Publications by authors named "Emma A Hughes"
Metabolism and pharmacokinetics characterization of metarrestin in multiple species.
Cancer Chemother Pharmacol
April 2020
Purpose: Metarrestin is a first-in-class pyrrolo-pyrimidine-derived small molecule targeting a marker of genome organization associated with metastasis and is currently in preclinical development as an anti-cancer agent. Here, we report the in vitro ADME characteristics and in vivo pharmacokinetic behavior of metarrestin.
Methods: Solubility, permeability, and efflux ratio as well as in vitro metabolism of metarrestin in hepatocytes, liver microsomes and S9 fractions, recombinant cytochrome P450 (CYP) enzymes, and potential for CYP inhibition were evaluated.
Article Synopsis
- Metarrestin is a new small molecule that targets the perinucleolar compartment, specifically designed for treating metastatic cancer cells, and this study assesses its pharmacokinetic properties and how it affects cancer-related biological markers.
- The study involved administering different doses of metarrestin to mice with pancreatic tumors, revealing it has a good oral bioavailability and demonstrates significant tissue concentration in tumors, suggesting effective drug delivery.
- Results indicated that metarrestin achieves high levels in tumor tissues, with a strong correlation between dosage and drug concentration, alongside a favorable influence on certain mRNA expressions related to tumor biology.