In Vitro-In Vivo Correlation of Efavirenz Tablets Using GastroPlus®

In Vitro-In Vivo Correlation of Efavirenz Tablets Using GastroPlus®

Publication: AAPS PharmSciTech
Software: GastroPlus®

The aim of the present work was to use GastroPlus™ software for the prediction of pharmacokinetic profiles and in vitro-in vivo correlation (IVIVC) as tools to optimize the development of new generic medications.

Physiologically Based Pharmacokinetic Modelling to Predict Single- and Multiple-Dose Human Pharmacokinetics of Bitopertin

Physiologically Based Pharmacokinetic Modelling to Predict Single- and Multiple-Dose Human Pharmacokinetics of Bitopertin

Publication: Clin Pharmacokinet
Software: GastroPlus®

This paper describes the use of physiologically based pharmacokinetic (PBPK) modelling and preclinical data to gain insights into and predict bitopertin clinical pharmacokinetics.

In Vitro Characterization of Axitinib Interactions with Human Efflux and Hepatic Uptake Transporters: Implications for Disposition and Drug Interactions

In Vitro Characterization of Axitinib Interactions with Human Efflux and Hepatic Uptake Transporters: Implications for Disposition and Drug Interactions

Publication: Drug Metab Dispos
Software: GastroPlus®

Axitinib is an inhibitor of tyrosine kinase vascular endothelin growth factor receptors 1, 2, and 3. The ATP-binding cassette (ABC) and solute carrier (SLC) transport properties of axitinib...

Investigation of clinical pharmacokinetic variability of an opioid antagonist through physiologically based absorption modeling

Investigation of clinical pharmacokinetic variability of an opioid antagonist through physiologically based absorption modeling

Publication: J Pharm Sci
Software: GastroPlus®

Identifying the source of inter- and/or intrasubject variability in pharmacokinetics (PK) provides fundamental information in understanding the pharmacokinetics-pharmacodynamics relationship...

Dendritic Cell Immunoreceptor Is a New Target for Anti-AIDS Drug Development: Identification of DCIR/HIV-1 Inhibitors

Dendritic Cell Immunoreceptor Is a New Target for Anti-AIDS Drug Development: Identification of DCIR/HIV-1 Inhibitors

Publication: PLoS One
Software: ADMET Predictor®

The HIV-1 pandemic continues to expand while no effective vaccine or cure is yet available. Existing therapies have managed to limit mortality and control viral proliferation, but are associated with side effects...

Similarity-based virtual screening for microtubule stabilizers reveals novel antimitotic scaffold

Similarity-based virtual screening for microtubule stabilizers reveals novel antimitotic scaffold

Publication: J Mol Graph Model
Software: ADMET Predictor®

Microtubules are among the most studied and best characterized cancer targets identified to date. Many microtubule stabilizers have been introduced so far that work by disrupting the...

It’s like playing with a better tennis partner

It’s like playing with a better tennis partner

Are you a whistle-blower? Or do you cringe just to read those words? According to Margaret Heffernan* (links to a dead link) in a 2012 TEDTalk, most whistle-blowers are good guys. A whistle-blower can provide constructive conflict, which is vital for success. Heffernan says that great research teams, relationships, and businesses allow people to deeply disagree. When we are afraid of conflict, our doubts remain hidden. But when we dare to break that silence – when we dare to create conflict – we enable ourselves and the people around us to do our very best thinking.

Physiologically based pharmacokinetic and pharmacodynamic modeling of an antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in a mouse xenograft model of human breast cancer

Physiologically based pharmacokinetic and pharmacodynamic modeling of an antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in a mouse xenograft model of human breast cancer

Publication: Biopharm Drug Dispos
Software: GastroPlus®

The inhibitors of apoptosis proteins (IAPs) are a class of key apoptosis regulators overexpressed or dysregulated in cancer. SM-406/AT-406 is a potent and selective small molecule mimetic of...

A population pharmacokinetic and pharmacodynamic analysis of peginesatide in patients with chronic kidney disease on dialysis

A population pharmacokinetic and pharmacodynamic analysis of peginesatide in patients with chronic kidney disease on dialysis

Publication: PLoS One

Peginesatide (OMONTYS®) is an erythropoiesis-stimulating agent that was indicated in the United States for the treatment of anemia due to chronic kidney disease in adult patients on dialysis prior to...

Intelligent Wondering 8211 Investigative Clinical Pharmacology

Intelligent Wondering 8211 Investigative Clinical Pharmacology

Reviews of new drug applications by regulatory authorities worldwide grow ever more rigorous. I think that one reason for this heightened scrutiny is that reviewers have, over the last 10 years, read many submissions containing results of pharmacometric modeling and simulation analyses. With the use of modeling, explorations of the determinants of drug efficacy and safety are more thorough, and the analyses provide solid support for dose recommendations and labeling content. In short, I think that model-based analyses have raised reviewers’ expectations.