Title : P-Glycoprotein (MDR1/ABCB1) Restricts Brain Penetration of the Bruton's Tyrosine Kinase Inhibitor Ibrutinib, While Cytochrome P450-3A (CYP3A) Limits Its Oral Bioavailability.

Pub. Date : 2018 Nov 5

PMID : 30247919






6 Functional Relationships(s)
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1 P-Glycoprotein (MDR1/ABCB1) Restricts Brain Penetration of the Bruton"s Tyrosine Kinase Inhibitor Ibrutinib, While Cytochrome P450-3A (CYP3A) Limits Its Oral Bioavailability. ibrutinib Bruton agammaglobulinemia tyrosine kinase Mus musculus
2 Ibrutinib (Imbruvica), an oral tyrosine kinase inhibitor (TKI) approved for treatment of B-cell malignancies, irreversibly inhibits the Bruton"s tyrosine kinase (BTK). ibrutinib Bruton agammaglobulinemia tyrosine kinase Mus musculus
3 Ibrutinib (Imbruvica), an oral tyrosine kinase inhibitor (TKI) approved for treatment of B-cell malignancies, irreversibly inhibits the Bruton"s tyrosine kinase (BTK). ibrutinib Bruton agammaglobulinemia tyrosine kinase Mus musculus
4 Ibrutinib (Imbruvica), an oral tyrosine kinase inhibitor (TKI) approved for treatment of B-cell malignancies, irreversibly inhibits the Bruton"s tyrosine kinase (BTK). ibrutinib Bruton agammaglobulinemia tyrosine kinase Mus musculus
5 Ibrutinib (Imbruvica), an oral tyrosine kinase inhibitor (TKI) approved for treatment of B-cell malignancies, irreversibly inhibits the Bruton"s tyrosine kinase (BTK). ibrutinib Bruton agammaglobulinemia tyrosine kinase Mus musculus
6 Its abundant metabolite, dihydrodiol-ibrutinib (ibrutinib-DiOH), which is primarily formed by CYP3A, has a 10-fold reduced BTK inhibitory activity. ibrutinib Bruton agammaglobulinemia tyrosine kinase Mus musculus