Biricodar

Biricodar (VX-710, Incel) is a clinically applicable modulator of P-glycoprotein (Pgp) with potential chemosensitizing activity. Biricodar blood concentration at the time of mitoxantrone administration averaged 4.52 microg/ml. In 8226/Dox6 cells (Pgp), Biricodar (VX-710) increased mitoxantrone and daunorubicin uptake by 55 and 100%, respectively, increased their retention by 100 and 60%, respectively, and increased their cytotoxicity 3.1- and 6.9-fold, respectively. Biricodar (VX-710) modulates Pgp, MRP-1, and BCRP(R482), and has potential as a clinical broad-spectrum MDR modulator in malignancies such as the acute leukemias in which these proteins are expressed.