BMS-663068 is a phosphonooxymethyl ester prodrug under development for the treatment of HIV/AIDS. The prodrug is designed to overcome the solubility-limited bioavailability of the active moiety, BMS-626529.
Application of Target-Mediated Drug Disposition Model to Small Molecule Heat Shock Protein 90 Inhibitors
Replacement of hydrogen with fluorine within three pairs of structurally similar small molecule inhibitors of heat shock protein 90 (HSP90) resulted in differences in inhibition constants (K(i)) in vitro as well...
In silico modeling to predict drug-induced phospholipidosis
Drug-induced phospholipidosis (DIPL) is a preclinical finding during pharmaceutical drug development that has implications on the course of drug development and regulatory safety review.
Simulations Plus Releases ADMET Predictor™ 6.5
Software Upgrade Increases Number of Predictive Models, Adds User Convenience Features
Get over it!
Brené Brown is a researcher at the University of Houston who studies vulnerability, courage, authenticity, and shame.* She speaks to many different audiences, including corporations and universities. Often, the person arranging a presentation timidly suggests that it might be better if she does not mention vulnerability or shame in her presentation. When asked what they want to hear about, the reply is “innovation, creativity, and change.” Her emphatic retort is that, “vulnerability is the birthplace of innovation, creativity and change!” To learn more, watch her second TEDTalk, Listening to Shame, here:
Reduction in Interindividual Variability and Clinical Significance Ratio in Covariate Assessment
Covariate analysis has become a customary and expected part of population pharmacokinetic (PK) and pharmacokinetic/ pharmacodynamic (PK/PD) modeling.1 The covariate submodel describes, explains, and…
Simulations Plus Software Used in Regulatory Submittals
US FDA, UK MHRA, and European EMA Accept Simulation Results in Applications
A Population PK Model for Cariprazine and the Metabolites
Cariprazine (CAR) is a potent dopamine D3/D2 receptor partial agonist with preferential binding to D3 receptors. Cariprazine was originally discovered by Gedeon Richter Plc. in Budapest, Hungary, and is…
Physiologically Based Pharmacokinetic (PBPK) Modeling of Amoxicillin in Neonates and Infants
An amoxicillin PBPK model was previously developed and validated in healthy adults as well as adults with altered renal function [1-2]. The purpose of this study was to explore the utility of the model in...
Single-Dose Safety, Tolerability, and Pharmacokinetics of the Antibiotic GSK1322322, a Novel Peptide Deformylase Inhibitor
GSK1322322 is a potent inhibitor of peptide deformylase, an essential bacterial enzyme required for protein maturation. GSK1322322 is active against community-acquired skin and respiratory...
Interaction of Silymarin Flavonolignans with Organic Anion-Transporting Polypeptides
Organic anion-transporting polypeptides (OATPs) are multispecific transporters mediating the uptake of endogenous compounds and xenobiotics in tissues that are important for drug...
Simulations Plus Announces Quarterly Cash Dividend Increase
Company declares increased cash dividend of $0.03 per share
The Role of Paracellular and Carrier-Mediated Pathways in the Nonlinear Absorption of BCS Class III Substrates for Influx and Efflux Transporters
Mechanistic oral absorption simulation of nonlinear dose dependence for BCS Class III transporter substrates is an important objective in preclinical development of NCEs as well as in generic formulation…
How a tax begat bebop.
During World War 2, a federal excise tax was imposed on supper clubs to raise funds from their wealthy patrons. According to Eric Felton in The Wall Street Journal, this so-called cabaret tax imposed a 30% tax at venues that featured dancing to a live band and served food. Clubs that provided instrumental music with no dancing were exempt. Within 5 years, the big band sound was dead, replaced by “a new and undanceable jazz performed primarily by small instrumental groups – bebop. . ..” The cabaret tax was finally eliminated in 1965, but by then the rock-and-roll revolution was well underway.
Clinical Pharmacokinetics of Buffered Propranolol Sublingual Tablet (Promptol™)—Application of a New “Physiologically Based” Model to Assess Absorption and Disposition
Sublingual administration of certain buffered propranolol may improve the rate and extent of absorption compared to oral administration.
Docking and in silico ADMET studies of noraristeromycin, curcumin and its derivatives with Plasmodium falciparum SAH hydrolase: A molecular drug target against malaria
The Plasmodium falciparum S-adenosyl-L-homocysteine hydrolase (pfSAHH) enzyme has been considered as a potential chemotherapeutic target against malaria due to the amino acid differences...
Computational Exploration of the Role of a Prototypical Damage-Associated Molecular Pattern (DAMP) Molecule in Acetaminophen Hepatotoxicity
Drug-induced liver injury (DILI) is a major source of acute liver failure and is one of the leading causes of drug development failures. As such, there remains an important unmet need for earlier...
Simulations Plus Reports Second Quarter and First Six Months FY2013 Financial Results
Second quarter net sales increase 11.8%; net income up 26.5%
Simulations Plus Sets Date for 2nd Quarter 2013 Earnings Release and Conference Call
Conference Call to be on Wednesday, April 10, at 4:30 PM ET