Phase I study of the investigational oral mTORC1/2 inhibitor sapanisertib (TAK-228): tolerability and food effects of a milled formulation in patients with advanced solid tumours

Phase I study of the investigational oral mTORC1/2 inhibitor sapanisertib (TAK-228): tolerability and food effects of a milled formulation in patients with advanced solid tumours

Publication: ESMO Open
Software: GastroPlus®

Sapanisertib (TAK-228) is an investigational, orally available, potent and highly selective mTORC1/2 inhibitor demonstrating promise in numerous malignancies.

Physiologically-Based Pharmacokinetic Modeling in Lead Optimization II: “Rational Bioavailability Design” by Global Sensitivity Analysis to Identify Properties Affecting Bioavailability.

Physiologically-Based Pharmacokinetic Modeling in Lead Optimization II: “Rational Bioavailability Design” by Global Sensitivity Analysis to Identify Properties Affecting Bioavailability.

Publication: Mol Pharm
Division: PBPK

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

Physiologically-Based Pharmacokinetic Modeling in Lead Optimization I: Evaluation and Adaptation of GastroPlus to Predict Bioavailability of Medchem Series

Publication: Mol Pharm
Division: PBPK

When medicinal chemists need to improve bioavailability (%F) within a chemical series during lead optimization, they synthesize new series members with systematically modified properties...

Preparation and Evaluation of Progesterone Nanocrystals to Decrease Muscle Irritation and Improve Bioavailability.

Preparation and Evaluation of Progesterone Nanocrystals to Decrease Muscle Irritation and Improve Bioavailability.

Publication: AAPS PharmSciTech
Software: GastroPlus®

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.

Model-informed drug development for malaria therapeutics

Model-informed drug development for malaria therapeutics

Publication: Annu Rev Pharmacol Toxicol

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...

Developing a mechanistic absorption model to predict the pharmacokinetics of immediate-release weak base drugs with a long Tmax by incorporating lysosomal trapping.

Developing a mechanistic absorption model to predict the pharmacokinetics of immediate-release weak base drugs with a long Tmax by incorporating lysosomal trapping.

Publication: Drug Metab Pharmacokinet
Software: GastroPlus®

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...

Physiologically Based Oral Absorption Modelling to Study Gut-Level Drug Interactions

Physiologically Based Oral Absorption Modelling to Study Gut-Level Drug Interactions

Authors: Chung J, Kesisoglou F
Publication: J Pharm Sci
Software: GastroPlus®

Physiologically based oral absorption models are in silico tools primarily used to guide formulation development and project the clinical performance of formulation variants.