Publications by authors named "Janine Wank"
Background: Setipiprant, a tetrahydropyridoindole derivative, is a CRTH2 (chemoattractant receptor-homologous molecule expressed on T-helper [Th]-2 cells) antagonist that has the potential to be effective in the treatment of patients with diseases with an allergic etiology, such as allergic rhinitis and asthma.
Objectives: This study investigated the disposition, metabolism, and elimination of setipiprant.
Study Design: In this open-label study, a single oral dose of 1,000 mg (14)C-labeled setipiprant was administered.
Article Synopsis
- Macitentan is a dual endothelin receptor antagonist in phase 3 trials for treating pulmonary arterial hypertension, and a study investigated its metabolism in six healthy male subjects after a single 10 mg oral dose.
- The study found that about 73.6% of the administered radioactive dose was recovered in urine and feces, with urine accounting for nearly 50% of the total recovery.
- Several metabolites were identified, including a pharmacologically active one called ACT-132577, with lower concentrations of radioactivity found in whole blood compared to plasma, suggesting poor binding to red blood cells.