A naturally-occurring, orally bioavailable bisbenzylisoquinoline plant alkaloid with potential chemosensitization activity. MDR modulator CBT-1 binds to and inhibits the MDR efflux pump P-glycoprotein (P-gp), which may inhibit the efflux of various chemotherapeutic agents from tumor cells and reverse P-gp-mediated tumor cell MDR. P-gp is a transmembrane ATP-binding cassette (ABC) transporter and is overexpressed by some multidrug resistant tumors.
