Medicinal chemists have traditionally realized assessments of chemical diversity and subsequent compound acquisition, although a recent study suggests that experts are usually inconsistent in reviewing large data sets.
A strategy for preclinical formulation development using GastroPlus™ as pharmacokinetic simulation tool and a statistical screening design applied to a dog study.
The aim of this paper is to propose a pharmaceutical risk assessment strategy that goes beyond the usual characterisation of a clinical candidate molecule according to the biopharmaceutical classification system (BCS).
Comparison of censored regression and standard regression analyses for modeling relationships between antimicrobial susceptibility and patient- and institution-specific variables
In order to identify patients likely to be infected with resistant bacterial pathogens, analytic methods such as standard regression (SR) may be applied to surveillance data to determine patient- and institution-specific...
Challenges in the transition to model-based development
Practitioners of the art and science of pharmacometrics are well aware of the considerable effort required to successfully complete modeling and simulation activities...
An evaluation of the utility of physiologically based models of pharmacokinetics in early drug discovery
Generic physiologically-based models of pharmacokinetics were evaluated for early drug discovery.
Use of pharmacokinetic-pharmacodynamic target attainment analyses to support phase 2 and 3 dosing strategies for doripenem
A doripenem population pharmacokinetic model and Monte Carlo simulations were utilized for dose regimen decision support for future clinical development.
Viral and cellular gene transcription in fibroblasts infected with small plaque mutants of varicella-zoster virus
Varicella-zoster virus (VZV) is an alphaherpesvirus that causes varicella and herpes zoster. In these experiments, cDNA corresponding to 69 VZV open reading frames was...
Antimicrobial safety: focus on fluoroquinolones
Infrequent toxicities associated with certain drugs and drug classes have recently gained much attention from different health-care perspectives.
Application of an in vitro infection model and simulation for reevaluation of fluoroquinolone breakpoints for Salmonella enterica serotype typhi
Salmonella enterica serotype Typhi and nontyphoidal Salmonella remain major causes of morbidity and mortality worldwide.
Classifying “Kinase Inhibitor‐Likeness” by Using Machine‐Learning Methods
By using an in-house data set of small-molecule structures, encoded by Ghose–Crippen parameters, several machine learning techniques were applied to distinguish between kinase inhibitors...
Application of Full Physiological Models for Pharmaceutical Drug Candidate Selection and Extrapolation of Pharmacokinetics to Man
This paper describes how we are applying physiologically based models of pharmacokinetics as an integrated part in the research and preclinical development of novel drugs.
Relationship between increased levofloxacin use and decreased susceptibility of Streptococcus pneumoniae in the United States
Increasing reports of fluoroquinolone-non-susceptible Streptococcus pneumoniae are of clinical concern. We examined the relationship between outpatient fluoroquinolone...
Pharmacokinetics of oritavancin in plasma and skin blister fluid following administration of a 200-milligram dose for 3 days or a single 800-milligram dose
Oritavancin is a novel glycopeptide currently being developed for the treatment of complicated skin and skin structure infections (cSSSI), including those caused by multidrug...
Assessment of pharmacokinetic-pharmacodynamic target attainment of gemifloxacin against Streptococcus pneumoniae
The treatment of community-acquired respiratory tract infections has been complicated by the emergence of multidrug-resistant Streptococcus pneumoniae.
Population pharmacokinetics and pharmacodynamics of garenoxacin in patients with community-acquired respiratory tract infections
Garenoxacin (T-3811ME, BMS-284756) is a novel, broad-spectrum des-F(6) quinolone currently under study for the treatment of community-acquired respiratory tract infections.
The cost-effectiveness of cefepime plus metronidazole versus imipenem/cilastatin in the treatment of complicated intra-abdominal infection
Our objective was to compare the economic benefits of cefepime plus metronidazole with those of imipenem/cilastatin in the treatment of complicated intra-abdominal infections.
Pharmacokinetics, safety, and tolerability of ascending single intravenous doses of oritavancin administered to healthy human subjects
tavancin (LY333328 diphosphate) is a novel glycopeptide antimicrobial agent with potent microbiological activity in vitro against Gram-positive bacteria.
Regional Intestinal Absorption and Biliary Excretion of Fluvastatin in the Rat: Possible Involvement of mrp2
The first purpose of this study was to investigate the in vivo absorption, biliary secretion, and first-pass effect of fluvastatin following regional intestinal dosing in the rat.