HM 30181A

PET scans with the Pgp substrate (R)-[¹¹C]NSC 657799 in FVB wild-type mice pretreated i.v. with Encequidar (HM30181) (10 or 21 mg/kg) failes to show significant increases in (R)-[¹¹C]NSC 657799 brain uptake compared with vehicle treated animals^[1]. Encequidar (HM30181) inhibits P-gp mainly in the intestinal endothelium, which can be beneficial because pan-inhibition of P-gp, particularly in the brain, could lead to detrimental adverse events. Encequidar (HM30181) increases the oral bioavailability of co-administered NSC 125973 by more than 12 times in rats^[2].