Using Mechanistic Modeling Approaches to Support Bioequivalence Assessments for Oral Products

Using Mechanistic Modeling Approaches to Support Bioequivalence Assessments for Oral Products

Publication: AAPS J
Software: GastroPlus®

This report summarizes the proceedings for Day 1 Session 3 of the 2-day public workshop entitled “Best Practices for Utilizing Modeling Approaches to Support Generic Product Development,” a jointly sponsored workshop by the US Food and Drug Administration (FDA) and the Center for Research on Complex Generics (CRCG) in the year 2022.

Population pharmacokinetics of the dual endothelin receptor antagonist aprocitentan in subjects with or without essential or resistant hypertension

Population pharmacokinetics of the dual endothelin receptor antagonist aprocitentan in subjects with or without essential or resistant hypertension

Publication: J Pharmacokinet Pharmacodyn

Aprocitentan is a novel, potent, dual endothelin receptor antagonist that recently demonstrated efficacy in the treatment of difficult-to-treat (resistant) hypertension.

Using molecularly dissolved drug concentrations in PBBMs improves the prediction of oral absorption from supersaturating formulations

Using molecularly dissolved drug concentrations in PBBMs improves the prediction of oral absorption from supersaturating formulations

Publication: Eur J Pharm Sci
Software: GastroPlus®

Predicting the absorption of drugs from enabling formulations is still challenging due to the limited capabilities of standard physiologically based biopharmaceutics models (PBBMs) to capture complex absorption processes.

PBPK Modeling Approach to Predict the Behavior of Drugs Cleared by Metabolism in Pregnant Subjects and Fetuses

PBPK Modeling Approach to Predict the Behavior of Drugs Cleared by Metabolism in Pregnant Subjects and Fetuses

Publication: Pharmaceutics
Software: GastroPlus®
Therapeutic Areas: PBPK

This study aimed to develop a physiologically based pharmacokinetic (PBPK) model that simulates metabolically cleared compounds’ pharmacokinetics (PK) in pregnant subjects and fetuses.

Pharmacokinetic model of human exposure to ciprofloxacin through consumption of fish

Pharmacokinetic model of human exposure to ciprofloxacin through consumption of fish

Publication: Environ Toxicol Pharmacol
Software: GastroPlus®
Division: PBPK

Fluoroquinolones are broad-spectrum antibiotics that accumulate in the environment.

Use of the Same Model or Modeling Strategy Across Multiple Submissions: Focus on Complex Drug Products

Use of the Same Model or Modeling Strategy Across Multiple Submissions: Focus on Complex Drug Products

Publication: AAPS J
Software: GastroPlus®
Division: PBPK

Evidence shows that there is an increasing use of modeling and simulation to support product development and approval for complex generic drug products in the USA, which includes the use of mechanistic modeling and model-integrated evidence (MIE).

An Integrated Computational Approaches for Designing of Potential Piperidine based Inhibitors of Alzheimer Disease by Targeting Cholinesterase and Monoamine Oxidases Isoenzymes

An Integrated Computational Approaches for Designing of Potential Piperidine based Inhibitors of Alzheimer Disease by Targeting Cholinesterase and Monoamine Oxidases Isoenzymes

Publication: Appl Biochem Biotechnol

The study aimed to evaluate the potential of piperidine-based 2H chromen-2-one derivatives against targeted enzymes, i.e., cholinesterase’s and monoamine oxidase enzymes.

Oligoadenylate Synthetases 1 Enhances DNA Sensor Cgas Translation to Mediate Antiviral Activity

Oligoadenylate Synthetases 1 Enhances DNA Sensor Cgas Translation to Mediate Antiviral Activity

Publication: SSRN Electronic Journal

Oligoadenylate synthetases (OAS) are a family of interferon (IFN)-stimulated genes known to inhibit viral replication through the enzymatic synthesis of 2'-5' oligoadenylates and activation of Ribonuclease L.