Dependence of nelfinavir brain uptake on dose and tissue concentrations of the selective P-glycoprotein inhibitor zosuquidar in rats

Drug Metabolism and Disposition

Volumn 34, Issue 4, 2006, Pages 653-659

  Anderson, Bradley D ^a,b   May, Melissa J ^a   Jordan, Sherri ^a   Song, Lin ^a   Roberts, Michael J ^a   Leggas, Markos ^a  

^a University of Kentucky   (United States)

^b UNIVERSITY OF KENTUCKY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

NELFINAVIR; ZOSUQUIDAR;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BRAIN; CONTROLLED STUDY; DRUG ACTIVITY; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG EFFECT; DRUG PENETRATION; DRUG TARGETING; DRUG TOLERANCE; DRUG TRANSPORT; FEMALE; NONHUMAN; PRIORITY JOURNAL; RAT;

ANIMALS; ANTINEOPLASTIC AGENTS; BRAIN; DIBENZOCYCLOHEPTENES; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG INTERACTIONS; FEMALE; HIV PROTEASE INHIBITORS; NELFINAVIR; P-GLYCOPROTEIN; PROTEIN BINDING; QUINOLINES; RATS; RATS, SPRAGUE-DAWLEY;

ANIMALIA; HUMAN IMMUNODEFICIENCY VIRUS;

EID: 33645097407     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.105.006536     Document Type: Article

References (40)

1. Brew BJ (1999) Central nervous system infections - AIDS dementia complex. Neurol Clin 17:862-881.
2. Callies S, de Alwis DP, Harris A, Vasey P, Beijnen JH, Schellens JH, Burgess M, and Aarons L (2003) A population pharmacokinetic model for paclitaxel in the presence of a novel P-gp modulator, zosuquidar trihydrochloride (LY335979). Br J Clin Pharmacol 56:46-56.
3. Carpenter CCJ, Cooper DA, Fischl MA, Gatell JM, and Gazzard BG (2000) Antiretroviral therapy in adults - updated recommendations of the international AIDS Society-USA panel. J Am Med Assoc 283:381-390.
4. Choo EF, Leake B, Wandel C, Imamura H, Wood AJ, Wilkinson GR, and Kim RB (2000) Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes. Drug Metab Dispos 28:655-660.
5. Cunningham PH, Smith DG, Satchell C, Cooper DA, and Brew BJ (2000) Evidence for independent development of resistance to HIV-1 reverse transcriptase inhibitors in the cerebrospinal fluid. AIDS 14:499-507.
6. Dantzig AH, Shepard RL, Law KL, Tabas L, Pratt S, Gillespie JS, Binkley SN, Kuhfeld MT, Starling JJ, and Wrighton SA (1999) Selectivity of the multidrug resistance modulator, LY335979 for P-glycoprotein and effect on cytochrome P-450 activities. J Pharmacol Exp Ther 290:854-862.
7. Edwards JE, Alcorn J, Savolainen J, Anderson BD, and McNamara PJ (2005) Role of P-glycoprotein in distribution of nelfinavir across the blood-mammary tissue barrier and bloodbrain barrier. Antimicrob Agents Chemother 49:1626-1628.
8. Edwards JE, Brouwer KR, and McNamara PJ (2002) GF120918, a P-glycoprotein modulator,increases the concentration of unbound amprenavir in the central nervous system in rats. Antimicrob Agents Chemother 46:2284-2286.
9. Ford JM, Yang JM, and Hait WN (1996) P-glycoprotein-mediated multidrug resistance: experimental and clinical strategies for its reversal. Cancer Treat Res 87:3-38.
10. Groothuis DR and Levy RM (1997) The entry of antiviral and antiretroviral drugs into the central nervous system. J Neurovirol 3:387-400.
11. Herforth C, Stone JA, Jayewardene AL, Blaschke TF, Fang F, Motoya T, and Aweeka FT (2002) Determination of nelfinavir free drug concentrations in plasma by equilibrium dialysis and liquid chromatography/tandem mass spectrometry: important factors for method optimization. Eur J Pharm Sci 15:185-195.
12. Hirsch MS, Conway B, D'Aquila RT, Johnson VA, Brun-Vezinet F, Clotet B, Demeter LM, Hammer SM, Jacobsen DM, Kutitzkes DR, et al. (1998) Antiretroviral drug resistance testing in adults with HIV infections: implications for clinical management. J Am Med Assoc 279:1984-1991.
13. Husstedt I-W, Frohne L, Bockenholt S, Frese A, Rahmann A, Heese C, Reichelt D, and Evers S (2002) Impact of highly active antiretroviral therapy on cognitive processing in HIV infection: cross-sectional and longitudinal studies of event-related potentials. AIDS Res Human Retroviruses 18:485-490.
14. Karssen AM, Meijer OC, van der Sandt ICJ, de Boer AG, de Lange ECM, and de Kloet ER (2002) The role of the efflux transporter P-glycoprotein in brain penetration of prednisolone. J Endocrinol 175:251-260.
15. Kemper EM, Cleypool C, Boogerd W, Beijnen JH, and van Telligen O (2004) The influence of the P-glycoprotein inhibitor zosuquidar trihydrochloride (LY335979) on the brain penetration of paclitaxel in mice. Cancer Chemother Pharmacol 53:173-178.
16. Kepler TB and Perelson AS (1998) Drug concentration heterogeneity facilitates the evolution of drug resistance. Proc Natl Acad Sci USA 95:11514-11519.
17. Kim RB, Fromm MF, Wandel C, Leake B, Wood AJJ, Roden DM, and Wilkinson GR (1998) The drug transporter P-glycoprotein limits oral absorption and brain entry of HIV-1 protease inhibitors. J Clin Investig 101:289-294.
18. Kirschner DE and Webb GF (1997) Resistance, remission and qualitative differences in HIV chemotherapy. Emerg Infect Dis 3:273-283.
19. Kravcik S, Gallicano K, Roth V, Cassol S, Hawley-Foss N, Badley A, and Cameron DW (1999) Cerebrospinal fluid HIV RNA and drug levels with combination ritonavir and saquinavir. J Acquir Immune Defic Syndr 21:371-375.
20. Kroin JS and Norman BH (1998) Drug resistance and multidrug resistance modulators, Eli Lilly and Co.
21. Lafeuillade A, Solas C, Halfon P, Chadapaud S, Hittinger G, and Lacarelle B (2002) Differences in the detection of three HIV-1 protease inhibitors in non-blood compartments: clinical correlations. HIV Clin Trials 3:27-35.
22. Lee CG, Gottesman MM, Cardarelli CO, Ramachandra M, Jeang KT, Ambudkar SV, Pastan I, and Dey S (1998) HIV-1 protease inhibitors are substrates for the MDR1 multidrug transporter. Biochemistry 37:3594-3601.
23. McArthur JC, Haughey N, Gartner S, Conant K, Pardo C, Nath A, and Sacktor N (2003) Human immunodeficiency virus-associated dementia: an evolving disease. J Neurovirol 9:205-221.
24. Pialoux G, Fournier S, Moulignier A, Poveda JD, Clavel F, and Dupont B (1997) Central nervous system as a sanctuary for HIV-1 infection despite treatment with zidovudine, lamivudine and indinavir. AIDS 11:1302-1303.
25. Rubin EH, de Alwis DP, Pouliquen I, Green L, Marder P, Lin Y, Musanti R, Grospe SL, Smith SL, Toppmeyer DL, et al. (2002) A phase I trial of a potent P-glycoprotein inhibitor, zosuquidar.·3HCl trihydrochloride (LY335979), administered orally in combination with doxorubicin in patients with advanced malignancies. Clin Cancer Res 8:3710-3717.
26. Salama NN, Kelly EJ, Bui T, and Ho RJY (2005) The impact of pharmacologic and genetic knockout of P-glycoprotein on nelfinavir levels in the brain and other tissues in mice. J Pharm Sci 94:1216-1225.
27. Sankatsing SUC, Beijnen JH, Schinkel AH, Lange JMA, and Prins JM (2004) P glycoprotein in human immunodeficiency virus type 1 infection and therapy. Antimicrob Agents Chemother 48:1073-1081.
28. Savolainen J, Edwards JE, Morgan ME, McNamara PJ, and Anderson BD (2002) Effects of a P-glycoprotein inhibitor on brain and plasma concentrations of anti-human immunodeficiency virus drugs administered in combination in rats. Drug Metab Dispos 30:479-482.
29. Sawchuk RJ and Yang Z (1999) Investigation of distribution, transport and uptake of anti-HIV drugs to the central nervous system. Adv Drug Deliv Rev 39:5-31.
30. Schinkel AH, Kemp S, Dolle M, Rudenko G, and Wagenaar E (1993) N-glycosylation and deletion mutants of the human MDR1 P-glycoprotein. J Biol Chem 268:7474-7481.
31. Schon A, del Mar IM, and Freire E (2003) The binding of HIV-1 protease inhibitors to human serum proteins. Biophys Chem 105:221-230.
32. Schrager LK and D'Souza MP (1998) Cellular and anatomical reservoirs of HIV-1 in patients receiving potent antiretroviral combination therapy. J Am Med Assoc 280:67-71.
33. Shetty BV, Kosa MB, Khalil DA, and Webber S (1996) Preclinical pharmacokinetics and distribution to tissue of AG1343, an inhibitor of human immunodeficiency virus type 1 protease. Antimicrob Agents Chemother 40:110-114.
34. Smit TK, Brew BJ, Tourtellotte W, Morgello S, Gelman BB, and Saksena NK (2004) Independent evolution of human immunodeficiency virus (HIV) drug resistance mutations in diverse areas of the brain in HIV-infected patients, with and without dementia, on antiretroviral treatment. J Virol 78:10133-10148.
35. Solas C, Lafeuillade A, Halfon P, Chadapaud S, Hittinger G, and Lacarelle B (2003) Discrepancies between protease inhibitor concentrations and viral load in reservoirs and sanctuary sites in human immunodeficiency virus-infected patients. Antimicrob Agents Chemother 47:238-243.
36. Suzuki T, Fukazawa N, San-nohe K, Sato W, Yano O, and Tsuruo T (1997) Structure-activity relationship of newly synthesized quinoline derivatives for reversal of multidrug resistance in cancer. J Med Chem 40:2047-2052.
37. van der Sandt CJ, Vos CM, Nabulsi L, Blom-Roosemalen MC, Voorwinden HH, de Boer AG, and Breimer DD (2001) Assessment of active transport of HIV protease inhibitors in various cell lines and the in vitro blood-brain barrier. AIDS 15:483-491.
38. Waynforth HB and Flecnell PA (1994) Experimental and Surgical Technique in the Rat. Academic Press, Inc., San Diego, CA.
39. Wierdl M, Wall A, Morton CL, Sampath J, Danks MK, Schuetz JD, and Potter PM (2003) Carboxylesterase-mediated sensitization of human tumor cells to CPT-11 cannot override ABCG2-mediated drug resistance. Mol Pharmacol 64:279-288.
40. Winters MA, Baxter JD, Mayers DL, Wentworth DN, Hoover ML, Neaton JD, and Merigan TC (2000) Frequency of antiretroviral drug resistance mutations in HIV-1 strains from patients failing triple drug regimens. The Terry Beirn Community Programs for Clinical Research on AIDS. Antivir Ther 5:57-63.