P-glycoprotein inhibitors

Ekins S, Kim RB, Leake BE, Dantzig AH, Schuetz E, Lan LB, et al. Application of three dimensional quantitative structure-activity relationships of P-glycoprotein inhibitors and substrates. Mol Pharmacol 2002 61 974-981. 

Schwarz, U. I., Gramatte, T., Krappweis, J., Oertel, R., Kirch, W., P-glycoprotein inhibitor erythromycin increases oral bioavailability of talinolol in humans, Int. J. Clin. Pharmacol. Ther. 2000, 38, 161-167. 

Kruijtzer, C.M., Beijnen, J.H., Rosing, H., ten Bokkel Huinink, W.W., Schot, M., Jewell, R.C., Paul, E.M. and Schellens, J. H. (2002) Increased oral bioavailability of topotecan in combination with the breast cancer resistance protein and P-glycoprotein inhibitor GF120918. Journal of Clinical Oncology, 20, 2943-2950. 

Bisi, A., Gobbi, S., Rampa, A., Belluti, F., Piazzi, L., Valenti, P., Gyemant, N. and Molnar, J. (2006) New potent P-glycoprotein inhibitors carrying a polycyclic scaffold. Journal of Medicinal Chemistry, 49, 3049-3051. 

Ferlini C, Distefano M, Pignatelli F, et al. Antitumour activity of novel taxanes that act at the same time as cytotoxic agents and P-glycoprotein inhibitors. BrJ Cancer 2000 83(12) 1762-1768. 

Because digitoxin is a substrate for p-glycoprotein, inhibitors of this transporter, such as atorvastatin, will increase drug levels and potentially cause toxicity. There have also been suggestions that the target receptor Na+/K+ ATPase shows variability between individuals. 

Varma, M.V., et al. 2003. P-glycoprotein inhibitors and their screening A perspective from bioavailability enhancement. Pharmacol Res 48 347. 

Woo, J.S., et al. 2003. Enhanced oral bioavailability of paclitaxel by coadministration of the P-glycoprotein inhibitor KR30031. Pharm Res 20 24. 

Bardelmeijer, H.A., et al. 2004. Efficacy of novel P-glycoprotein inhibitors to increase the oral uptake of paclitaxel in mice. Invest New Drugs 22 219. 

Yang, S., et al. 2004. Enhanced oral absorption of paclitaxel in a novel self-microemulsifying drug delivery system with or without concomitant use of P-glycoprotein inhibitors. Pharm Res 21 261. 

Kemper, E.M., et al. 2004. The influence of the P-glycoprotein inhibitor zosuquidar trihydrochloride (LY335979) on the brain penetration of paclitaxel in mice. Cancer Chemother Pharmacol 53 173. 

Breedveld P, Pluim D, Cipriani G, et al. The effect of Bcrpl (Abcg2) on the in vivo pharmacokinetics and brain penetration of imatinib mesylate (Gleevec) implications for the use of breast cancer resistance protein and P-glycoprotein inhibitors to enable the brain penetration of imatinib in patients. Cancer Res 2005 65 2577-2582. 

Lum BL, Gosland MP. MDR expression in normal tissues. Pharmacologic implications for the clinical use of P-glycoprotein inhibitors. Hematol Oncol Clin North Am 1995 9(2) 319-336. 

Wang Q, Yang H, Miller DW, et al. Effect of the p-glycoprotein inhibitor, cyclosporin A, on the distribution of rhodamine-123 to the brain an in vivo microdialysis study in freely moving rats. Biochem Biophys Res Commun 1995 211(3) 719-726. 

Theis JG, Chan HS, Greenberg ML, et al. Increased systemic toxicity of sarcoma chemotherapy due to combination with the P-glycoprotein inhibitor cyclosporin. Int J Clin Pharmacol Ther 1998 36(2) 61-64. 

New 4-aryl-1,4-dihydropyridines and 4-arylpyridines as P-glycoprotein inhibitors. Drug Metab Dispos 33 321-328... 

Voigt B, Coburger C, Monar J, Andreas H (2007) Structure-activity relationships of novel W-acyloxy-1,4-dihydropyridines as P-glycoprotein inhibitors. Biorg Med Chem 15 5110-5120... 

Gmol, D. J. Bernd, J. Phippard, A. E. Ojima, I. Bernacki, R. J. The use of a novel taxane-base p-glycoprotein inhibitor to identifiy mutations that alter the interaction of the protein with paclitaxel. Mol. Pharmacol., 2001, 60 104—113. 

EndoT, KImura O, and Sakata M. Effects of P-glycoprotein inhibitors on cadmium accumulation in cultured renal epithelial cells, LLC-PKl, and OK.Toxicol AppI Pharmacol 185 166-171,2002. 

Desrayaud S, Guntz P, Scherrmann JM, Lemaire M. 1997. Effect of the P-glycoprotein inhibitor, SDZ PSC 833, on the blood and brain pharmacokinetics of colchicine. Life Sci. 61 153-63... 

Letrent SP, Pollack GM, Brouwer KR, Brouwer KLR. 1999. Effects of a potent and specific P-glycoprotein inhibitor on the blood-brain barrier distribution and antinociceptive effect of morphin in the rat. DrugMetab. Dispos. 27(7) 827-34... 

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