The acute effects of daily nicotine intake on heart rate – A toxicokinetic and toxicodynamic modelling study

The acute effects of daily nicotine intake on heart rate – A toxicokinetic and toxicodynamic modelling study

Publication: Regul Toxicol Pharmacol
Software: ADMET Predictor®

Joint physiologically-based toxicokinetic and toxicodynamic (PBTK/TD) modelling was applied to simulate concentration-time profiles of nicotine, a well-known stimulant, in the human body following single and repeated dosing.

Viscosity-mediated negative food effect on oral absorption of poorly-permeable drugs with an absorption window in the proximal intestine: In vitro experimental simulation and computational verification

Viscosity-mediated negative food effect on oral absorption of poorly-permeable drugs with an absorption window in the proximal intestine: In vitro experimental simulation and computational verification

Publication: Eur J Pharm Sci
Software: GastroPlus®

Concomitant food intake can diminish oral absorption of drugs with limited permeability and an absorption window in the proximal intestine, due to viscosity-mediated decrease in dosage form disintegration time and drug dissolution rate.

Detection and phenotyping of circulating tumor cells in high-risk localized prostate cancer

Detection and phenotyping of circulating tumor cells in high-risk localized prostate cancer

Publication: Clin Genitourin Cancer

Background: In this study, we aimed to determine the feasibility of identifying CTCs in patients with HRLPC, using a modified isolation procedure using the CellSearch...

Eslicarbazepine and the enhancement of slow inactivation of voltage-gated sodium channels: A comparison with carbamazepine, oxcarbazepine and lacosamide

Eslicarbazepine and the enhancement of slow inactivation of voltage-gated sodium channels: A comparison with carbamazepine, oxcarbazepine and lacosamide

Publication: Neuropharmacology
Software: ADMET Predictor®

This study aimed at evaluating the effects of eslicarbazepine, carbamazepine (CBZ), oxcarbazepine (OXC) and lacosamide (LCM) on the fast and slow inactivated states of voltage-gated sodium channels (VGSC).

Computational Predictions of Glass-Forming Ability and Crystallization Tendency of Drug Molecules

Computational Predictions of Glass-Forming Ability and Crystallization Tendency of Drug Molecules

Publication: Mol Pharm
Software: ADMET Predictor®

Amorphization is an attractive formulation technique for drugs suffering from poor aqueous solubility as a result of their high lattice energy.

RNA-seq reveals aurora kinase-driven mTOR pathway activation in patients with sarcomatoid metastatic renal cell carcinoma

RNA-seq reveals aurora kinase-driven mTOR pathway activation in patients with sarcomatoid metastatic renal cell carcinoma

Publication: Mol Cancer Res

Sarcomatoid metastatic renal cell carcinoma (mRCC) is associated with a poor prognosis, and the biology of the disease has been inadequately characterized.

Physiologically Based Absorption Modelling to Predict the Impact of Drug Properties on Pharmacokinetics of Bitopertin

Physiologically Based Absorption Modelling to Predict the Impact of Drug Properties on Pharmacokinetics of Bitopertin

Publication: AAPS J
Software: GastroPlus®

Bitopertin (RG1678) is a glycine reuptake inhibitor in phase 3 trials for treatment of schizophrenia. Its clinical oral pharmacokinetics is sensitive to changes in drug substance particle size and dosage form.

Discovery of furan-2-carbohydrazides as orally active glucagon receptor antagonists

Discovery of furan-2-carbohydrazides as orally active glucagon receptor antagonists

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

Furan-2-carbohydrazides were found as orally active glucagon receptor antagonists. Starting from the hit compound 5, we successfully determined the structure activity relationships of a series...

In Silico Prediction of Major Drug Clearance Pathways by Support Vector Machines with Feature-Selected Descriptors

In Silico Prediction of Major Drug Clearance Pathways by Support Vector Machines with Feature-Selected Descriptors

Publication: Drug Metab Dispos
Software: ADMET Predictor®

We have previously established an in silico classification method ("CPathPred") to predict the major clearance pathways of drugs based on an empirical decision with only four physicochemical...