Assessing Drug–Drug Interaction and Food Effect for BCS Class 2 Compound BI 730357 (Retinoic Acid-Related Orphan Receptor Gamma Antagonist, Bevurogant) Using a Physiology-Based Pharmacokinetics Modeling (PBPK) Approach with Semi-Mechanistic Absorption

This study, published in the special issue of MDPI Pharmaceutics: Advances in Pharmacokinetics and Drug Interactions, explored drug-drug interactions (DDIs) and food effects for Bevurogant (BI 730357), a competitive antagonist of the retinoic acid-related orphan receptor γ (RORγ), investigated as an oral treatment for plaque psoriasis.

The publication was co-authored by Dr. Tobias Kanacher, Assoc. Prof Dr. Erik Sjögren, and Dr. Elodie Plan, in collaboration with Dr. Ibrahim Ince (Head of PBPK working group, Senior Principal Scientist in Pharmacometrics) and colleagues at Boehringer Ingelheim. Medical writing by provided by Dr. Annika Eklund, Pharmetheus.

• Illustrates how applying empirical functions to describe in vivo formulation kinetics—aligned with clinical data—can bridge gaps in mechanistic understanding and enable predictions across a range of clinical scenarios and tested doses.
• Serves as a case example of using PK-Sim® to evaluate clinical DDIs in a BCS Class II compound, characterized by complex absorption, sub-proportional dose-exposure, pH-dependent low solubility, and a late-phase absorption peak.
• Highlights the role of physiologically based pharmacokinetics (PBPK) and physiologically based biopharmaceutics modeling (PBBM) in supporting drug development.

Find the full publication here (open source)