Distribution of STI-571 to the brain is limited by P-glycoprotein-mediated efflux

Journal of Pharmacology and Experimental Therapeutics

Volumn 304, Issue 3, 2003, Pages 1085-1092

  Dai, Haiqing ^a   Marbach, Peter ^b   Lemaire, Michel ^b   Hayes, Michael ^b   Elmquist, William F ^a  

^a UNIVERSITY OF MINNESOTA   (United States)

^b NOVARTIS PHARMA AG   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

GLYCOPROTEIN P; IMATINIB; ZOSUQUIDAR;

ANIMAL TISSUE; APICAL MEMBRANE; ARTICLE; BASOLATERAL MEMBRANE; BLOOD BRAIN BARRIER; CENTRAL NERVOUS SYSTEM; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG DELIVERY SYSTEM; DRUG DISTRIBUTION; DRUG TRANSPORT; KNOCKOUT MOUSE; MOUSE; NONHUMAN; PRIORITY JOURNAL;

ANIMALS; ANTINEOPLASTIC AGENTS; BIOLOGICAL TRANSPORT; BRAIN; CELLS, CULTURED; DOGS; MICE; MICE, KNOCKOUT; P-GLYCOPROTEIN; PIPERAZINES; PYRIMIDINES; TRANSFECTION;

EID: 0344520475     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: 10.1124/jpet.102.045260     Document Type: Article

References (43)

1. Abbruscato TJ, Thomas SA, Hruby VJ, and Davis TP (1997) Blood-brain barrier permeability and bioavailability of a highly potent and μ-selective opioid receptor antagonist, CTAP: comparison with morphine. J Pharmacol Exp Ther 280:402-409.
2. Bakhtiar R, Khemani L, Hayes M, Bedman T, and Tse F (2002) Quantification of the anti-leukemia drug STI571 (Gleevec) and its metabolite (CGP 74588) in monkey plasma using a semi-automated solid phase extraction procedure and liquid chromatography-tandem mass spectrometry. J Pharm Biomed Anal 28:183-1194.
3. Beaulieu E, Demeule M, Ghitescu L, and Beliveau R (1997) P-glycoprotein is strongly expressed in the luminal membranes of the endothelium of blood vessels in the brain. Biochem J 326:539-544.
4. Buchdunger E, Cioffi CL, Law N, Stover D, Ohno-Jones S, Druker BJ, and Lydon NB (2000) Abl protein-tyrosine kinase inhibitor STI571 inhibits in vitro signal transduction mediated by c-kit and platelet-derived growth factor receptors. J Pharmacol Exp Ther 295:139-145.
5. Buchdunger E, Zimmermann J, Mett H, Meyer T, Muller M, Druker BJ, and Lydon NB (1996) Inhibition of the Abl protein-tyrosine kinase in vitro and in vivo by a 2-phenylaminopyrimidine derivative. Cancer Res 56:100-104.
6. Cordon-Cardo C, O'Brien JP, Casals D, Rittman-Grauer L, Biedler JL, Melamed MR, and Bertino JR (1989) Multidrug-resistance gene (P-glycoprotein) is expressed by endothelial cells at blood-brain barrier sites. Proc Natl Acad Sci USA 86:695-698.
7. Daley GQ, Van Etten RA, and Baltimore D (1990) Induction of chronic myelogenous leukemia in mice by the P210bcr/abl gene of the Philadelphia chromosome. Science (Wash DC) 247:824-830.
8. 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.
9. Davies DC (2002) Blood-brain barrier breakdown in septic encephalopathy and brain tumours. J Anat 200:639-646.
10. Deininger MW, Goldman JM, Lydon N, and Melo JV (1997) The tyrosine kinase inhibitor CGP57148B selectively inhibits the growth of BCR-ABL-positive cells. Blood 90:3691-3698.
11. Demeule M, Shedid D, Beaulieu E, Del Maestro RF, Moghrabi A, Ghosn PB, Moumdjian R, Berthelet F, and Beliveau R (2001) Expression of multidrug-resistance P-glycoprotein (MDR1) in human brain tumors. Int J Cancer 93:62-66.
12. Druker BJ, Talpaz M, Resta DJ, Peng B, Buchdunger E, Ford JM, Lydon NB, Kantarjian H, Capdeville R, Ohno-Jones S, et al. (2001) Efficacy and safety of a specific inhibitor of the BCR-ABL tyrosine kinase in chronic myeloid leukemia. N Engl J Med 344:1031-1037.
13. Druker BJ, Tamura S, Buchdunger E, Ohno S, Segal GM, Fanning S, Zimmermann J, and Lydon NB (1996) Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of Bcr-Abl positive cells. Nat Med 2:561-566.
14. Gambacorti-Passerini C, le Coutre P, Mologni L, Fanelli M, Bertazzoli C, Marchesi E, Di Nicola M, Biondi A, Corneo GM, Belotti D, et al. (1997) Inhibition of the ABL kinase activity blocks the proliferation of BCR/ABL+ leukemic cells and induces apoptosis. Blood Cells Mol Dis 23:380-394.
15. Gorre ME, Mohammed M, Ellwood K, Hsu N, Paquette R, Rao PN, and Sawyers CL (2001) Clinical resistance to STI-571 cancer therapy caused by BCR-ABL gene mutation or amplification. Science (Wash DC) 293:876-880.
16. Groothuis DR (2000) The blood-brain and blood-tumor barriers: a review of strategies for increasing drug delivery. Neurooncology 2:45-59.
17. Heinrich MC, Griffith DJ, Druker BJ, Wait CL, Ott KA, and Zigler AJ (2000) Inhibition of c-kit receptor tyrosine kinase activity by STI 571, a selective tyrosine kinase inhibitor. Blood 96:925-932.
18. Joensuu H, Roberts PJ, Sarlomo-Rikala M, Andersson LC, Tervahartiala P, Tuveson D, Silberman S, Capdeville R, Dimitrijevic S, Druker B, et al. (2001) Effect of the tyrosine kinase inhibitor STI571 in a patient with a metastatic gastrointestinal stromal tumor. N Engl J Med 344:1052-1056.
19. Kelliher MA, McLaughlin J, Witte ON, and Rosenberg N (1990) Induction of a chronic myelogenous leukemia-like syndrome in mice with v-abl and BCR/ABL. Proc Natl Acad Sci USA 87:6649-6653.
20. Kilic T, Alberta JA, Zdunek PR, Acar M, Iannareli P, O'Reilly T, Buchdunger E, Black PM, and Stiles CD (2000) Intracranial inhibition of platelet-derived growth factor-mediated glioblastoma cell growth by an orally active kinase inhibitor of the 2-phenylaminopyrimidine class. Cancer Res 60:5143-5150.
21. Konopka JB, Watanabe SM, and Witte ON (1984) An alteration of the human c-abl protein in K562 leukemia cells unmasks associated tyrosine kinase activity. Cell 37:1035-1042.
22. Krystal GW, Honsawek S, Litz J, and Buchdunger E (2000) The selective tyrosine kinase inhibitor STI571 inhibits small cell lung cancer growth. Clin Cancer Res 6:3319-3326.
23. Kusuhara H and Sugiyama Y (2002) Role of transporters in the tissue-selective distribution and elimination of drugs: transporters in the liver, small intestine, brain and kidney. J Control Release 78:43-54.
24. Leis JF, Stepan DE, Curtin PT, Peng B, Ford JM, Schubach SE, Fleming WH, Druker BJ, and Maziarz RT (2001) Low penetration of imatinib (STI571) into the CSF indicates need for standard CNS prophylaxis in patients with CML lymphoid blast crisis and Philadelphia Chromosome Positive ALL. The Proceedings of the American Society of Hematology 43rd Annual Meeting, abstract no. 2593.
25. Lesniak MS, Langer R, and Brem H (2001) Drug delivery to tumors of the central nervous system. Curr Neurol Neurosci Rep 1:210-216.
26. Levin VA, Freeman-Dove M, and Landahl HD (1975) Permeability characteristics of brain adjacent to tumors in rats. Arch Neurol 32:785-791.
27. Mahon FX, Deininger MW, Schultheis B, Chabrol J, Reiffers J, Goldman JM, and Melo JV (2000) Selection and characterization of BCR-ABL positive cell lines with differential sensitivity to the tyrosine kinase inhibitor STI571: diverse mechanisms of resistance. Blood 96:1070-1079.
28. Melo JV (1996) The molecular biology of chronic myeloid leukemia. Leukemia 10: 751-756.
29. Murakami H, Takanaga H, Matsuo H, Ohtani H, and Sawada Y (2000) Comparison of blood-brain barrier permeability in mice and rats using in situ brain perfusion technique. Am J Physiol Heart Circ Physiol 279:H1022-H1028.
30. Petzer AL, Gunsilius E, Hayes M, Stockhammer G, Duba HC, Schneller F, Grunewald K, Poewe W, and Gasti G (2002) Low concentrations of STI571 in the cerebrospinal fluid: a case report. Br J Haematol 117:623-625.
31. Plaat BE, Hollema H, Molenaar WM, Torn Broers GH, Pijpe J, Mastik MF, Hoekstra HJ, van den Berg E, Scheper RJ, and van der Graaf WT (2000) Soft tissue leiomyosarcomas and malignant gastrointestinal stromal tumors: differences in clinical outcome and expression of multidrug resistance proteins. J Clin Oncol 18:3211-3220.
32. Regina A, Demeuk M, Laplante A, Jodoin J, Dagenais C, Berthelet F, Moghrabi A, and Beliveau R (2001) Multidrug resistance in brain tumors: roles of the bloodbrain barrier. Cancer Metastasis Rev 20:13-25.
33. Rowley JD (1973) A new consistent abnormality in chronic myelogenous leukaemia identified by quinacrine fluorescence and giemsa staining. Nature (Lond) 243: 290-293.
34. Schinkel AH, Wagenaar E, Mol CA, and van Deemter L (1996) P-glycoprotein in the blood-brain barrier of mice influences the brain penetration and pharmacological activity of many drugs. J Clin Invest 97:2517-2524.
35. Smith QR, Ziylan YZ, Robinson PJ, and Rapoport SI (1988) Kinetics and distribution volumes for tracers of different sizes in the brain plasma space. Brain Res 462:1-9.
36. Starling JJ, Shepard RL, Cao J, Law KL, Norman BH, Kroin JS, Ehlhardt WJ, Baughman TM, Winter MA, Bell MG, et al. (1997) Pharmacological characterization of LY335979: a potent cyclopropyldibenzosuberane modulator of P-glycoprotein. Adv Enzyme Regul 37:335-347.
37. Takayama N, Sato N, O'Brien SG, Ikeda Y, and Okamoto S (2002) Imatinib mesylate has limited activity against the central nervous system involvement of Philadel-phia chromosome-positive acute lymphoblastic leukaemia due to poor penetration into cerebrospinal fluid. Br J Haematol 119:106-108.
38. Tews DS, Nissen A, Kulgen C, and Gaumann AK (2000) Drug resistance-associated factors in primary and secondary glioblastomas and their precursor tumors. J Neurooncol 50:227-237.
39. Thiebaut F, Tsuruo T, Hamada H, Gottesman MM, Pastan I, and Willingham MC (1989) Immunohistochemical localization in normal tissues of different epitopes in the multidrug transport protein P170: evidence for localization in brain capillaries and crossreactivity of one antibody with a muscle protein. J Histochem Cytochem 37:159-164.
40. Tuveson DA, Willis NA, Jacks T, Griffin JD, Singer S, Fletcher CD, Fletcher JA, and Demetri GD (2001) STI571 inactivation of the gastrointestinal stromal tumor c-KIT oncoprotein: biological and clinical implications. Oncogene 20:5054-5058.
41. Uhrbom L, Hesselager G, Ostman A, Nister M, and Westermark B (2000) Dependence of autocrine growth factor stimulation in platelet-derived growth factor-B-induced mouse brain tumor cells. Int J Cancer 85:398-406.
42. van Oosterom AT, Judson I, Verweij J, Stroobants S, Donato di Paola E, Dimitrijevic S, Martens M, Webb A, Sciot R, Van Glabbeke M, et al. (2001) Safety and efficacy of imatinib (STI571) in metastatic gastrointestinal stromal tumours: a phase I study. Lancet 358:1421-1423.
43. Wang WL, Healy ME, Sattler M, Verma S, Lin J, Maulik G, Stiles CD, Griffin JD, Johnson BE, and Salgia R (2000) Growth inhibition and modulation of kinase pathways of small cell lung cancer cell lines by the novel tyrosine kinase inhibitor STI 571. Oncogene 19:3521-3628.