ArticleFrontiers in pharmacology2026
Regional absorption of talinolol mediated by intestinal transporters: insights from PBPK modeling analysis.
Article in Frontiers in pharmacology, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
Intestinal transporters play a pivotal role in oral absorption dynamics to shape the plasma or blood concentration-time curves of drugs, influencing interindividual pharmacokinetic (PK) variability and drug-drug or drug-food interactions. Plasma concentration-time profiles of several drugs, such as talinolol, bedaquiline, irbesartan, and amisulpride, exhibit dose-dependent dual or multiple absorption peaks, yet the mechanism underlying these phenomena remains elusive. It is hypothesized that the regional expression and interplay of intestinal transporters contribute to the observed dual peaks. To elucidate the mechanisms underlying these unique absorption phenomena, the concentration- and pH-dependent transport of talinolol, a substrate of intestinal transporter P-glycoprotein (P-gp) and organic anion transporting polypeptide (OATP) 2B1, was examined using Caco-2 cells, along with the development of a comprehensive physiologically-based pharmacokinetic (PBPK) model that includes a multi-layer gut wall within an advanced dissolution, absorption, and metabolism (M-ADAM) model built in SimBiology
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