Interactions of Oral Molecular Excipients with Breast Cancer Resistance Protein, BCRP.

ABSTRACT: Mechanistic-understanding-based selection of excipients may improve formulation development strategies for generic drug products and potentially accelerate their approval. Our study aimed at investigating the effects of molecular excipients present in orally administered FDA-approved drug products on the intestinal efflux transporter, BCRP (ABCG2), which plays a critical role in drug absorption with potential implications on drug safety and efficacy. We determined the interactions of 136 oral molecular excipients with BCRP in isolated membrane vesicles and identified 26 excipients as BCRP inhibitors with IC₅₀ values less than 5 μM using ³H-cholecystokinin octapeptide (³H-CCK8). These BCRP inhibitors belonged to three functional categories of excipien

SUBMITTER: Zou L 

PROVIDER: S-EPMC8177814 | biostudies-literature | 2020 Mar

REPOSITORIES: biostudies-literature