The third-generation P-glycoprotein inhibitor tariquidar may overcome bacterial multidrug resistance by increasing intracellular drug concentration

Journal of Antimicrobial Chemotherapy

Volumn 66, Issue 4, 2011, Pages 834-839

  Leitner, I ^a   Nemeth, J ^a   Feurstein, T ^a   Abrahim, A ^a   Matzneller, P ^a   Lagler, H ^a   Erker, T ^b   Langer, O ^a,c   Zeitlinger, M ^a  

^a MEDICAL UNIVERSITY OF VIENNA   (Austria)

^b UNIVERSITY OF VIENNA   (Austria)

^c AIT AUSTRIAN INSTITUTE OF TECHNOLOGY   (Austria)

Author keywords

ABC; Ciprofloxacin; Efflux pump inhibitors; MDR

Indexed keywords

CIPROFLOXACIN; ELACRIDAR; GLYCOPROTEIN P; TARIQUIDAR;

ANTIBIOTIC RESISTANCE; ANTIBIOTIC SENSITIVITY; ARTICLE; BACTERIAL CELL; BACTERIAL STRAIN; CONTROLLED STUDY; DRUG EFFECT; DRUG POTENCY; MINIMUM INHIBITORY CONCENTRATION; MULTIDRUG RESISTANCE; NONHUMAN; PHARMACODYNAMICS; PSEUDOMONAS AERUGINOSA; STAPHYLOCOCCUS AUREUS; STENOTROPHOMONAS MALTOPHILIA;

ANTI-BACTERIAL AGENTS; DRUG RESISTANCE, MULTIPLE, BACTERIAL; ENZYME INHIBITORS; MICROBIAL SENSITIVITY TESTS; MICROBIAL VIABILITY; P-GLYCOPROTEIN; PSEUDOMONAS AERUGINOSA; QUINOLINES; STAPHYLOCOCCUS AUREUS; STENOTROPHOMONAS MALTOPHILIA; TIME FACTORS;

EID: 79952802131     PISSN: 03057453     EISSN: 14602091     Source Type: Journal    
DOI: 10.1093/jac/dkq526     Document Type: Article

References (37)

1. Poole K. Efflux-mediated antimicrobial resistance. J Antimicrob Chemother 2005; 56: 20-51.
2. Normark BH, Normark S. Evolution and spread of antibiotic resistance. J Intern Med 2002; 252: 91-106.
3. Gibbons S, Oluwatuyi M, Kaatz GW. A novel inhibitor of multidrug efflux pumps in Staphylococcus aureus. J Antimicrob Chemother 2003; 51: 13-7.
4. Levy SB, Marshall B. Antibacterial resistance worldwide: causes, challenges and responses. Nat Med 2004; 10: S122-9.
5. Huet AA, Raygada JL, Mendiratta K et al. Multidrug efflux pump overexpression in Staphylococcus aureus after single and multiple in vitro exposures to biocides and dyes. Microbiology 2008; 154: 3144-53.
6. Escribano I, Rodriguez JC, Llorca B et al. Importance of the efflux pump systems in the resistance of Mycobacterium tuberculosis to fluoroquinolones and linezolid. Chemotherapy 2007; 53: 397-401.
7. Lomovskaya O, Bostian KA. Practical applications and feasibility of efflux pump inhibitors in the clinic-a vision for applied use. Biochem Pharmacol 2006; 71: 910-8.
8. Lomovskaya O, Zgurskaya HI, Totrov M et al. Waltzing transporters and 'the dance macabre' between humans and bacteria. Nat Rev Drug Discov 2007; 6: 56-65.
9. Amaral L, Engi H, Viveiros M et al. Review. Comparison of multidrug resistant efflux pumps of cancer and bacterial cells with respect to the same inhibitory agents. In Vivo 2007; 21: 237-44.
10. Markham PN, Westhaus E, Klyachko K et al. Multiple novel inhibitors of the NorA multidrug transporter of Staphylococcus aureus. Antimicrob Agents Chemother 1999; 43: 2404-8.
11. Markham PN. Inhibition of the emergence of ciprofloxacin resistance in Streptococcus pneumoniae by the multidrug efflux inhibitor reserpine. Antimicrob Agents Chemother 1999; 43: 988-9.
12. Renau TE, Leger R, Flamme EM et al. Inhibitors of efflux pumps in Pseudomonas aeruginosa potentiate the activity of the fluoroquinolone antibacterial levofloxacin. J Med Chem 1999; 42: 4928-31.
13. Van Bambeke F, Pages JM, Lee VJ. Inhibitors of bacterial efflux pumps as adjuvants in antibiotic treatments and diagnostic tools for detection of resistance by efflux. Recent Pat Antiinfect Drug Discov 2006; 1: 157-75.
14. Fox E, Bates SE. Tariquidar (XR9576): a P-glycoprotein drug efflux pump inhibitor. Expert Rev Anticancer Ther 2007; 7: 447-59.
15. Malingre MM, Beijnen JH, Rosing H et al. Co-administration of GF120918 significantly increases the systemic exposure to oral paclitaxel in cancer patients. Br J Cancer 2001; 84: 42-7.
16. Kuppens IE, Witteveen EO, Jewell RC et al. A phase I, randomized, open-label, parallel-cohort, dose-finding study of elacridar (GF120918) and oral topotecan in cancer patients. Clin Cancer Res 2007; 13: 3276-85.
17. Pusztai L, Wagner P, Ibrahim N et al. Phase II study of tariquidar, a selective P-glycoprotein inhibitor, in patients with chemotherapyresistant, advanced breast carcinoma. Cancer 2005; 104: 682-91.
18. Raguz S, Yague E. Resistance to chemotherapy: new treatments and novel insights into an old problem. Br J Cancer 2008; 99: 387-91.
19. Alonso A, Martinez JL. Multiple antibiotic resistance in Stenotrophomonas maltophilia. Antimicrob Agents Chemother 1997; 41: 1140-2.
20. Alonso A, Martinez JL. Cloning and characterization of SmeDEF, a novel multidrug efflux pump from Stenotrophomonas maltophilia. Antimicrob Agents Chemother 2000; 44: 3079-86.
21. Mahamoud A, Chevalier J, Alibert-Franco S et al. Antibiotic efflux pumps in Gram-negative bacteria: the inhibitor response strategy. J Antimicrob Chemother 2007; 59: 1223-9.
22. Muller M, Brunner M, Hollenstein U et al. Penetration of ciprofloxacin into the interstitial space of inflamed foot lesions in non-insulindependent diabetes mellitus patients. Antimicrob Agents Chemother 1999; 43: 2056-8.
23. de Lange EC, Marchand S, van den Berg D et al. In vitro and in vivo investigations on fluoroquinolones: effects of the P-glycoprotein efflux transporter on brain distribution of sparfloxacin. Eur J Pharm Sci 2000; 12: 85-93.
24. Kaatz GW, Moudgal VV, Seo SM. Identification and characterization of a novel efflux-related multidrug resistance phenotype in Staphylococcus aureus. J Antimicrob Chemother 2002; 50: 833-8.
25. Abraham J, Edgerly M, Wilson R et al. A phase I study of the P-glycoprotein antagonist tariquidar in combination with vinorelbine. Clin Cancer Res 2009; 15: 3574-82.
26. Wong HL, Bendayan R, Rauth AM et al. Simultaneous delivery of doxorubicin and GG918 (elacridar) by new polymer-lipid hybrid nanoparticles (PLN) for enhanced treatment of multidrug-resistant breast cancer. J Control Release 2006; 116: 275-84.
27. 11C-verapamil and PET. J Nucl Med 2009; 50: 1954-61.
28. 11C-N-desmethyl-loperamide. J Nucl Med 2010; 51: 559-66.
29. Kuppens IE, Breedveld P, Beijnen JH et al. Modulation of oral drug bioavailability: from preclinical mechanism to therapeutic application. Cancer Invest 2005; 23: 443-64.
30. Kuhnle M, Egger M, Muller C et al. Potent and selective inhibitors of breast cancer resistance protein (ABCG2) derived from the P-glycoprotein (ABCB1) modulator tariquidar. J Med Chem 2009; 52: 1190-7.
31. Kiser TH, Obritsch MD, Jung R et al. Efflux pump contribution to multidrug resistance in clinical isolates of Pseudomonas aeruginosa. Pharmacotherapy 2010; 30: 632-8.
32. Gould IM, Milne K, Jason C. Concentration-dependent bacterial killing, adaptive resistance and post-antibiotic effect of ciprofloxacin alone and in combination with gentamicin. Drugs Exp Clin Res 1990; 16: 621-8.
33. Joyanes P, Pascual A, Gimenez MJ et al. Differences between two new quinolones (gemifloxacin and trovafloxacin) and ciprofloxacin in their concentration-dependent killing of Streptococcus pneumoniae. Chemotherapy 2001; 47: 409-14.
34. Imbert F, Jardin M, Fernandez C et al. Effect of efflux inhibition on brain uptake of itraconazole in mice infected with Cryptococcus neoformans. Drug Metab Dispos 2003; 31: 319-25.
35. 11C-verapamil and PET. J Nucl Med 2008; 49: 1328-35.
36. Martins A, Spengler G, Martins M et al. Physiological characterisation of the efflux pump system of antibiotic-susceptible and multidrug-resistant Enterobacter aerogenes. Int J Antimicrob Agents 2010; 36: 313-8.
37. Martins A, Spengler G, Rodrigues L et al. pH modulation of efflux pump activity of multi-drug resistant Escherichia coli: protection during its passage and eventual colonization of the colon. PLoS One 2009; 4: e6656.