When medicinal chemists need to improve oral bioavailability (%F) during lead optimization, they systematically modify compound properties mainly based on their own experience and general rules of thumb.
Physiologically-Based Pharmacokinetic Modeling in Lead Optimization I: Evaluation and Adaptation of GastroPlus to Predict Bioavailability of Medchem Series
When medicinal chemists need to improve bioavailability (%F) within a chemical series during lead optimization, they synthesize new series members with systematically modified properties...
DILIsym Services Inc., a Simulations Plus Company, Releases DILIsym® Version 7A
Significant update of liver safety program includes performance and capability enhancements
Simulations Plus Reports First Quarter FY2018 Financial Results
Consolidated net income up 26.0%; diluted earnings per share increased 22.8%
Preparation and Evaluation of Progesterone Nanocrystals to Decrease Muscle Irritation and Improve Bioavailability.
Progesterone (PG) is a crucial immunomodulatory agent during early pregnancy, and nowadays PG oil-based injection (PG/OI) has a huge market all over the world.
Tracking Metoprolol Metabolites in GastroPlus® 9.5
This video shows how to track the metabolites of metoprolol in GastroPlus 9.5.
Model-informed drug development for malaria therapeutics
Malaria is a critical public health problem resulting in substantial morbidity and mortality, particularly in developing countries. Owing to the development of resistance toward current therapies, novel approaches to accelerate...
Simulations Plus Sets Date for 1st Quarter 2018 Earnings Release and Conference Call
Conference Call to be on Tuesday, January 9, 2018, at 4:15 PM ET
Developing a mechanistic absorption model to predict the pharmacokinetics of immediate-release weak base drugs with a long Tmax by incorporating lysosomal trapping.
The objectives of this study were 1) to develop and verify mechanistic absorption models to predict the pharmacokinetics (PK) of two immediate-release weak base drug (WBD) products (Drug X and Drug Y) with a...
In Vitro Dissolution Methodology And Estimated Consequences Of Biowaiver Extension For Immediate Release Solid Oral Dosage Forms With Metformin Hydrochloride
The in vitro dissolution methodologies are frequently used as quality control tools for the assessment of solid oral dosage forms.
Every Jack has His Jill: Finding a Target for Your Combinatorial Library
Pharmaceutical companies regularly run campaigns to evolve their proprietary chemical libraries which are among their most valuable assets.
Physiologically Based Oral Absorption Modelling to Study Gut-Level Drug Interactions
Physiologically based oral absorption models are in silico tools primarily used to guide formulation development and project the clinical performance of formulation variants.
The Combination of GIS and Biphasic to Better Predict In Vivo Dissolution of BCS Class IIb Drugs, Ketoconazole and Raloxifene
The formulation developments and the in vivo assessment of Biopharmaceutical Classification System (BCS) class II drugs are challenging due to their low solubility and high permeability in the...
Synaptophysin expression on circulating tumor cells in patients with castration resistant prostate cancer undergoing treatment with abiraterone acetate or enzalutamide
Background: With the advent of secondary androgen receptor (AR)-targeted therapies in metastatic castration resistant prostate cancer (PC), nonadenocarcinoma PCs are...
Identification of mechanisms of resistance to treatment with abiraterone acetate or enzalutamide in patients with castration-resistant prostate cancer (CRPC)
Background: Two androgen receptor (AR)-targeted therapies, enzalutamide and abiraterone acetate plus prednisone (abiraterone), have been approved for the treatment...
Tracking Metabolites in GastroPlus®
This video shows how to track the N-debutyl metabolite of dronedarone in GastroPlus.
Wildfire Forces Cancelation of LD Micro Conference
Presentations Canceled for Celsius Holdings, Inc., GSI Technology, Inc., PCM, Inc., Simulations-Plus, ADOMANI, Inc., HUTN, Inc., NanoVibronix, Inc. and WidePoint Corp.
IVIVC using in silico and PBPK methods for inhaled drug product development
The physiologically based model of the lung included in GastroPlus™ was used to simulate the absorption, distribution, and pharmacokinetics of two APIs from an inhaled combination product.