{"id":3028,"date":"2026-08-22T21:12:54","date_gmt":"2026-08-22T20:12:54","guid":{"rendered":"https:\/\/seamlessbio.de\/?page_id=3028"},"modified":"2026-08-23T00:19:29","modified_gmt":"2026-08-22T23:19:29","slug":"what-is-bcrp-abcg2","status":"publish","type":"page","link":"https:\/\/seamlessbio.de\/de\/what-is-bcrp-abcg2\/","title":{"rendered":"What is BCRP (ABCG2)?"},"content":{"rendered":"\t\t
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Quick Definition<\/p>\n

What is BCRP (Breast Cancer Resistance Protein \/ ABCG2)?:<\/strong> BCRP (Breast Cancer Resistance Protein), encoded by the ABCG2 gene, is an ABC efflux half-transporter expressed at the intestinal epithelium, blood-brain barrier, liver, kidney, and placenta. It limits oral bioavailability, restricts CNS penetration, and confers multidrug resistance in cancer. Along with P-gp, BCRP is one of two mandatory DDI transporter targets for all NMEs under FDA, EMA, and ICH M12 guidance.<\/p>\n<\/div>\n

BCRP vs P-gp \u2014 key differences<\/h2>\n

BCRP and P-gp share overlapping but distinct substrate profiles. Several drugs are substrates of both (topotecan, imatinib, gefitinib) \u2014 additive efflux limitation at the intestinal barrier. Clinical co-administration of dual BCRP\/P-gp inhibitors causes the largest DDI effects due to simultaneous inhibition of both pathways.<\/p>\n

In vitro BCRP assessment<\/h2>\n

Substrate: cell-based bidirectional transport (MDCKII-BCRP) \u2014 preferred for low-permeability compounds. Inhibitor IC50: vesicular transport assay with HEK293-BCRP inside-out vesicles \u2014 preferred for high-permeability compounds where cell-based efflux ratio is compressed.<\/p>\n

Key Facts<\/h2>\n