Quizartinib is an FMS-like tyrosine kinase 3 (FLT3) inhibitor that has shown robust clinical activity in patients with FLT3-internal tandem duplication-mutated relapsed/refractory acute myeloid leukemia (AML).
Cumulative Fraction of Response for Once- and Twice-Daily Delamanid in Patients with Pulmonary Multidrug-Resistant Tuberculosis
Pharmacokinetic (PK) and pharmacodynamic (PD) analyses were conducted to determine the cumulative fraction of response (CFR) for 100 mg twice-daily (BID)
Reliance: a smarter way of regulating medical products – The IPRP survey
A survey was conducted among national regulatory authorities' members of the International Pharmaceutical Regulators Programme (IPRP) to collect and share experiences of reliance approaches.
Effect of QTC-4-MeOBnE Treatment on Memory, Neurodegeneration, and Neurogenesis in a Streptozotocin-Induced Mouse Model of Alzheimer’s Disease
Growing evidence suggests that drugs targeting neurogenesis and myelinization could be novel therapeutic targets against Alzheimer’s disease (AD).
Modulating target engagement of small molecules via drug delivery: approaches and applications in drug discovery and development
Drug-delivery technologies for modified drug release have been in existence for decades, but their utilization has been largely limited..
Insights of Tris(2-pyridylmethyl)amine as anti-tumor agent for osteosarcoma: experimental and in silico studies
Osteosarcoma (OS) is a malignant bone tumor and its occurrence is associated with high levels of microRNAs (miRNAs) and critical protein involved on intracellular signaling pathways.
The Intestinal Efflux Transporter Inhibition Activity of Xanthones from Mangosteen Pericarp: An In Silico, In Vitro and Ex Vivo Approach
The capacity of α-mangostin (α-MG) and β-mangostin (β-MG) from mangosteen pericarp on P-glycoprotein (Pgp) in silico, in vitro...
Proving the Mode of Action of Phytotoxic Phytochemicals
Knowledge of the mode of action of an allelochemical can be valuable for several reasons, such as proving and...
Computational evaluation of endocrine activity of biocidal active substances
Exposure to endocrine disrupting chemicals is an important public health concern although only a few endocrine disruption chemicals have been identified so far.
A Latent Variable Approach to Account for Correlated Inputs in Global Sensitivity
In pharmaceutical research and development decision-making related to drug candidate selection, efficacy and safety...
A latent variable approach to account for correlated inputs in global sensitivity analysis with cases from pharmacological systems modelling
In pharmaceutical research and development decision-making related to drug candidate selection...
BCS Class IV Oral Drugs and Absorption Windows: Regional-Dependent Intestinal Permeability of Furosemide
Biopharmaceutical classification system (BCS) class IV drugs (low-solubility low-permeability) are generally poor drug candidates, yet...
5-Fluorouracil Loaded Biogenic and Albumin Capped Gold Nanoparticles Using Bacterial Enzyme—In Vitro-In Silico Gastroplus® Simulation and Prediction
The study investigated in situ biosynthesis of albumin capped 5-fluorouracil (5-FU) loaded gold nanoparticles (NPs) using bacterial extract for enhanced...
Circulating tumor DNA analysis of metastatic renal cell carcinoma
The genomic landscape of metastatic renal cell carcinoma (RCC) is not well understood, and currently available data suggest that it is functionally distinct from that of localized...
Ocular Physiologically Based Pharmacokinetic Modeling for Ointment Formulations
The purpose of this study is to show how the Ocular Compartmental Absorption & Transit (OCAT™) model in GastroPlus® can be used to characterize ocular...
Public Workshop Summary Report on Fiscal Year 2021 Generic Drug Regulatory Science Initiatives: Data Analysis and Model‐Based Bioequivalence
On May 4, 2020, the US Food and Drug Administration (FDA) hosted an online public workshop titled “FY 2020 Generic Drug Regulatory Science...
In vitro investigation of metabolic fate of α-mangostin and gartanin via skin permeation by LC-MS/MS and in silico evaluation of the metabolites by ADMET predictor™
Mangosteen, Garciniam angostana L., is a juicy fruit commonly found in Thailand.
A Novel Eutectic-Based Transdermal Delivery System for Risperidone
This paper reports for the first time the possible formation of a novel room temperature therapeutic deep eutectic solvent (THEDES)...
Novel substituted N-benzyl(oxotriazinoindole) inhibitors of aldose reductase exploiting ALR2 unoccupied interactive pocket
Recently we have developed novel oxotriazinoindole inhibitors (OTIs) of aldose reductase (ALR2), characterized by high efficacy and selectivity.
Managing the challenge of drug-induced liver injury: a roadmap for the development and deployment of preclinical predictive models
Drug-induced liver injury (DILI) is a patient-specific, temporal, multifactorial pathophysiological process that cannot yet be recapitulated in a single in vitro model.