Skip to main content

Certara Releases D360 Version 6.0, with Extended Capabilities for Preclinical and Clinical Data

Latest release extends cross-platform data access, analysis and collaboration capabilities ST. LOUIS, MO – December 20, 2011 – Certara™, a leading provider of software and services to improve productivity and decision-making from discovery through clinical development, announced today that it has released D360™ version 6.0, with key enhancements that enable users to access data from … Continued

3D-quantitative Structure-activity Relationship and Docking Studies of the Tachykinin NK3 Receptor

The tachykinin NK(3) receptor (NK(3)R) is a novel drug target for schizophrenia and drug abuse. Since few non-peptide antagonists of this G protein-coupled receptor are available, we have initiated this study to gain a better understanding of the structure-activity relationships of NK(3) antagonist compounds. We developed a 3D comparative molecular similarity index analysis (CoMSIA) model … Continued

Population Pharmacokinetic-pharmacodynamic-disease Progression Model for Effects of Anakinra in Lewis Rats with Collagen-induced Arthritis

A population pharmacokinetic-pharmacodynamic-disease progression (PK/PD/DIS) model was developed to characterize the effects of anakinra in collagen-induced arthritic (CIA) rats and explore the role of interleukin-1ß (IL-1ß) in rheumatoid arthritis. The CIA rats received either vehicle, or anakinra at 100 mg/kg for about 33 h, 100 mg/kg for about 188 h, or 10 mg/kg for about … Continued

Pre-clinical Metabolism and Disposition of SB939 (Pracinostat), an Orally Active Histone Deacetylase Inhibitor, and Prediction of Human Pharmacokinetics

The preclinical absorption, distribution, metabolism, and excretion (ADME) properties of Pracinostat [(2E)-3-[2-butyl-1-[2-(diethylamino) ethyl]-1H-benzimidazol-5-yl]-N-hydroxyarylamide hydrochloride; SB939], an orally active histone deacetylase inhibitor, were characterized and its human pharmacokinetics (PK) was predicted using Simcyp® and allometric scaling. SB939 showed high aqueous solubility with high Caco-2 permeability. Metabolic stability was relatively higher in dog and human liver microsomes … Continued

Effect of Microgravity on the Pharmacokinetics of Ibuprofen in Humans

The pharmacokinetics of ibuprofen were studied under microgravity (µG) conditions and compared with those at normal gravity (1G) in humans. Six healthy human volunteers were given 600 mg oral dose ibuprofen during 1-day simulated µG antiorthostatic bed rest position, then at normal position (1G) in a sequential design with 7 days washout time. Saliva and … Continued

Model-based Meta-analysis for Comparative Efficacy and Safety: Application in Drug Development and Beyond

High development cost, low development success, cost-disciplined health-care policies, and intense competition demand an efficient drug development process. New compounds need to bring value to patients by being safe, efficacious, and cost-effective as compared with existing treatment options. Model-based meta-analysis (MBMA) facilitates integration and utilization of summary-level efficacy and safety data, providing a quantitative framework … Continued

Therapeutic Index of Anticoagulants for Prevention of Venous Thromboembolism Following Orthopedic Surgery: A Dose-response Meta-analysis

Information on the comparative effectiveness of drugs is crucial for drug development decisions, in addition to being needed by regulators, prescribers, and payers. We have carried out a dose-response meta-analysis of three end points each for efficacy and bleeding for various anticoagulants evaluated for the prevention of venous thromboembolism (VTE) following orthopedic surgery to assess … Continued

A Dose-response Meta-analysis for Quantifying Relative Efficacy of Biologics in Rheumatoid Arthritis

We present a dose-response meta-analysis to quantify relative efficacy of biologic disease-modifying antirheumatic drugs (DMARDs) in patients with rheumatoid arthritis (RA). There is a strong rationale for this analysis because, although multiple biologics are available, information on head-to-head comparisons is limited. Data on the percentage of patients attaining American College of Rheumatology (ACR) 20, 50, … Continued

Application of a Systems Approach to the Bottom-up Assessment of Pharmacokinetics in Obese Patients: Expected Variations in Clearance

The maintenance dose of a drug is dependent on drug clearance, and thus any biochemical and physiological changes in obesity that affect parameters such as cardiac output, renal function, expression of drug-metabolizing enzymes and protein binding may result in altered clearance compared with that observed in normal-weight subjects (corrected or uncorrected for body weight). Because … Continued

1 of 12