A comprehensive mechanistic investigation of factors affecting intestinal absorption and bioavailability of two PROTACs in rats
In the rat, ARV-110 and ARV-471 were enzymatically degraded in the intestinal lumen and in plasma, and their intestinal permeability and systemic exposure seem to be reduced due to P-gp efflux.
Authors
- Thomas B. Borchardt
- Mirko Koziolek (ORCID: https://orcid.org/0000-0002-1385-182X)
- David Dahlgren (ORCID: https://orcid.org/0000-0002-5586-2906)
- Markus Sjöblom (ORCID: https://orcid.org/0000-0002-1406-9389)
- Mikael Hedeland (ORCID: https://orcid.org/0000-0001-8962-2815)
- Anura Indulkar
- Janis Niessen (ORCID: https://orcid.org/0000-0003-3703-0062)
- Ilse R. Dubbelboer (ORCID: https://orcid.org/0000-0002-7806-0447)
- Hans Lennernäs (ORCID: https://orcid.org/0000-0002-1578-5184)
- Nathalie Arendt
Institutions
- Uppsala University (SE)
- AbbVie (United States) (US)
- Klinikum Ludwigshafen (DE)
Publication Details
- Journal
- European Journal of Pharmaceutics and Biopharmaceutics
- Published
- 2025-04-12
- DOI
- https://doi.org/10.1016/j.ejpb.2025.114719
- Citations
- 6
- Primary Topic
- Protein Degradation and Inhibitors
- Type
- article
- Field-Weighted Citation Impact
- 4.84
Funders
- AbbVie