The Poorly Membrane Permeable Antipsychotic Drugs Amisulpride and Sulpiride Are Substrates of the Organic Cation Transporters from the SLC22 Family

The Poorly Membrane Permeable Antipsychotic Drugs Amisulpride and Sulpiride Are Substrates of the Organic Cation Transporters from the SLC22 Family

Publication: AAPS J
Software: ADMET Predictor®

Variations in influx transport at the blood-brain barrier might affect the concentration of psychotropic drugs at their site of action and as a consequence might alter therapy response.

Systems pharmacology modeling predicts delayed presentation and species differences in bile acid-mediated troglitazone hepatotoxicity.

Systems pharmacology modeling predicts delayed presentation and species differences in bile acid-mediated troglitazone hepatotoxicity.

Publication: Clin Pharmacol Ther
Software: DILIsym®

Troglitazone (TGZ) causes delayed, life-threatening drug-induced liver injury in some patients but was not hepatotoxic in rats.

Improving genetic programming for the prediction of pharmacokinetic parameters

Improving genetic programming for the prediction of pharmacokinetic parameters

Authors: Vanneschi L
Publication: Memetic Computing
Software: ADMET Predictor®

The prediction of pharmacokinetic parameters is a crucial phase of the drug discovery process, and the automatization of this task is a hot topic in computational bio-medicine.

Development of nanocrystal formulation of meloxicam with improved dissolution and pharmacokinetic behaviors

Development of nanocrystal formulation of meloxicam with improved dissolution and pharmacokinetic behaviors

Publication: Int J Pharm
Software: GastroPlus®

The present study aimed to develop nanocrystal formulations of meloxicam (MEL) in order to enhance its biopharmaceutical properties and provide a rapid onset of action. Nanocrystal formulations were...

Systems Pharmacology Modeling Predicts Hepatotoxic Potential Of Troglitazone And Pioglitazone

Systems Pharmacology Modeling Predicts Hepatotoxic Potential Of Troglitazone And Pioglitazone

Conference: ISSX
Software: DILIsym®

Troglitazone (TGZ) caused life-threatening drug-induced liver injury (DILI) in diabetic patients, whereas the next in class, pioglitazone (PGZ), has rarely been associated with DILI. Inhibition of bile acid...

Synthesis of a novel universal opioid receptor agonist with the 1,3,5-trioxazatriquinane skeleton and its pharmacologies

Synthesis of a novel universal opioid receptor agonist with the 1,3,5-trioxazatriquinane skeleton and its pharmacologies

Publication: Bioorg Med Chem
Software: ADMET Predictor®

We designed and synthesized of 1,3,5-trioxazatriquinanes with o- or p-hydroxyphenyl rings as analogs of the κ opioid receptor agonist SYK-146 with m-hydroxyphenyl groups.

Biopharmaceutical profiling of new antitumor pyrazole derivatives

Biopharmaceutical profiling of new antitumor pyrazole derivatives

Publication: Molecules
Software: GastroPlus®

Several new pyrazole derivatives have demonstrated promising antiproliferative and cytotoxic effects, but their poor solubility raised concerns over possible biopharmaceutical limitations.

History of Pharma of the Future

History of Pharma of the Future

Pharmacometric modeling and simulation has moved from its infancy as a novel way of approaching the analysis of clinical pharmacokinetic data to become an invaluable tool in pharmaceutical and biotechnology research and development.

Pazopanib as third line therapy for metastatic renal cell carcinoma: clinical efficacy and temporal analysis of cytokine profile

Pazopanib as third line therapy for metastatic renal cell carcinoma: clinical efficacy and temporal analysis of cytokine profile

Publication: J Urol

Purpose: Pazopanib has been assessed primarily in cytokine refractory or treatment naïve patients with metastatic renal cell carcinoma. Outcomes have been associated...

Model-Based Bioequivalence assessment of a commercial Azithromycin Capsule against Pfizer Zithromax® Tablet marketed in Jamaica

Model-Based Bioequivalence assessment of a commercial Azithromycin Capsule against Pfizer Zithromax® Tablet marketed in Jamaica

Publication: J Appl Pharm Sci
Software: GastroPlus®

Clinical evidence indicated that effective substitution of azithromycin capsule with a tablet dosage form should be based on evidence of providing equivalent in vivo AUC/MIC ratio at the site of infection.

Isoxazolotacrines as non-toxic and selective butyrylcholinesterase inhibitors for Alzheimer’s disease

Isoxazolotacrines as non-toxic and selective butyrylcholinesterase inhibitors for Alzheimer’s disease

Publication: Future Med Chem
Software: ADMET Predictor®

Owing to the complex nature of Alzheimer's disease, there is a renewed and growing search for multitarget non-toxictacrines as simple, easily available drugs in order to stop the progress and development of the disease.

PEGylated cyclodextrins as novel siRNA nanosystems: Correlations between polyethylene glycol length and nanoparticle stability

PEGylated cyclodextrins as novel siRNA nanosystems: Correlations between polyethylene glycol length and nanoparticle stability

Publication: Int J Pharm
Software: GastroPlus®

Silencing disease-related genes in the central nervous system (CNS) using short interfering RNA (siRNA) holds great promise for treating neurological disorders.

In vitro – in silico – in vivo drug absorption model development based on mechanistic gastrointestinal simulation and artificial neural networks: Nifedipine osmotic release tablets case study

In vitro – in silico – in vivo drug absorption model development based on mechanistic gastrointestinal simulation and artificial neural networks: Nifedipine osmotic release tablets case study

Publication: Eur J Pharm Sci
Software: GastroPlus®

In vitro--in vivo correlations (IVIVC) are generally accepted as a valuable tool in modified release formulation development aimed at (i) quantifying the in vivo drug delivery profile and...