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Updated: Dec 26, 2025

Expression, Solubilization, and Purification of Eukaryotic Borate Transporters
Published on: March 7, 2019
Organic anion transporting polypeptide 2B1 (OATP2B1), an expanded substrate profile, does it align with OATP2B1's
Dallas Bednarczyk1, Menaka V Sanghvi1
1Pharmacokinetic Sciences, Novartis Institutes of BioMedical Science, Cambridge, MA, USA.
This study identified novel organic anion transporting polypeptide (OATP) 2B1 substrates, including angiotensin II receptor blockers (ARBs). However, OATP2B1 has minimal impact on oral absorption and brain penetration of these substrates.
Area of Science:
- Pharmacology
- Drug Metabolism
- Biochemistry
Background:
- Organic anion transporting polypeptide (OATP) 2B1 plays a role in drug transport.
- Understanding OATP2B1 substrates is crucial for predicting drug absorption and brain penetration.
Purpose of the Study:
- To expand the known substrate landscape of OATP2B1.
- To investigate the impact of novel OATP2B1 substrates on intestinal absorption and brain penetration.
Main Methods:
- Cellular accumulation assays were used to identify OATP2B1 substrates.
- Inhibition, time dependence, and kinetic studies were performed on identified substrates.
Main Results:
- Angiotensin II receptor blockers (ARBs) were identified as OATP2B1 substrates.
- Balsalazide, olsalazine, and gavestinel were confirmed as novel OATP2B1 substrates.
- Aliskiren, erlotinib, montelukast, fexofenadine, and taurocholate were not confirmed as OATP2B1 substrates.
Conclusions:
- OATP2B1 has a limited impact on the oral absorption and brain penetration of its substrates.
- Current suggestions for including OATP2B1 assessment in drug approval processes may be premature.
- Further research with robust OATP2B1 substrates is needed.
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