The distribution of the anti-HIV drug, tenofovir (PMPA), into the brain, CSF and choroid plexuses

Cerebrospinal Fluid Research

Volumn 3, Issue , 2006, Pages

  Anthonypillai, Christy ^a   Gibbs, Julie E ^a,b   Thomas, Sarah A ^a  

^a KING'S COLLEGE LONDON   (United Kingdom)

^b ST GEORGE'S UNIVERSITY OF LONDON   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

ANTI HUMAN IMMUNODEFICIENCY VIRUS AGENT; CARBON 14; MANNITOL; PROBENECID; PRODRUG; RNA DIRECTED DNA POLYMERASE INHIBITOR; TENOFOVIR DISOPROXIL;

ANALYSIS OF VARIANCE; ANIMAL EXPERIMENT; ARTICLE; BLOOD BRAIN BARRIER; BLOOD CEREBROSPINAL FLUID BARRIER; BRAIN CAPILLARY; BRAIN PERFUSION; BRAIN REGION; CAROTID ARTERY FLOW; CEREBELLUM; CEREBROSPINAL FLUID; CHOROID PLEXUS; CONTROLLED STUDY; DRUG APPROVAL; DRUG BLOOD LEVEL; DRUG DISTRIBUTION; DRUG PENETRATION; DRUG STABILITY; DRUG STRUCTURE; DRUG TRANSPORT; DRUG USE; ENDOTHELIUM CELL; GUINEA PIG; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; HYDROPHILICITY; HYPOPHYSIS; LATERAL BRAIN VENTRICLE; MACROPHAGE; MICROGLIA; NEUROLOGIC DISEASE; NONHUMAN; PARTITION COEFFICIENT; PRIORITY JOURNAL; SCINTILLATION COUNTING; STUDENT T TEST;

EID: 33645895267     PISSN: 17438454     EISSN: None     Source Type: Journal    
DOI: 10.1186/1743-8454-3-1     Document Type: Article

References (57)

1. Cundy KC, Sueoka C, Lynch GR, Griffin L, Lee WA, Shaw JP: Pharmacokinetics and bioavailability of the anti-human immunodeficiency virus nucleotide analog 9-[(R)-2(phosphonomethoxy)propyl]adenine (PMPA) in dogs. Antimicrob Agents Chemother 1998, 42:687-690.
2. Schooley RT, Ruane P, Myers RA, Beall G, Lampiris H, Berger D, Chen SS, Miller MD, Isaacson E, Cheng AK: Tenofovir DF in antiretroviral-experienced patients: results from a 48-week, randomized, double-blind study. AIDS 2002, 16:1257-1263.
3. Barditch-Crovo P, Deeks SG, Collier A, Safrin S, Coakley DF, Miller M, Kearney BP, Coleman RL, Lamy PD, Kahn JO, McGowan I, Lietman PS: Phase i/ ii trial of the pharmacokinetics, safety, and antiretroviral activity of tenofovir disoproxil fumarate in human immunodeficiency virus-infected adults. Antimicrob Agents Chemother 2001, 45:2733-2739.
4. Louie M, Hogan C, Hurley A, Simon V, Chung C, Padte N, Lamy P, Flaherty J, Coakley D, Di Mascio M, Perelson AS, Markowitz M: Determining the antiviral activity of tenofovir disoproxil fumarate in treatment-naive chronically HIV-1-infected individuals. AIDS 2003, 17:1151-1156.
5. Gallant JE, Deresinski S: Tenofovir disoproxil fumarate. Clin Infect Dis 2003, 37:944-950.
6. Back DJ, Burger DM, Flexner CW, Gerber JG: The pharmacology of antiretroviral nucleoside and nucleotide reverse transcriptase inhibitors: implications for once-daily dosing. J Acquir Immune Defic Syndr 2005, 39 Suppl 1:S1-23, quiz.
7. Sabin CA: The changing clinical epidemiology of AIDS in the highly active antiretroviral therapy era. AIDS 2002, 16 Suppl 4:S61-S68.
8. Finzi D, Blankson J, Siliciano JD, Margolick JB, Chadwick K, Pierson T, Smith K, Lisziewicz J, Lori F, Flexner C, Quinn TC, Chaisson RE, Rosenberg E, Walker B, Gange S, Gallant J, Siliciano RF: Latent infection of CD4+ T cells provides a mechanism for lifelong persistence of HIV-1, even in patients on effective combination therapy. Nat Med 1999, 5:512-517.
9. Stebbing J, Gazzard B, Douek DC: Where does HIV live? N Engl J Med 2004, 350:1872-1880.
10. Blankson JN, Persaud D, Siliciano RF: The challenge of viral reservoirs in HIV-1 infection. Annu Rev Med 2002, 53:557-593.
11. Schrager LK, D'Souza MP: Cellular and anatomical reservoirs of HIV-1 in patients receiving potent antiretroviral combination therapy. JAMA 1998, 280:67-71.
12. Wong JK, Hezareh M, Gunthard HF, Havlir DV, Ignacio CC, Spina CA, Richman DD: Recovery of replication-competent HIV despite prolonged suppression of plasma viremia. Science 1997, 278:1291-1295.
13. Siliciano JD, Siliciano RF: Latency and viral persistence in HIV-1 infection. J Clin Invest 2000, 106:823-825.
14. Chun TW, Fauci AS: Latent reservoirs of HIV: obstacles to the eradication of virus. Proc Natl Acad Sci U S A 1999, 96:10958-10961.
15. Aquaro S, Bagnarelli P, Guenci T, De Luca A, Clementi M, Balestra E, Calio R, Perno, CF: Long-term survival and virus production in human primary macrophages infected by human immunodeficiency virus. J Med Virol 2002, 68:479-488.
16. Crowe SM, Mills J, Kirihara J, Boothman J, Marshall JA, McGrath MS: Full-length recombinant CD4 and recombinant gp 120 inhibit fusion between HIV infected macrophages and uninfected CD4-expressing T-lymphoblastoid cells. AIDS Res Hum Retroviruses 1990, 6:1031-1037.
17. Smith BA, Gartner S, Liu Y, Perelson AS, Stilianakis NI, Keele BF, Kerkering TM, Ferreira-Gonzalez A, Szakal AK, Tew JG, Burton GF: Persistence of infectious HIV on follicular dendritic cells. J Immunol 2001, 166:690-696.
18. Gunthard HF, Havlir DV, Fiscus S, Zhang ZQ, Eron J, Mellors J, Gulick R, Frost SD, Brown AJ, Schleif W, Valentine F, Jonas L, Meibohm A, Ignacio CC, Isaacs R, Gamagami R, Emini E, Haase A, Richman DD, Wong JK: Residual human immunodeficiency virus (HIV) Type 1 RNA and DNA in lymph nodes and HIV RNA in genital secretions and in cerebrospinal fluid after suppression of viremia for 2 years. J Infect Dis 2001, 183:1318-1327.
19. McArthur JC, McClernon DR, Cronin MF, Nance-Sproson TE, Saah AJ, St Clair M, Lanier ER: Relationship between human immunodeficiency virus-associated dementia and viral load in cerebrospinal fluid and brain. Ann Neurol 1997, 42:689-698.
20. Arendt G, von Giesen HJ, Hefter H, Theisen A: Therapeutic effects of nucleoside analogues on psychomotor slowing in HIV infection. AIDS 2001, 15:493-500.
21. von Giesen HJ, Koller H, Theisen A, Arendt G: Therapeutic effects of nonnucleoside reverse transcriptase inhibitors on the central nervous system in HIV-1-infected patients. J Acquir Immune Defic Syndr 2002, 29:363-367.
22. Cunningham PH, Smith DG, Satchell C, Cooper DA, Brew B: Evidence for independent development of resistance to HIV-1 reverse transcriptase inhibitors in the cerebrospinal fluid. AIDS 2000, 14:1949-1954.
23. Stingele K, Haas J, Zimmermann T, Stingele R, Hubsch-Muller C, Freitag M, Storch-Hagenlocher B, Hartmann M, Wildemann B: Independent HIV replication in paired CSF and blood viral isolates during antiretroviral therapy. Neurology 2001, 56:355-361.
24. Venturi G, Catucci M, Romano L, Corsi P, Leoncini F, Valensin PE, Zazzi M: Antiretroviral resistance mutations in human immunodeficiency virus type 1 reverse transcriptase and protease from paired cerebrospinal fluid and plasma samples. J Infect Dis 2000, 181:740-745.
25. Gibbs JE, Thomas SA: The distribution of the anti-HIV drug, 2′3′-dideoxycytidine (ddC), across the blood-brain and blood-cerebrospinal fluid barriers and the influence of organic anion transport inhibitors. J Neurochem 2002, 80:392-404.
26. Sisson WB, Oldendorf WH: Brain distribution spaces of mannitol-3H, inulin-14C, and dextran-14C in the rat. Am J Physiol 1971, 221:214-217.
27. Anthonypillai C, Sanderson RN, Gibbs JE, Thomas SA: The distribution of the HIV protease inhibitor, ritonavir, to the brain, cerebrospinal fluid, and choroid plexuses of the guinea pig. J Pharmacol Exp Ther 2004, 308:912-920.
28. Cornford EM, Braun LD, Oldendorf WH, Hill MA: Comparison of lipid-mediated blood-brain-barrier penetrability in neonates and adults. Am J Physiol 1982, 243:C161-C168.
29. Gross PM: Circumventricular organ capillaries. Prog Brain Res 1992, 91:219-233.
30. Smith QR, Woodbury DM, Johanson CE: Kinetic analysis of [36Cl]-, [22Na]- and [3H]mannitol uptake into the in vivo choroid plexus-cerebrospinal fluid brain system: ontogeny of the blood brain and blood-CSF barriers. Brain Res 1982, 255:181-198.
31. Bouldin TW, Krigman MR: Differential permeability of cerebral capillary and choroid plexus to lanthanum ion. Brain Res 1975, 99:444-448.
32. Ek CJ, Habgood MD, Dziegielewska KM, Potter A, Saunders NR: Permeability and route of entry for lipid-insoluble molecules across brain barriers in developing Monodelphis domestica. J Physiol 2001, 536:841-853.
33. Thomas SA, Segal MB: The transport of the anti-HIV drug, 2′,3′-didehydro-3′-deoxythymidine (D4T), across the blood-brain and blood-cerebrospinal fluid barriers. Br J Pharmacol 1998, 125:49-54.
34. Ghersi-Egea JF, Finnegan W, Chen JL, Fenstermacher JD: Rapid distribution of intraventricularly administered sucrose into cerebrospinal fluid cisterns via subarachnoid velae in rat. Neuroscience 1996, 75:1271-1288.
35. Rennels ML, Gregory TF, Blaumanis OR, Fujimoto K, Grady PA: Evidence for a 'paravascular' fluid circulation in the mammalian central nervous system, provided by the rapid distribution of tracer protein throughout the brain from the subarachnoid space. Brain Res 1985, 326:47-63.
36. Fischer-Smith T, Croul S, Sverstiuk AE, Capini C, L'Heureux D, Regulier EG, Richardson MW, Amini S, Morgello S, Khalili K, Rappaport J: CNS invasion by CD14+/CD16+ peripheral blood-derived monocytes in HIV dementia: perivascular accumulation and reservoir of HIV infection. J Neurovirol 2001, 7:528-541.
37. Wiley CA, Schrier RD, Nelson JA, Lampert PW, Oldstone MB: Cellular localization of human immunodeficiency virus infection within the brains of acquired immune deficiency syndrome patients. Proc Natl Acad Sci U S A 1986, 83:7089-7093.
38. Takahashi K, Wesselingh SL, Griffin DE, McArthur JC, Johnson RT, Glass JD: Localization of HIV-1 in human brain using polymerase chain reaction/ in situ hybridization and immunocytochemistry. Ann Neurol 1996, 39:705-711.
39. Williams K, Alvarez X, Lackner AA: Central nervous system perivascular cells are immunoregulatory cells that connect the CNS with the peripheral immune system. Glia 2001, 36:156-164.
40. Cihlar T, Ho ES, Lin DC, Mulato AS: Human renal organic anion transporter 1 (hOAT1) and its role in the nephrotoxicity of antiviral nucleotide analogs. Nucleosides Nucleotides Nucleic Acids 2001, 20:641-648.
41. Izzedine H, Launay-Vacher V, Deray G: Renal tubular transporters and antiviral drugs: an update. AIDS 2005, 19:455-462.
42. Sweet DH, Miller DS, Pritchard JB, Fujiwara Y, Beier DR, Nigam SK: Impaired organic anion transport in kidney and choroid plexus of organic anion transporter 3 (Oat3 (Slc22a8)) knockout mice. J Biol Chem 2002, 277:26934-26943.
43. Nagata Y, Kusuhara H, Endou H, Sugiyama Y: Expression and functional characterization of rat organic anion transporter 3 (rOat3) in the choroid plexus. Mol Pharmacol 2002, 61:982-988.
44. Choudhuri S, Cherrington NJ, Li N, Klaassen CD: Constitutive expression of various xenobiotic and endobiotic transporter mRNAs in the choroid plexus of rats. Drug Metab Dispos 2003, 31:1337-1345.
45. Pritchard JB, Sweet DH, Miller DS, Walden R: Mechanism of organic anion transport across the apical membrane of choroid plexus. J Biol Chem 1999, 274:33382-33387.
46. Sun H, Dai H, Shaik N, Elmquist WF: Drug efflux transporters in the CNS. Adv Drug Deliv Rev 2003, 55:83-105.
47. Race JE, Grassi SM, Williams WJ, Holtzman EJ: Molecular cloning and characterization of two novel human renal organic anion transporters (hOAT1 and hOAT3). Biochem Biophys Res Commun 1999, 255:508-514.
48. Sekine T, Cha SH, Endou H: The multispecific organic anion transporter (OAT) family. Pflugers Arch 2000, 440:337-350.
49. Kusuhara H, He Z, Nagata Y, Nozaki Y, Ito T, Masuda H, Meier PJ, Abe T, Sugiyama Y: Expression and functional involvement of organic anion transporting polypeptide subtype 3 (Slc21a7) in rat choroid plexus. Pharm Res 2003, 20:720-727.
50. Ohtsuki S, Kikkawa T, Mori S, Hori S, Takanaga H, Otagiri M, Terasaki T: Mouse reduced in osteosclerosis transporter functions as an organic anion transporter 3 and is localized at abluminal membrane of blood-brain barrier. J Pharmacol Exp Ther 2004, 309:1273-1281.
51. Gibbs JE, Jayabalan P, Thomas SA: Mechanisms by which 2′,3′-dideoxyinosine (ddl) crosses the guinea-pig CNS barriers; relevance to HIV therapy. J Neurochem 2003, 84:725-734.
52. Ray AS, Myrick F, Vela JE, Olson LY, Eisenberg EJ, Borroto-Esodo K, Miller MD, Fridland A: Lack of a metabolic and antiviral drug interaction between tenofovir, abacavir and lamivudine. Antivir Ther 2005, 10:451-457.
53. Mulato AS, Cherrington JM: Anti-HIV activity of adefovir (PMEA) and PMPA in combination with antiretroviral compounds: in vitro analyses. Antiviral Res 1997, 36:91-97.
54. Hawkins T, Veikley W, St CRL III, Guyer B, Clark N, Kearney BP: Intracellular pharmacokinetics of tenofovir diphosphate, carbovir triphosphate, and lamivudine triphosphate in patients receiving triple-nucleoside regimens. J Acquir Immune Defic Syndr 2005, 39:406-411.
55. Lanier ER, Hazen R, Ross L, Freeman A, Harvey R: Lack of antagonism between abacavir, lamivudine, and tenofovir against wild-type and drug-resistant HIV-1. J Acquir Immune Defic Syndr 2005, 39:519-522.
56. Perez-Elias MJ, Moreno S, Gutierrez C, Lopez D, Abraira V, Moreno A, Dronda F, Casado JL, Antela A, Rodriguez MA: High virological failure rate in HIV patients after switching to a regimen with two nucleoside reverse transcriptase inhibitors plus tenofovir. AIDS 2005, 19:695-698.
57. Maitland D, Moyle G, Hand J, Mandalia S, Boffito M, Nelson M, Gazard B: Early virologic failure in HIV-1 infected subjects on didanosine/ tenofovir/efavirenz: 12-week results from a randomized trial. AIDS 2005, 19:1183-1188.