ARRY-403 is a glucokinase activator developed for the treatment of diabetes. Less than dose-proportional exposure was observed during single ascending dose studies with ARRY-403.
Simulations Plus Reports First Quarter FY2015 Financial Results
Final report of first quarter financial results after Cognigen merger; net revenues up 54%; gross profit increased 41%
Physiologically based pharmacokinetic modelling in drug discovery and development: A pharmaceutical industry perspective
The application of physiologically based pharmacokinetic (PBPK) modeling has developed rapidly within the pharmaceutical industry and is becoming an integral part of drug discovery and development.
Simulations Plus Sets Date for 1st Quarter 2015 Earnings Release and Conference Call
Conference Call to be on Wednesday, January 14, at 4:15 PM ET
Comparison of in silico tools for evaluating rat oral acute toxicity
Different in silico models have been developed and implemented for the evaluation of mammalian acute toxicity, exploring acute oral toxicity data expressed as median lethal dose (LD(50)).
The potency–insolubility conundrum in pharmaceuticals: Mechanism and solution for hepatitis C protease inhibitors
As compounds are optimized for greater potency during pharmaceutical discovery, their aqueous solubility often decreases, making them less viable as orally-administered drugs.
The potency-insolubility conundrum in pharmaceuticals: Mechanism and solution for hepatitis C protease inhibitors
As compounds are optimized for greater potency during pharmaceutical discovery, their aqueous solubility often decreases, making them less viable as orally-administered drugs.
Relationships between the antidotal efficacy and structure, PK/PD parameters and bio-relevant molecular descriptors of AChE reactivating oximes: inclusion and integration to biopharmaceutical classification systems
The therapeutic outcome of oximes used as reactivators of phosphorylated human acetylcholinesterase (AChE) is influenced, among other factors, by their biological distribution, their in vivo ability...
In vitro-in vivo correlations: general concepts, methodologies and regulatory applications
The major objective of in vitro-in vivo correlations is to be able to use in vitro data to predict in vivo performance serving as a surrogate for an in vivo bioavailability test and to support biowaivers.
Chromatographic lipophilicity as a predictor of antiproliferative activity of 17-picolyl and 17-picolinylidene androstane derivatives toward prostate cancer
Lipophilicity is a molecular parameter widely used in estimation of biological and environmental behavior of many substances (1-3).
Nonclinical and pharmacokinetic assessments to evaluate the potential of tedizolid and linezolid to affect mitochondrial function
Prolonged treatment with the oxazolidinone linezolid is associated with myelosuppression, lactic acidosis, and neuropathies, toxicities likely caused by impairment of mitochondrial protein synthesis (MPS). To evaluate the potential of the novel oxazolidinone tedizolid...
Predicting drug-drug interactions involving multiple mechanisms using physiologically based pharmacokinetic modeling: A case study with ruxolitinib
Physiologically based pharmacokinetic modeling was applied to characterize the potential drug–drug interactions for ruxolitinib.
MITOsym®: A Mechanistic, Mathematical Model of Hepatocellular Respiration and Bioenergetics
MITOsym, a new mathematical model of hepatocellular respiration and bioenergetics, has been developed in partnership with the DILIsym® model with the purpose of translating in vitro compound screening data...
Eslicarbazepine Acetate Monotherapy: A Population Ppharmacokinetic Analysis
Eslicarbazepine acetate (ESL) is a once-daily (QD) oral antiepileptic drug (AED), approved by the US Food and Drug Administration for the treatment of partial-onset seizures (POS) as monotherapy or…
Relationship between exposure and efficacy of eslicarbazepine acetate monotherapy
Eslicarbazepine acetate (ESL) is a once-daily, oral antiepileptic drug (AED), approved by the US Food and Drug Administration for the treatment of partialonset seizures (POS) as monotherapy or adjunctive...
Relationship Between Eslicarbazepine Exposure and Efficacy of Eslicarbazepine Acetate Adjunctive Therapy
Eslicarbazepine acetate (ESL; Aptiom®) is a novel once-daily (QD) oral antiepileptic drug, approved in then US, Canada and the EU as adjunctive treatment of partial-onset seizures (POS). ESL is extensively...
Relationship Between Eslicarbazepine Exposure and Safety Endpoints for Eslicarbazepine Acetate Adjunctive Therapy
Eslicarbazepine acetate (ESL) is a once-daily (QD) oral antiepileptic drug (AED), approved in the US, Canada and the EU as adjunctive treatment of partial-onset seizures (POS). After oral administration, ESL...
Relationship Between Eslicarbazepine Exposure and Safety Endpoints for Eslicarbazepine Acetate Monotherapy
In two Phase III trials (093-045 and -046) of eslicarbazepine acetate (ESL) monotherapy in patients with partial-onset seizures (POS) uncontrolled by 1−2 antiepileptic drugs (AEDs), the incidence of...