Physiologically based pharmacokinetic modeling to characterize enterohepatic recirculation and predict food effect on the pharmacokinetics of hyzetimibe

Physiologically based pharmacokinetic modeling to characterize enterohepatic recirculation and predict food effect on the pharmacokinetics of hyzetimibe

Authors: Chen W, Ruan Z, Lou H, Yang D, Chen J, Shao R, Jiang B
Publication: Eur J Pharm Sci
Keywords: biopharmaceutics, ehc, gastroplus, pbbm, PBPK modeling, physiologically based pharmacokinetics, virtual bioequivalence
Software: GastroPlus®

Hyzetimibe is a cholesterol absorption inhibitor indicated for the treatment of hypercholesterolemia.

Predictive performance of physiologically based kinetic (PBK) models based on in silic o/ in vitro to in vivo extrapolation (IS/IVIVE)

Predictive performance of physiologically based kinetic (PBK) models based on in silic o/ in vitro to in vivo extrapolation (IS/IVIVE)

Authors: Kalra P, Zhou H, Lawless M
Conference: EuroTox
Keywords: admet predictor, gastroplus, in silico in vitro–in vivo extrapolation (IVIVE), machine learning (ML), PBPK modeling
Software: ADMET Predictor®, GastroPlus®
Division: PBPK

The applicability of PBK modelling in next generation risk assessment ( hinges on accurate prediction of human plasma concentrations without reliance on animal in vivo kinetics data.

The anti-infective crotalicidin peptide analog RhoB-Ctn[1–9] is harmless to bovine oocytes and able to induce parthenogenesis in vitro

The anti-infective crotalicidin peptide analog RhoB-Ctn[1–9] is harmless to bovine oocytes and able to induce parthenogenesis in vitro

Authors: dos Santos AT, Kumar S, Albuquerque JVS, Arcce IML, Chaves OA, Cruz GS, Carretero VJ, Melo LM, Chaves MS, Guijo JMH, Freitas VJF, Rádis-Baptista G
Publication: Toxicon
Keywords: antimicrobial, crotalicidin, cytotoxicity, in vitro, venom glands
Software: ADMET Predictor®
Therapeutic Areas: Anti-effective

Crotalicidin is a cathelicidin-related anti-infective (antimicrobial) peptide expressed in the venom glands of the South American rattlesnake Crotalus durissus terrificus. 

Drug–drug interaction prediction of ziritaxestat using a physiologically based enzyme and transporter pharmacokinetic network interaction model

Drug–drug interaction prediction of ziritaxestat using a physiologically based enzyme and transporter pharmacokinetic network interaction model

Authors: Perrier J, Gualano V, Helmer E, Namour F, Lukacova V, Taneja A
Publication: Clinical and Translational Science
Keywords: CYP inhibition, drug-drug interactions (DDIs), PBPK modeling, pharmacokinetics (PK)
Division: PBPK

Ziritaxestat, an autotaxin inhibitor, was under development for the treatment of idiopathic pulmonary fibrosis.

Physiologically based pharmacokinetic modelling to predict drug–drug interactions for encorafenib. Part I. Model building, validation, and prospective predictions with enzyme inhibitors, inducers, and transporter inhibitors

Physiologically based pharmacokinetic modelling to predict drug–drug interactions for encorafenib. Part I. Model building, validation, and prospective predictions with enzyme inhibitors, inducers, and transporter inhibitors

Authors: Sivacharan K, Ahmed T, Praveen S
Publication: Xenobiotica
Keywords: cyp induction, CYP inhibition, ddI, gastroplus, p-gp, PBPK modeling, physiologically based pharmacokinetics, transporter-based interactions
Software: GastroPlus®

Encorafenib, a potent BRAF kinase inhibitor undergoes significant metabolism by CYP3A4 (83%) and CYP2C19 (16%) and also a substrate of P-glycoprotein (P-gp).

Mind the Gap: Model-Based Switching from Selatogrel to Maintenance Therapy with Oral P2Y12 Receptor Antagonists

Mind the Gap: Model-Based Switching from Selatogrel to Maintenance Therapy with Oral P2Y12 Receptor Antagonists

Authors: Hsin CH, Dingemanse J, Henrich A, Bernaud C, Gehin M, Krause A
Publication: Biomolecules
Keywords: emergency treatment, injections, myocardial infarction, P2Y12 receptor antagonists, platelet aggregation

The P2Y12 receptor antagonist selatogrel is being developed for subcutaneous self-administration with a ready-to-use autoinjector at the onset of acute myocardial infarction (AMI)symptoms.

Dabigatran Dosing Proposal for Adults With Atrial Fibrillation: Stress-Testing Renal Function Range in Real World Patients

Dabigatran Dosing Proposal for Adults With Atrial Fibrillation: Stress-Testing Renal Function Range in Real World Patients

Authors: Powell JR, AlQaraghuli F, Fiedler-Kelly J, Gonzalez D, Weiner D
Publication: Clin Pharmacol Ther
Keywords: atrial fibrillation, Dabigatran
Division: Clinical Pharmacology and Pharmacometrics (CPP)

Dabigatran is the first of four direct-acting oral anticoagulants approved to prevent stroke in adult patients with atrial fibrillation using a fixed two-dose scheme compared with warfarin dosing adjusted to...

Physiologically based pharmacokinetic modeling (PBPK) to predict drug-drug interactions for encorafenib. Part II. Prospective predictions in hepatic and renal impaired populations with clinical inhibitors and inducers

Physiologically based pharmacokinetic modeling (PBPK) to predict drug-drug interactions for encorafenib. Part II. Prospective predictions in hepatic and renal impaired populations with clinical inhibitors and inducers

Authors: Kollipara S, Ahmed T, Praveen S
Publication: Xenobiotica
Keywords: cyp induction, CYP inhibition, ddI, disease populations, Drug-drug interactions, gastroplus, kidney impairment, liver impairment, PBPK modeling, physiologically based pharmacokinetics
Software: GastroPlus®

Encorafenib, a potent BRAF kinase inhibitor gets significantly metabolised by CYP3A4 (83%) and CYP2C19 (16%) and is a substrate for P-glycoprotein...

SubQ-Sim: A Subcutaneous Physiologically Based Biopharmaceutics Model. Part 1: The Injection and System Parameters

SubQ-Sim: A Subcutaneous Physiologically Based Biopharmaceutics Model. Part 1: The Injection and System Parameters

Authors: Pepin X, Grant I, Wood JM
Publication: Pharmaceutical Research
Keywords: HIV, Oncology, PBPK model, PBPK modeling, subcutaneous (SC) route
Division: PBPK

To construct a detailed mechanistic and physiologically based biopharmaceutics model capable of predicting 1) device-formulation-tissue interaction during the injection process and 2) binding, degradation, local distribution, diffusion, and drug absorption, following subcutaneous injection.