Cellular Pharmacokinetic Aspects of Reversal Effect of Itraconazole on P-Glycoprotein-Mediated Resistance of Anticancer Drugs.

Repurposing itraconazole as an anticancer agent

“…In the 1990s, itraconazole was demonstrated to reverse chemoresistance in cancer cells overexpressing P-gp ( Fig. 1; Table I) (4)(5)(6). In addition, the human breast cancer resistance protein is also inhibited by itraconazole (7).…”

Has the era of individualised medicine arrived for antifungals? A review of antifungal pharmacogenomics

“…178 Voriconazole Substrate for CYP2C19, CYP 3A4, CYP2C9. 73 Inhibitor of CYP2C9, CYP2C19, CYP3A4 and CYP2B6.…”

Effect of Efflux Inhibition on Brain Uptake of Itraconazole in Mice Infected withCryptococcus neoformans

“…Miyama et al (1998) described similar results in rats by showing that coadministration of the P-gp inhibitors ketoconazole or verapamil increased cerebral concentrations of ITC without affecting plasma levels. In vitro data only reported ITC as a P-gp inhibitor on the accumulation of vinblastine or vincristine in mouse brain capillary endothelial MBEC4 cells (Miyama et al, 1998) and of vinblastine, daunorubicin, and doxorubicin into porcine kidney epithelial LLC-PK1 cells (Takara et al, 1999). But no in vitro information is available for ITC as a P-gp substrate.…”