An updated patent review on P-glycoprotein inhibitors (2011-2018)

References

• Ayrton A, Morgan P. Role of transport proteins in drug absorption, distribution, and excretion. Xenobiotica. 2001;31:469–497.
   PubMed Web of Science ®Google Scholar
• Dean M, Rzhetsky A, Allikmets R. The human ATP-binding cassette (ABC) transporter superfamily. Genome Res. 2001;11:1156–1166.
   PubMed Web of Science ®Google Scholar
• Giacomini KM, Huang SM, Tweedie DJ, et al. Membrane transporters in drug development. Nat Rev Drug Discov. 2010;9:215–236.
   PubMed Web of Science ®Google Scholar
• Chang C, Bahadduri PM, Polli JE, et al. Rapid identification of P-glycoprotein substrates and inhibitors. Drug Metab Dispos. 2006;34:1976–1984.
   PubMed Web of Science ®Google Scholar
• Bankstahl JP, Kuntner C, Abrahim A, et al. Tariquidar-induced P-glycoprotein inhibition at the rat blood-brain barrier studied with (R)-11C-verapamil and PET. J Nucl Med. 2008;49:1328–1335.
   PubMed Web of Science ®Google Scholar
• Raaphorst RM, Windhorst AD, Elsinga PH, et al. Radiopharmaceuticals for assessing ABC transporters at the blood-brain barrier. Clin Pharmacol Ther. 2015;97:362–371.
   PubMed Web of Science ®Google Scholar
• Colabufo NA, Berardi F, Perrone MG, et al. Substrates, inhibitors and activators of P-glycoprotein: candidates for radiolabeling and imaging perspectives. Curr Top Med Chem. 2010;10:1703–1714.
   PubMed Web of Science ®Google Scholar
• Bauer M, Blaickner M, Philippe C, et al. Whole-Body Distribution and Radiation Dosimetry of 11C-Elacridar and 11C-Tariquidar in Humans. J Nucl Med. 2016;57:1265–1268.
   PubMed Web of Science ®Google Scholar
• Müllauer J, Karch R, Bankstahl JP, et al. Assessment of cerebral P-glycoprotein expression and function with PET by combined [11C]inhibitor and [11C]substrate scans in rats. Nucl Med Biol. 2013;407:755–763.
   Web of Science ®Google Scholar
• Muzi M, Mankoff DA, Link JM, et al. Imaging of cyclosporine inhibition of P-glycoprotein activity using 11C-verapamil in the brain: studies of healthy humans. J Nucl Med. 2009;50:1267–1275.
   PubMed Web of Science ®Google Scholar
• Loo TW, Clarke DM. Tariquidar inhibits P-glycoprotein drug efflux but activates ATPase activity by blocking transition to an open. Biochem Pharmacol. 2014;92:558–566.
   PubMed Web of Science ®Google Scholar
• van Waarde A, Ramakrishnan NK, Rybczynska AA, et al. Synthesis and preclinical evaluation of novel PET probes for P-glycoprotein function and expression. J Med Chem. 2009;52:4524–4532.
   PubMed Web of Science ®Google Scholar
• Kuntner C, Bankstahl JP, Bankstahl M, et al. Dose-response assessment of tariquidar and elacridar and regional quantification of P-glycoprotein inhibition at the rat blood-brain barrier using (R)-[(11)C]verapamil PET. Eur J Nucl Med Mol Imaging. 2010;37:942–953.
   PubMed Web of Science ®Google Scholar
• Kemper EM, Cleypool C, Boogerd W, et al. The influence of the P-glycoprotein inhibitor zosuquidar trihydrochloride (LY335979) on the brain penetration of paclitaxel in mice. Cancer Chemother Pharmacol. 2004;53:173–178.
   PubMed Web of Science ®Google Scholar
• Luurtsema G, Schuit RC, Klok RP, et al. Evaluation of [11C]laniquidar as a tracer of P-glycoprotein: radiosynthesis and biodistribution in rats. Nucl Med Biol. 2009;36:643–649.
   PubMed Web of Science ®Google Scholar
• Cantore M, Leopoldo M, Berardi F, et al. Design and synthesis of new selective P-gp. Curr Pharm Des. 2016;22:5774–5778.
   PubMed Web of Science ®Google Scholar
• Kim YK, Choi HY, Kim NH, et al. Reversine stimulates adipocyte differentiation and downregulates Akt and p70(s6k) signaling pathways in 3T3-L1 cells. Biochem Biophys Res Commun. 2007;358:553–558.
   PubMed Web of Science ®Google Scholar
• Gottesman MM, Fojo T, Bates SE. Multidrug resistance in cancer: role of ATP-dependent transporters. Nat Rev Cancer. 2002;2:48e58.
   Web of Science ®Google Scholar
• Robey R, Pluchino KM, Hall MD, et al. Revisiting the role of ABC transporters in multidrug-resistant cancer. Nat Rev Canc. 2018;18:452e464.
   Web of Science ®Google Scholar
• Wise JG, Vogel PD, Lippert AR, et al. Inhibitors of multidrug resistance transporter P-glycoprotein. US2018/0185366A1.
   Google Scholar
• Wise JG, Vogel PD, Brewer FK, et al., Inhibitors of multidrug resistance transporter P-glycoprotein. US2017/012844A1.
   Google Scholar
• Watanabe T, Maeda K, Nakai C, et al. Investigation of the effect of the uneven distribution of CYP3A4 and P-glycoprotein in the intestine on the barrier function against xenobiotics: a simulation study. J Pharm Sci. 2013;102:3196–3204.
   PubMed Web of Science ®Google Scholar
• Silva Pavia G Anti-tumor cocktail comprising an anti-tumor agent selective for tumor acidity, an antioxidant, and a P-glycoprotein inhibitor. WO2017/173509A1.
   Google Scholar
• Modi P Oral formulation of chemotherapeutic agents. US2015/0231069A.
   Google Scholar
• Capparelli E, Zinzi L, Cantore M, et al. SAR studies on tetrahydroisoquinoline derivatives: the role of flexibility and bioisosterism to raise potency and selectivity toward P-glycoprotein. J Med Chem. 2014;57:9983–9994.
   PubMed Web of Science ®Google Scholar
• Polli JW, Wring SA, Humphreys JE, et al. Rational use of in vitro P-glycoprotein assays in drug discovery. J Pharmacol Exp Ther. 2001;299:620–628.
   PubMed Web of Science ®Google Scholar
• Perrone MG, Inglese C, Berardi F, et al. Comparative evaluation of two dye probes in the rat everted gut sac model for unambiguous classification of P-gp substrate and inhibitor. J Pharmacol Toxicol Methods. 2013;67:5–8.
   PubMed Web of Science ®Google Scholar
• Karla PK Method of increasing the bioavailability of an HIV drug. US2016/0193237.
   Google Scholar
• Karla PK, Mangat HS Treating ocular disease with efflux transporter inhibitor. WO2015/060812A1.
   Google Scholar
• Karla PK, Mangat HS Method of treating an ocular disease and composition effective for treating an ocular disease. US2015/0352177A1.
   Google Scholar
• Bleier BS, Nocera A Secreted P-glycoprotein is a non invasive biomarker of chronic rhinosinusitis. WO2017/123933A1.
   Google Scholar
• Bleier BS Treatment of rhinosinusitis with P-glycoprotein inhibitor. US2017/0348384.
   Google Scholar
• Akhtar N, Ahad A, Khar RK, et al. The emerging role of P-glycoprotein inhibitors in drug delivery: a patent review. Expert Opin Ther Pat. 2011;21:561–576.
   PubMed Web of Science ®Google Scholar