaluated if the intrinsic surface properties of compounds are related to the solubility enhancement (SE) typically observed in biorelevant media like fasted state simulated intestinal fluids (FaSSIF).

Phenotypic and molecular characterization of circulating tumor cells (CTCs) in patients with castration resistant prostate cancer (CRPC) undergoing treatment with abiraterone acetate or enzalutamide

Phenotypic and molecular characterization of circulating tumor cells (CTCs) in patients with castration resistant prostate cancer (CRPC) undergoing treatment with abiraterone acetate or enzalutamide

Publication: Cancer

Despite the introduction of a number of new treatment options (such as abiraterone acetate and enzalutamide) for castration resistant prostate cancer (CRPC), patients with...

Understanding Disease-Drug Interactions in Cancer Patients: Implications for Dosing Within the Therapeutic Window

Understanding Disease-Drug Interactions in Cancer Patients: Implications for Dosing Within the Therapeutic Window

Publication: Clin Pharmacol Ther
Division: PBPK

The human inflammatory response can result in the alteration of drug clearance through effects on metabolizing enzymes or transporters.

In Silico Modeling Can Predict the Unforeseen Renal Failure Caused by SGX523, a c-MET Kinase Inhibitor

In Silico Modeling Can Predict the Unforeseen Renal Failure Caused by SGX523, a c-MET Kinase Inhibitor

Conference: SOT
Keywords: ADMET, PBPK, renal, renal failure
Division: PBPK

SGX523 is a quinoline containing,c-MET kinase inhibitor with an IC50 of 4nM (BuchananSGetal.,2009): Inhibited thegrowth of human glioblastoma lung and gastric cancer xenografts in mice, in a Phase 1 clinical...

Predicting Five Rat Acute Toxicity Endpoints with ANNE Models using ADMET Predictor™

Predicting Five Rat Acute Toxicity Endpoints with ANNE Models using ADMET Predictor™

Conference: SOT
Software: ADMET Predictor®
Division: PBPK

Alternative methods are being explored to predict the toxicity of chemicals to reduce use of animals. Laboratory/Animal tests are costly in time and money, Cheminformatics (QSTR) presents a good alternative to…

The influence of salt chaotropicity, column hydrophobicity and analytes’ molecular properties on the retention of pramipexole and its impurities

The influence of salt chaotropicity, column hydrophobicity and analytes’ molecular properties on the retention of pramipexole and its impurities

Publication: J of Chromatography
Software: ADMET Predictor®

The aim of this study was to examine the interaction of the chaotropic salts of different position in Hofmeister series (CF3COONa, NaClO4, NaPF6) added to the mobile phase with the stationary phases of...

Fluorometholone Ocular Suspension PBPK Simulations Using the OCAT™ Model in GastroPlus™

Fluorometholone Ocular Suspension PBPK Simulations Using the OCAT™ Model in GastroPlus™

Conference: GTCBio
Division: PBPK

Development of generic formulations of ophthalmic corticosteroids and regulatory acceptance of bioequivalence can be facilitated by analysis of the mechanisms of ocular dissolution, absorption...

Prediction of Pharmacokinetics and Penetration of Moxifloxacin in Human with Intra-Abdominal Infection Based on Extrapolated PBPK Model

Prediction of Pharmacokinetics and Penetration of Moxifloxacin in Human with Intra-Abdominal Infection Based on Extrapolated PBPK Model

Publication: Korean J Physiol Pharmacol
Software: GastroPlus®

The aim of this study is to develop a physiologically based pharmacokinetic (PBPK) model in intra-abdominal infected rats, and extrapolate it to human to predict moxifloxacin pharmacokinetics profiles in...

Design, Synthesis and Pharmacological evaluation of N-[4-(4-(alkyl/aryl/heteroaryl) -piperazin-1-yl) -phenyl] -carbamic acid ethyl ester derivatives as novel anticonvulsant agents

Design, Synthesis and Pharmacological evaluation of N-[4-(4-(alkyl/aryl/heteroaryl) -piperazin-1-yl) -phenyl] -carbamic acid ethyl ester derivatives as novel anticonvulsant agents

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

A series of alkyl/aryl/heteroaryl piperazine derivatives (37–54) were designed and synthesized as potential anticonvulsant agents. The target compounds are endowed with satisfactory physicochemical as well as pharmacokinetic properties.

Estimation of the chemical-induced eye injury using a weight-of-evidence (WoE) battery of 21 artificial neural network (ANN) c-QSAR models (QSAR-21): Part I: Irritation potential

Estimation of the chemical-induced eye injury using a weight-of-evidence (WoE) battery of 21 artificial neural network (ANN) c-QSAR models (QSAR-21): Part I: Irritation potential

Authors: Verma RP, Matthews EJ
Publication: Regul Toxicol Pharmacol
Software: ADMET Predictor®

Evaluation of potential chemical-induced eye injury through irritation and corrosion is required to ensure occupational and consumer safety for industrial, household and cosmetic ingredient chemicals.