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

Better bioavailability: The role of PBPK software predictions
If a new drug candidate behaves unexpectedly when dosed to animals or humans, it’s likely to delay or even terminate the drug’s development.

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

Assessing the utility of in silico tools in early drug development: The case of a pharmaceutically relevant formulation of the prodrug psilocybin
Depressive disorders contribute to an excruciating global mental health burden.

Exploring the impact of CYP2D6 and UGT2B7 gene-drug interactions, and CYP-mediated DDI on oxycodone and oxymorphone pharmacokinetics using physiologically-based pharmacokinetic modeling and simulation
Oxycodone is one of the most commonly used opioids to treat moderate to severe pain.

Preclinical characterization of the absorption and disposition of the brain penetrant PI3K/mTOR inhibitor paxalisib and prediction of its pharmacokinetics and efficacy in human
Glioblastoma multiforme (GBM) is the most common primary brain tumour in adults.

PBPK Modeling Approach to Predict the Behavior of Drugs Cleared by Metabolism in Pregnant Subjects and Fetuses
This study aimed to develop a physiologically based pharmacokinetic (PBPK) model that simulates metabolically cleared compounds’ pharmacokinetics (PK) in pregnant subjects and fetuses.

Simulations Plus Embarks on Collaboration with Northeastern University and The TIM Company Through New FDA Grant
Partnership aims to integrate experimental data and PBPK modeling to identify key formulation factors to accelerate modified-release product development

January 2024 GastroPlus Newsletter
GastroPlus® Newsletter January 2024

Pharmacokinetic model of human exposure to ciprofloxacin through consumption of fish
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
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).

January 2024 News/Events
10 Most Read Journal Articles of 2023

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

Prediction of pharmacokinetics of an anaplastic lymphoma kinase inhibitor in rat and monkey: application of physiologically based pharmacokinetic model as an alternative tool to minimise animal studies
The pharmacokinetic (PK) and toxicokinetic profile of a drug from its preclinical evaluation helps the researcher determine whether the drug should be tested in humans based on its safety and toxicity.

10 Most Read Journal Articles of 2023
In our industry, new research is constantly evolving our most current knowledge—and it’s critical to stay up-to-date with the latest advancements and best practices.

GP ADR-Dermal Module Flyer
The Transdermal Compartmental Absorption & Transit (TCAT™) model represents the skin as a collection of the following compartments: stratum corneum, viable epidermis, dermis, sebum, hair lipid, and hair core

GP ADR-Intraarticular Module Flyer
Understanding the knee joint physiology and its impact on drug PK after intraarticular (IA) injection is critical for developing new drugs aiming to cure rheumatoid arthritis (RA) and other specific diseases affecting human joints.

GP ADR-Intramuscular Module Flyer
The intramuscular (IM) drug delivery model represents the site of injection as a single compartment. Within this compartment, drug can be bound, and local clearance can take place. Drug can also be transported into the lymph or systemic circulation.