BCRP

ABCG2, more commonly referred to as BCRP (Breast Cancer Resistance Protein), is an efflux transporter that serves two major drug transport functions. Firstly, it restricts the distribution of its substrates into organs such as the brain, testes, placenta, and across the gastrointestinal tract (GIT). Secondly, it eliminates its substrates from excretory organs, mediating both biliary and renal excretion, and occasionally direct gut secretion. Although less well studied than e.g. MDR1, BCRP is generally co-expressed with MDR1, and shares many of its substrates, inhibitors and inducers. Of its known substrates, rosuvastatin has been implicated in DDI, especially with perpetrator drugs that also inhibit OATPs (e.g. cyclosporine). It is probable that a synergy exists between the action of BCRP, MDR1, and the drug-metabolizing enzyme CYP3A4, particularly in the GIT. BCRP is included in the list of important drug transporters that both the FDA and EMA consider necessary to investigate regarding liabilities for NCEs. Drugs whose ADME, and bioavailability in particular, is influenced by BCRP may require clinical investigation to reveal a potential DDI with potent clinical BCRP inhibitors. For instance, since the GIT absorption of rosuvastatin is modulated by BCRP, it may be necessary to study the impact of BCRP inhibitors on the oral absorption of rosuvastatin. Because of the potential synergy between BCRP, CYP3A4, and MDR1, a clinical investigation examining the contribution of both drug transporters and enzymes to drug ADME may be necessary.

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  1. Elacridar (GF120918)

    Catalog No. A12324
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    P-gp & BCRP 抑制剂
    Elacridar (GF120918)是一种原型BCRP抑制剂,可抑制Bcrp1介导的转运。 了解更多
  2. Ko-143

    Catalog No. A11475
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    BCRP 抑制剂
    ko 143是有效的选择性乳腺癌耐药蛋白多药转运蛋白(bcrp)抑制剂,ec90值为26 nm。 了解更多
  3. KS-176

    Catalog No. A16195
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    BCRP 抑制剂
    KS-176是乳腺癌抗性蛋白(BCRP)多药转运蛋白的有效和选择性抑制剂(在Pheo A和Hoechst 33342分析中,IC50值分别为0.59和1.39 uM)。 了解更多
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    YHO-13177

    Catalog No. A17127
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    BCRP/ABCG2 抑制剂
    YHO-13177是一种有效且特异性的乳腺癌抗性蛋白(BCRP/ABCG2)抑制剂。 了解更多
  4. FD 12-9

    Catalog No. A18393
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    P-gp/BCRP dual 抑制剂
    FD 12-9 is a flavonoid dimer, acts as a dual inhibitor of P-gp and BCRP, with EC50s of 285 nM and 0.9 nM, respectively. Anti-glioblastoma activity. 了解更多

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