Safety, tolerability, and pharmacokinetic evaluation of single- and multiple-ascending doses of a novel kappa opioid receptor antagonist LY2456302 and drug interaction with ethanol in healthy subjects

Safety, tolerability, and pharmacokinetic evaluation of single- and multiple-ascending doses of a novel kappa opioid receptor antagonist LY2456302 and drug interaction with ethanol in healthy subjects

Publication: Pharmacokinetics
Division: PBPK

Accumulating evidence indicates that selective antagonism of kappa opioid receptors may provide therapeutic benefit in the treatment of major depressive disorder, anxiety disorders, and substance use disorders.

Semi-mechanistic modelling of the analgesic effect of gabapentin in the formalin-induced rat model of experimental pain

Semi-mechanistic modelling of the analgesic effect of gabapentin in the formalin-induced rat model of experimental pain

Publication: Pharm Res
Division: PBPK

The formalin-induced rat model of nociception involves moderate continuous pain. Formalin-induced pain results in a typical repetitive flinching behaviour, which displays a biphasic pattern characterised by peaks of pain.

Imidazole aldoximes effective in assisting butyrylcholinesterase catalysis of organophosphate detoxification

Imidazole aldoximes effective in assisting butyrylcholinesterase catalysis of organophosphate detoxification

Publication: J Med Chem
Software: ADMET Predictor®

Intoxication by organophosphate (OP) nerve agents and pesticides should be addressed by efficient, quickly deployable countermeasures such as antidotes reactivating acetylcholinesterase or scavenging the parent OP.

A mechanistic model of drug-induced liver injury AIDS the interpretation of elevated liver transaminase levels in a phase I clinical trial

A mechanistic model of drug-induced liver injury AIDS the interpretation of elevated liver transaminase levels in a phase I clinical trial

Publication: CPT Pharmacometrics Syst Pharmacol
Software: DILIsym®

Entolimod (CBLB502) is a Toll-like receptor 5 agonist in development as a single-dose countermeasure against total body irradiation.

Differential effects of methoxy group on the interaction of curcuminoids with two major ligand binding sites of human serum albumin

Differential effects of methoxy group on the interaction of curcuminoids with two major ligand binding sites of human serum albumin

Publication: PLoS One
Software: ADMET Predictor®

Curcuminoids are a group of compounds with a similar chemical backbone structure but containing different numbers of methoxy groups that have therapeutic potential due to...

Use of Preclinical Dog Studies and Absorption Modeling to Facilitate Late Stage Formulation Bridging for a BCS II Drug Candidate

Use of Preclinical Dog Studies and Absorption Modeling to Facilitate Late Stage Formulation Bridging for a BCS II Drug Candidate

Authors: Kesisoglou F
Publication: AAPS PharmSciTech
Software: GastroPlus®

Formulation changes are common during drug development either due to clinical or manufacturing considerations. These changes especially at later stages of drug development oftentimes raise questions...

Population Pharmacokinetic Evaluation of Eslicarbazepine Acetate for Adjunctive Therapy in Refractory Partial Onset Seizures

Population Pharmacokinetic Evaluation of Eslicarbazepine Acetate for Adjunctive Therapy in Refractory Partial Onset Seizures

Conference: ACCP

Eslicarbazepine acetate (ESL), a once-daily antiepileptic drug (AED), is converted to eslicarbazepine, the primary active metabolite of ESL, after oral administration. The population pharmacokinetics (PK)…

Design, Synthesis, and in vitro Testing of Novel COX-2/COX-1 Inhibitors

Design, Synthesis, and in vitro Testing of Novel COX-2/COX-1 Inhibitors

Division: PBPK

To design,synthesize,and test new lead molecules that inhibit both COX-1 and COX-2 forms of the cyclooxygenase (COX) enzyme, with higher affinity for COX-2 than for COX-1.