P-glycoprotein and breast cancer resistance protein influence brain distribution of dasatinib

Journal of Pharmacology and Experimental Therapeutics

Volumn 330, Issue 3, 2009, Pages 956-963

  Chen, Ying ^a   Agarwal, Sagar ^a   Shaik, Naveed M ^a   Chen, Cliff ^b   Yang, Zheng ^b   Elmquist, William F ^a  

^a UNIVERSITY OF MINNESOTA   (United States)

^b BRISTOL MYERS SQUIBB   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 (6 ISOBUTYL 9 METHOXY 1,4 DIOXO 1,2,3,4,6,7,12,12ALPHA OCTAHYDROPYRAZINO 1',2':1,6 PYRIDO 3,4 B INDOL 3 YL)PROPIONIC ACID TERT BUTYL ESTER; BREAST CANCER RESISTANCE PROTEIN; DASATINIB; ELACRIDAR; GLYCOPROTEIN P; GLYCOPROTEIN P INHIBITOR; IMATINIB; KO 143; MITOXANTRONE; UNCLASSIFIED DRUG; VINBLASTINE SULFATE; ZOSUQUIDAR;

ANIMAL CELL; ANIMAL EXPERIMENT; APICAL MEMBRANE; ARTICLE; BASOLATERAL MEMBRANE; BLOOD BRAIN BARRIER; BRAIN METASTASIS; CENTRAL NERVOUS SYSTEM; CONTROLLED STUDY; DRUG ACCUMULATION; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG DISTRIBUTION; DRUG PENETRATION; DRUG TRANSPORT; IN VIVO STUDY; MOUSE; NONHUMAN; PRIORITY JOURNAL; WILD TYPE;

ACRIDINES; ANIMALS; ANTINEOPLASTIC AGENTS, PHYTOGENIC; ATP-BINDING CASSETTE TRANSPORTERS; BLOOD-BRAIN BARRIER; BRAIN; CELL LINE; CELL MEMBRANE PERMEABILITY; DIBENZOCYCLOHEPTENES; DOGS; DRUG RESISTANCE, NEOPLASM; INDICATORS AND REAGENTS; MASS SPECTROMETRY; MICE; MICE, KNOCKOUT; NEURONS; P-GLYCOPROTEIN; P-GLYCOPROTEINS; PROTEIN KINASE INHIBITORS; PYRIMIDINES; QUINOLINES; TETRAHYDROISOQUINOLINES; THIAZOLES; VINBLASTINE;

EID: 70349142722     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.109.154781     Document Type: Article

References (29)

1. Allen JD, van Loevezijn A, Lakhai JM, van der Valk M, van Tellingen O, Reid G, Schellens JH, Koomen GJ, and Schinkel AH (2002) Potent and specific inhibition of the breast cancer resistance protein multidrug transporter in vitro and in mouse intestine by a novel analogue of fumitremorgin C. Mol Cancer Ther 1:417-425.
2. Anonymous (2006) Dasatinib: BMS 354825. Drugs R D 7:129-132.
3. Bihorel S, Camenisch G, Lemaire M, and Scherrmann JM (2007a) Influence of breast cancer resistance protein (Abcg2) and p-glycoprotein (Abcb1a) on the transport of imatinib mesylate (Gleevec) across the mouse blood-brain barrier. J Neurochem 102:1749-1757. (Pubitemid 47329285)
4. Bihorel S, Camenisch G, Lemaire M, and Scherrmann JM (2007b) Modulation of the brain distribution of imatinib and its metabolites in mice by valspodar, zosuquidar and elacridar. Pharm Res 24:1720-1728. (Pubitemid 47206611)
5. Breedveld P, Beijnen JH, and Schellens JH (2006) Use of P-glycoprotein and BCRP inhibitors to improve oral bioavailability and CNS penetration of anticancer drugs. Trends Pharmacol Sci 27:17-24. (Pubitemid 43063120)
6. Breedveld P, Pluim D, Cipriani G, Wielinga P, van Tellingen O, Schinkel AH, and Schellens JH (2005) The effect of Bcrp1 (Abcg2) on the in vivo pharmacokinetics and brain penetration of imatinib mesylate (Gleevec): implications for the use of breast cancer resistance protein and P-glycoprotein inhibitors to enable the brain penetration of imatinib in patients. Cancer Res 65:2577-2582. (Pubitemid 40490054)
7. Cortes J, Rousselot P, Kim DW, Ritchie E, Hamerschlak N, Coutre S, Hochhaus A, Guilhot F, Saglio G, Apperley J, et al. (2007) Dasatinib induces complete hematologic and cytogenetic responses in patients with imatinib-resistant or -intolerant chronic myeloid leukemia in blast crisis. Blood 109:3207-3213. (Pubitemid 46572505)
8. Dai H, Marbach P, Lemaire M, Hayes M, and Elmquist WF (2003) Distribution of STI-571 to the brain is limited by P-glycoprotein-mediated efflux. J Pharmacol Exp Ther 304:1085-1092. (Pubitemid 36254421)
9. Dai Y, Rahmani M, Corey SJ, Dent P, and Grant S (2004) A Bcr/Abl-independent, Lyn-dependent form of imatinib mesylate (STI-571) resistance is associated with altered expression of Bcl-2. J Biol Chem 279:34227-34239. (Pubitemid 39318046)
10. de Vries NA, Zhao J, Kroon E, Buckle T, Beijnen JH, and van Tellingen O (2007) P-glycoprotein and breast cancer resistance protein: two dominant transporters working together in limiting the brain penetration of topotecan. Clin Cancer Res 13:6440-6449. (Pubitemid 350075034)
11. Donato NJ, Wu JY, Stapley J, Gallick G, Lin H, Arlinghaus R, and Talpaz M (2003) BCR-ABL independence and LYN kinase overexpression in chronic myelogenous leukemia cells selected for resistance to STI571. Blood 101:690-698. (Pubitemid 36077594)
12. Druker BJ (2003) Overcoming resistance to imatinib by combining targeted agents. Mol Cancer Ther 2:225-226.
13. Druker BJ, David A, and Karnofsky (2003) Award lecture. Imatinib as a paradigm of targeted therapies. J Clin Oncol 21:239s-245s.
14. Du J, Bernasconi P, Clauser KR, Mani DR, Finn SP, Beroukhim R, Burns M, Julian B, Peng XP, Hieronymus H, et al. (2009) Bead-based profiling of tyrosine kinase phosphorylation identifies SRC as a potential target for glioblastoma therapy. Nat Biotechnol 27:77-83.
15. Kantarjian H, Pasquini R, Hamerschlak N, Rousselot P, Holowiecki J, Jootar S, Robak T, Khoroshko N, Masszi T, Skotnicki A, et al. (2007) Dasatinib or high-dose imatinib for chronic-phase chronic myeloid leukemia after failure of first-line imatinib: a randomized phase 2 trial. Blood 109:5143-5150. (Pubitemid 46890528)
16. Leis JF, Stepan DE, Curtin PT, Ford JM, Peng B, Schubach S, Druker BJ, and Maziarz RT (2004) Central nervous system failure in patients with chronic myelogenous leukemia lymphoid blast crisis and Philadelphia chromosome positive acute lymphoblastic leukemia treated with imatinib (STI-571). Leuk Lymphoma 45:695-698. (Pubitemid 38256028)
17. Lombardo LJ, Lee FY, Chen P, Norris D, Barrish JC, Behnia K, Castaneda S, Cornelius LA, Das J, Doweyko AM, et al. (2004) Discovery of N-(2-chloro-6-methylphenyl)-2-(6-(4-(2-hydroxyethyl)-piperazin-1-yl) -2-methylpyrimidin-4-ylamino) thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. J Med Chem 47:6658-6661. (Pubitemid 40053752)
18. Milano V, Piao Y, LaFortune T, and de Groot J (2009) Dasatinib-induced autophagy is enhanced in combination with temozolomide in glioma. Mol Cancer Ther 8:394-406.
19. Nam S, Kim D, Cheng JQ, Zhang S, Lee JH, Buettner R, Mirosevich J, Lee FY, and Jove R (2005) Action of the Src family kinase inhibitor, dasatinib (BMS-354825), on human prostate cancer cells. Cancer Res 65:9185-9189. (Pubitemid 41507982)
20. Neville K, Parise RA, Thompson P, Aleksic A, Egorin MJ, Balis FM, McGuffey L, McCully C, Berg SL, and Blaney SM (2004) Plasma and cerebrospinal fluid pharmacokinetics of imatinib after administration to nonhuman primates. Clin Cancer Res 10:2525-2529. (Pubitemid 38445714)
21. Ottmann O, Dombret H, Martinelli G, Simonsson B, Guilhot F, Larson RA, Rege-Cambrin G, Radich J, Hochhaus A, Apanovitch AM, et al. (2007) Dasatinib induces rapid hematologic and cytogenetic responses in adult patients with Philadelphia chromosome positive acute lymphoblastic leukemia with resistance or intolerance to imatinib: interim results of a phase 2 study. Blood 110:2309-2315. (Pubitemid 47523149)
22. Ottmann OG, Druker BJ, Sawyers CL, Goldman JM, Reiffers J, Silver RT, Tura S, Fischer T, Deininger MW, Schiffer CA, et al. (2002) A phase 2 study of imatinib in patients with relapsed or refractory Philadelphia chromosome-positive acute. Blood 100:1965-1971. (Pubitemid 35001224)
23. Polli JW, Olson KL, Chism JP, John-Williams LS, Yeager RL, Woodard SM, Otto V, Castellino S, and Demby VE (2009) An unexpected synergist role of P-glycoprotein and breast cancer resistance protein on the central nervous system penetration of the tyrosine kinase inhibitor lapatinib (N-{3-chloro-4- (3-fluorobenzyl)oxyphenyl}-6 -5-({2-(methylsulfonyl)ethy lamino}methyl)-2-furyl- 4-quinazolinamine; GW572016). Drug Metab Dispos 37:439-442.
24. Porkka K, Koskenvesa P, Lundán T, Rimpiläinen J, Mustjoki S, Smykla R, Wild R, Luo R, Arnan M, Brethon B, et al. (2008) Dasatinib crosses the blood-brain barrier and is an efficient therapy for central nervous system Philadelphia chromosome-positive leukemia. Blood 112:1005-1012.
25. Ptasznik A, Nakata Y, Kalota A, Emerson SG, and Gewirtz AM (2004) Short interfering RNA (siRNA) targeting the Lyn kinase induces apoptosis in primary, and drug-resistant, BCR-ABL1(+) leukemia cells. Nat Med 10:1187-1189. (Pubitemid 39540433)
26. Quintás-Cardama A, Kantarjian H, and Cortes J (2007) Flying under the radar: the new wave of BCR-ABL inhibitors. Nat Rev Drug Discov 6:834-848. (Pubitemid 47500507)
27. Rajappa S, Uppin SG, Raghunadharao D, Rao IS, and Surath A (2004) Isolated central nervous system blast crisis in chronic myeloid leukemia. Hematol Oncol 22:179-181. (Pubitemid 41342409)
28. Sawyers CL, Hochhaus A, Feldman E, Goldman JM, Miller CB, Ottmann OG, Schiffer CA, Talpaz M, Guilhot F, Deininger MW, et al. (2002) Imatinib induces hematologic and cytogenetic responses in patients with chronic myelogenous leukemia in myeloid blast crisis: results of a phase II study. Blood 99:3530-3539. (Pubitemid 34534519)
29. Shah NP (2007) Medical management of CML. Hematology Am Soc Hematol Educ Program 2007:371-375.