ATP-binding cassette transporter inhibitor potency and substrate drug affinity are critical determinants of successful drug delivery enhancement to the brain
This work shows that elacridar is an effective pharmacokinetic-enhancer for the brain delivery of ABCB1 and weaker ABCG2 substrate drugs when a plasma concentration of 1200 nM is exceeded.
Authors
- Amber Meurs (ORCID: https://orcid.org/0000-0003-1271-9154)
- Ceren H. Çitirikkaya
- Stefanie Zuidema
- Olaf van Tellingen (ORCID: https://orcid.org/0000-0002-1037-6269)
- Mark C. de Gooijer (ORCID: https://orcid.org/0000-0002-2812-991X)
- Aristeidis Lentzas
- Jos H. Beijnen (ORCID: https://orcid.org/0000-0003-0118-561X)
- Nikkie Venekamp
Institutions
- Utrecht University (NL)
- University of Manchester (GB)
- The Netherlands Cancer Institute (NL)
- Oncode Institute (NL)
- The Christie NHS Foundation Trust (GB)
Publication Details
- Journal
- Fluids and Barriers of the CNS
- Published
- 2024-08-05
- DOI
- https://doi.org/10.1186/s12987-024-00562-4
- Citations
- 6
- Primary Topic
- Drug Transport and Resistance Mechanisms
- Type
- article
- Field-Weighted Citation Impact
- 1.70