Pharmacokinetics and Absolute Bioavailability of Epristeride in Healthy Male Subjects

Physiologically Based Absorption Modeling for Amorphous Solid Dispersion Formulations

“…This 4-fold higher in vivo solubility was subsequently used in the human simulations, with the assumption that the higher in vivo solubility observed in dogs is representative of human in vivo solubility. It should be noted that compound C plasma concentration at 24 h postdose was unexpectedly high, but such observations have been reported previously . It is acknowledged that an increase in solubility due to better bile salt solubilization in vivo may not represent the only solution to obtaining an improved data fit.…”

5α-Reductase Inhibitors Do Not Prevent the Development and Progression of Urothelial Cancer: In Vitro Evidence

“…We first compared the cell proliferation of AR-positive bladder cancer lines cultured with various concentrations of dutasteride/finasteride/epristeride ( i.e. the highest doses greater than pharmacological concentrations –dutasteride 5.8 nM [27], finasteride 102 nM [28], or epristeride 373 nM [29]). MTT assay showed significant inhibition in the viability of UMUC3 (Fig.…”

Pharmacokinetics of darunavir in fixed‐dose combination with cobicistat compared with coadministration of darunavir and ritonavir as single agents in healthy volunteers

“…A similar phenomenon, however, is observed in the plasma concentration–time profile of epristeride, a 5α‐reductase inhibitor, when administered orally and intravenously. The investigators suggested that for epristeride, this may be due to enterohepatic recycling . Darunavir is metabolized mostly by CYP3A but does undergo glucuronidation as a minor pathway.…”