Translating Disposition of Sotalol from Healthy Adults to Predict Its Behavior in Pediatric and Adult Subjects with Enhanced and Diminished Renal Clearance

Translating Disposition of Sotalol from Healthy Adults to Predict Its Behavior in Pediatric and Adult Subjects with Enhanced and Diminished Renal Clearance

Conference: AAPS
Software: GastroPlus®
Division: PBPK

To extend a physiologically based pharmacokinetic (PBPK) model of sotalol developed in healthy adults to predict its behavior in pediatric subjects and adults with varying degrees of renal clearance…

A Pharmacokinetic and Safety Evaluation of Single Oral Doses of Eszopiclone in Pediatric Subjects from 6 to 17 Years of Age with Attention Deficit Hyperactivity Disorder and Insomnia

A Pharmacokinetic and Safety Evaluation of Single Oral Doses of Eszopiclone in Pediatric Subjects from 6 to 17 Years of Age with Attention Deficit Hyperactivity Disorder and Insomnia

Conference: American Academy of Child & Adolescent Psychiatry (AACAP)

Eszopiclone is a single-isomer, nonbenzodiazepine, cyclopyrrolone agent that has demonstrated efficacy with both polysomnography (PSG) and patient-reported measures in non-elderly adults with chronic primary…

It’s not gloom and doom if it helps to frame the problem.

It’s not gloom and doom if it helps to frame the problem.

I know, I know — you don’t want to read another doom and gloom blog. But, in a recent article in the National Review* (link is no longer available), Peter Thiel does an excellent job of linking the desperate necessity of advancements in technology and science with the broader societal crises we are now experiencing. Thiel posits that there is a mistaken, but nearly universal, background assumption about easy progress that underlies our unwillingness to tackle difficult problems.

Grouping Pharmacokinetic Profiles Using Kohonen Self-Organizing Maps

Grouping Pharmacokinetic Profiles Using Kohonen Self-Organizing Maps

Conference: ISSX
Division: PBPK

The shapes of plasma concentration versus time (Cp-time) profiles from large clinical trials are often highly variable, even in well-controlled trials involving homogeneous cohorts.

Transporter-Based in vitro-in vivo Extrapolation (IVIVE)

Transporter-Based in vitro-in vivo Extrapolation (IVIVE)

Conference: ISSX
Software: GastroPlus®
Division: PBPK

The use of in vitro data to predict the pharmacokinetics (PK) of drugs whose disposition is mediated by transporters is complicated due to unknown transporter expression levels in individual tissues both…

A sequence within the varicella-zoster virus (VZV) OriS is a negative regulator of DNA replication and is bound by a protein complex containing the VZV ORF29 protein

A sequence within the varicella-zoster virus (VZV) OriS is a negative regulator of DNA replication and is bound by a protein complex containing the VZV ORF29 protein

Publication: J Virol
Division: PBPK

The architecture of the varicella-zoster virus (VZV) origin of DNA replication (OriS) differs significantly from that of the herpes simplex virus (HSV) DNA replication origin.

Pharmacokinetic (PK) And Pharmacodynamic (PD) Modeling Of Subcutaneous (Sc) Ly2189102, A Neutralizing IL-1 Beta Antibody, In Patients With Type 2 Diabetes Mellitus

Pharmacokinetic (PK) And Pharmacodynamic (PD) Modeling Of Subcutaneous (Sc) Ly2189102, A Neutralizing IL-1 Beta Antibody, In Patients With Type 2 Diabetes Mellitus

Conference: European Association for the Study of Diabetes (EASD)

LY2189102, a humanized neutralizing IL-1β antibody, was studied in type 2 diabetes mellitus (T2DM) patients with C-reactive protein (CRP) ≥ 2 mg/L, who received weekly subcutaneous doses of LY2189102…

Development of a physiologically based model for oseltamivir and simulation of pharmacokinetics in neonates and infants

Development of a physiologically based model for oseltamivir and simulation of pharmacokinetics in neonates and infants

Publication: Clin Pharmacokinet
Software: GastroPlus®

Physiologically based pharmacokinetic (PBPK) modelling can assist in the development of drug therapies and regimens suitable for challenging patient populations such as very young children.

In Vitro and In Silico Strategies to Identify OATP1B1 Inhibitors and Predict Clinical Drug–Drug Interactions

In Vitro and In Silico Strategies to Identify OATP1B1 Inhibitors and Predict Clinical Drug–Drug Interactions

Publication: Pharm Res
Software: ADMET Predictor®

To establish in vitro and in silico models that predict clinical drug–drug interactions (DDIs) with the OATP1B1 (SLCO1B1) transporter.

Selection of oral bioavailability enhancing formulations during drug discovery

Selection of oral bioavailability enhancing formulations during drug discovery

Publication: Drug Dev Ind Pharm
Software: GastroPlus®

The objective of this paper was to identify oral bioavailability enhancing approaches for a poorly water-soluble research compound during drug discovery stages using minimal amounts of material.

Pre-clinical and clinical pharmacokinetics of PF-02413873, a non-steroidal progesterone receptor antagonist

Pre-clinical and clinical pharmacokinetics of PF-02413873, a non-steroidal progesterone receptor antagonist

Publication: Drug Metab Dispos
Software: GastroPlus®

The recently discovered selective nonsteroidal progesterone receptor (PR) antagonist 4-[3-cyclopropyl-1-(methylsulfonylmethyl)-5-methyl-1H-pyrazol-4-yl]oxy-2,6-dimethylbenzonitrile (PF-02413873)...

Simulation of Tobramycin Pharmacokinetics After Topical Ophthalmic Administration

Simulation of Tobramycin Pharmacokinetics After Topical Ophthalmic Administration

Conference: CRS
Software: GastroPlus®
Division: PBPK

Tobramycin belongs to the class of aminoglycoside antibiotics. It does not bind to serum proteins [1], is eliminated mainly by renal secretion [2] and is poorly absorbed from the gastrointestinal tract [3].

The Application of Physiologically Based Pharmacokinetic Modelling to Understanding the Clinical Pharmacokinetics of UK-369,003

The Application of Physiologically Based Pharmacokinetic Modelling to Understanding the Clinical Pharmacokinetics of UK-369,003

Publication: Drug Metab Dispos
Software: GastroPlus®

5-[2-Ethoxy-5-(4-ethyl-piperazine-1-sulfonyl)-pyridin-3-yl]-3-ethyl-2-(2-methoxy-ethyl)-2,6-dihydro-pyrazolo[4,3-d]pyrimidin-7-one (UK-369,003) is a phosphodiesterase-5...