P-glycoprotein (MDR1/ABCB1) and breast cancer resistance protein (BCRP/ABCG2) restrict brain accumulation of the JAK1/2 inhibitor, CYT387

Pharmacological Research

Volumn 76, Issue , 2013, Pages 9-16

  Durmus, S ^a   Xu, N ^a   Sparidans, R W ^b   Wagenaar, E ^a   Beijnen, J H ^b,c   Schinkel, A H ^a  

^a NETHERLANDS CANCER INSTITUTE   (Netherlands)

^b UTRECHT UNIVERSITY   (Netherlands)

^c SLOTERVAART HOSPITAL   (Netherlands)

Author keywords

BCRP; Brain accumulation; CYT387; JAK1 2 inhibitor; Oral availability; P glycoprotein

Indexed keywords

1,2,3,4,6,7,12,12A OCTAHYDRO 6 ISOBUTYL 9 METHOXY 1,4 DIOXOPYRAZINO[1',2':1,6]PYRIDO[3,4 B]INDOLE 3 PROPANOIC ACID TERT BUTYL ESTER; BREAST CANCER RESISTANCE PROTEIN; BREAST CANCER RESISTANCE PROTEIN 1; JANUS KINASE INHIBITOR; MOMELOTINIB; MULTIDRUG RESISTANCE PROTEIN 1; MULTIDRUG RESISTANCE PROTEIN 1A; MULTIDRUG RESISTANCE PROTEIN 1B; UNCLASSIFIED DRUG; ZOSUQUIDAR;

ANIMAL CELL; ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; BLOOD BRAIN BARRIER; CONTROLLED STUDY; DRUG ABSORPTION; DRUG ACCUMULATION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG DISTRIBUTION; DRUG EXPOSURE; DRUG PENETRATION; DRUG TRANSPORT; IN VITRO STUDY; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN BLOOD LEVEL; STRAIN DIFFERENCE; SYSTEMIC THERAPY; TIME TO MAXIMUM PLASMA CONCENTRATION;

AREA UNDER THE PLASMA CONCENTRATION-TIME CURVE; AUC; BBB; BCRP; BLOOD-BRAIN BARRIER; BRAIN ACCUMULATION; BREAST CANCER RESISTANCE PROTEIN; CMAX; CYT387; JAK1/2 INHIBITOR; MAXIMUM DRUG CONCENTRATION IN PLASMA; MDR1; MULTIDRUG RESISTANCE PROTEIN; ORAL AVAILABILITY; P-GLYCOPROTEIN; SD; STANDARD DEVIATION; THE TIME AFTER ADMINISTRATION OF A DRUG WHEN THE MAXIMUM PLASMA CONCENTRATION IS REACHED; TMAX;

ANIMALS; ATP-BINDING CASSETTE TRANSPORTERS; BENZAMIDES; BRAIN; CELL LINE; FEMALE; GENE DELETION; HUMANS; JANUS KINASE 1; JANUS KINASE 2; JANUS KINASES; MICE; NEOPLASM PROTEINS; P-GLYCOPROTEIN; P-GLYCOPROTEINS; PYRIMIDINES;

EID: 84882768125     PISSN: 10436618     EISSN: 10961186     Source Type: Journal    
DOI: 10.1016/j.phrs.2013.06.009     Document Type: Article

References (35)

1. J.S. Lagas, R.W. Sparidans, R.A. van Waterschoot, E. Wagenaar, J.H. Beijnen, and A.H. Schinkel P-glycoprotein limits oral availability, brain penetration, and toxicity of an anionic drug, the antibiotic salinomycin Antimicrobial Agents and Chemotherapy 52 2008 1034 1039 (Pubitemid 351358385)
2. L. Zhou, K. Schmidt, F.R. Nelson, V. Zelesky, M.D. Troutman, and B. Feng The effect of breast cancer resistance protein and P-glycoprotein on the brain penetration of flavopiridol, imatinib mesylate (Gleevec), prazosin, and 2-methoxy-3-(4-(2-(5-methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)propanoic acid (PF-407288) in mice Drug Metabolism and Disposition: The Biological Fate of Chemicals 37 2009 946 955
3. J.W. Polli, K.L. Olson, J.P. Chism, L.S. John-Williams, R.L. Yeager, and S.M. Woodard 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)oxy]phenyl}-6-[5- ({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine; GW572016) Drug Metabolism and Disposition: The Biological Fate of Chemicals 37 2009 439 442
4. S. Agarwal, R. Sane, J.L. Gallardo, J.R. Ohlfest, and W.F. Elmquist Distribution of gefitinib to the brain is limited by P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2)-mediated active efflux Journal of Pharmacology and Experimental Therapeutics 334 2010 147 155
5. H. Kodaira, H. Kusuhara, J. Ushiki, E. Fuse, and Y. Sugiyama Kinetic analysis of the cooperation of P-glycoprotein (P-gp/Abcb1) and breast cancer resistance protein (Bcrp/Abcg2) in limiting the brain and testis penetration of erlotinib, flavopiridol, and mitoxantrone Journal of Pharmacology and Experimental Therapeutics 333 2010 788 796
6. B. Poller, D. Iusuf, R.W. Sparidans, E. Wagenaar, J.H. Beijnen, and A.H. Schinkel Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics Drug Metabolism and Disposition: The Biological Fate of Chemicals 39 2011 729 735
7. S. Durmus, R.W. Sparidans, E. Wagenaar, J.H. Beijnen, and A.H. Schinkel Oral availability and brain penetration of the B-RAFV600E inhibitor vemurafenib can be enhanced by the P-GLYCOprotein (ABCB1) and breast cancer resistance protein (ABCG2) inhibitor elacridar Molecular Pharmacology 9 2012 3236 3245
8. R.K. Mittapalli, S. Vaidhyanathan, A.Z. Dudek, and W.F. Elmquist Mechanisms limiting distribution of the BRAFV600E inhibitor Dabrafenib to the brain: implications for the treatment of melanoma brain metastases Journal of Pharmacology and Experimental Therapeutics 344 3 2013 655 664
9. S.C. Tang, J.S. Lagas, N.A. Lankheet, B. Poller, M.J. Hillebrand, and H. Rosing Brain accumulation of sunitinib is restricted by P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and can be enhanced by oral elacridar and sunitinib coadministration International Journal of Cancer 130 2012 223 233
10. P.R. Lockman, R.K. Mittapalli, K.S. Taskar, V. Rudraraju, B. Gril, and K.A. Bohn Heterogeneous blood-tumor barrier permeability determines drug efficacy in experimental brain metastases of breast cancer Clinical Cancer Research 16 2010 5664 5678
11. K.S. Taskar, V. Rudraraju, R.K. Mittapalli, R. Samala, H.R. Thorsheim, and J. Lockman Lapatinib distribution in HER2 overexpressing experimental brain metastases of breast cancer Pharmaceutical Research 29 2012 770 781
12. R. Kralovics, F. Passamonti, A.S. Buser, S.S. Teo, R. Tiedt, and J.R. Passweg A gain-of-function mutation of JAK2 in myeloproliferative disorders New England Journal of Medicine 352 2005 1779 1790 (Pubitemid 40570926)
13. R.L. Levine, M. Wadleigh, J. Cools, B.L. Ebert, G. Wernig, and B.J. Huntly Activating mutation in the tyrosine kinase JAK2 in polycythemia vera, essential thrombocythemia, and myeloid metaplasia with myelofibrosis Cancer Cell 7 2005 387 397 (Pubitemid 40544655)
14. C.G. Mullighan, J. Zhang, R.C. Harvey, J.R. Collins-Underwood, B.A. Schulman, and L.A. Phillips JAK mutations in high-risk childhood acute lymphoblastic leukemia Proceedings of the National Academy of Sciences of the United States of America 106 2009 9414 9418
15. L.M. Scott, W. Tong, R.L. Levine, M.A. Scott, P.A. Beer, and M.R. Stratton JAK2 exon 12 mutations in polycythemia vera and idiopathic erythrocytosis New England Journal of Medicine 356 2007 459 468 (Pubitemid 46193073)
16. J.W. Tyner, T.G. Bumm, J. Deininger, L. Wood, K.J. Aichberger, and M.M. Loriaux CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms Blood 115 2010 5232 5240
17. A. Pardanani, and A. Tefferi Targeting myeloproliferative neoplasms with JAK inhibitors Current Opinion in Hematology 18 2011 105 110
18. B.L. Stein, J.D. Crispino, and A.R. Moliterno Janus kinase inhibitors: an update on the progress and promise of targeted therapy in the myeloproliferative neoplasms Current Opinion in Oncology 23 2011 609 616
19. C.J. Burns, D.G. Bourke, L. Andrau, X. Bu, S.A. Charman, and A.C. Donohue Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs) Bioorganic and Medicinal Chemistry Letters 19 2009 5887 5892
20. A. Pardanani, T. Lasho, G. Smith, C.J. Burns, E. Fantino, and A. Tefferi CYT387 a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients Leukemia 23 2009 1441 1445
21. K.A. Monaghan, T. Khong, C.J. Burns, and A. Spencer The novel JAK inhibitor CYT387 suppresses multiple signalling pathways, prevents proliferation and induces apoptosis in phenotypically diverse myeloma cells Leukemia 25 2011 1891 1899
22. A. Quintas-Cardama, H. Kantarjian, J. Cortes, and S. Verstovsek Janus kinase inhibitors for the treatment of myeloproliferative neoplasias and beyond Nature Reviews Drug Discovery 10 2011 127 140
23. R.W. Sparidans, S. Durmus, N. Xu, A.H. Schinkel, J.H. Schellens, and J.H. Beijnen Liquid chromatography-tandem mass spectrometric assay for the JAK2 inhibitor CYT387 in plasma Journal of chromatography B, Analytical Technologies in the Biomedical and Life Sciences 895-896 2012 174 177
24. J.S. Lagas, R.A. van Waterschoot, R.W. Sparidans, E. Wagenaar, J.H. Beijnen, and A.H. Schinkel Breast cancer resistance protein and P-glycoprotein limit sorafenib brain accumulation Molecular Cancer Therapeutics 9 2010 319 326
25. R.L. Oostendorp, T. Buckle, J.H. Beijnen, T.O. van, and J.H. Schellens The effect of P-gp (Mdr1a/1b), BCRP (Bcrp1) and P-gp/BCRP inhibitors on the in vivo absorption, distribution, metabolism and excretion of imatinib Investigational New Drugs 27 2009 31 40
26. J.S. Lagas, R.A. van Waterschoot, V.A. van Tilburg, M.J. Hillebrand, N. Lankheet, and H. Rosing Brain accumulation of dasatinib is restricted by P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and can be enhanced by elacridar treatment Clinical Cancer Research 15 2009 2344 2351
27. D. Damiani, M. Tiribelli, A. Michelutti, A. Geromin, M. Cavallin, and D. Fabbro Fludarabine-based induction therapy does not overcome the negative effect of ABCG2 (BCRP) over-expression in adult acute myeloid leukemia patients Leukemia Research 34 2010 942 945
28. M. Grundy, C. Seedhouse, N.H. Russell, and M. Pallis P-glycoprotein and breast cancer resistance protein in acute myeloid leukaemia cells treated with the aurora-B kinase inhibitor barasertib-hQPA BMC Cancer 11 2011 254
29. M. Tiribelli, A. Geromin, A. Michelutti, M. Cavallin, A. Pianta, and D. Fabbro Concomitant ABCG2 overexpression and FLT3-ITD mutation identify a subset of acute myeloid leukemia patients at high risk of relapse Cancer 117 2011 2156 2162
30. P.S. Chauhan, B. Bhushan, L.C. Singh, A.K. Mishra, S. Saluja, and V. Mittal Expression of genes related to multiple drug resistance and apoptosis in acute leukemia: response to induction chemotherapy Experimental and Molecular Pathology 92 2012 44 49
31. K.J. Aichberger, S. Herndlhofer, H. Agis, W.R. Sperr, H. Esterbauer, and W. Rabitsch Liposomal cytarabine for treatment of myeloid central nervous system relapse in chronic myeloid leukaemia occurring during imatinib therapy European Journal of Clinical Investigation 37 2007 808 813 (Pubitemid 47480846)
32. Y. Isobe, K. Sugimoto, A. Masuda, Y. Hamano, and K. Oshimi Central nervous system is a sanctuary site for chronic myelogenous leukaemia treated with imatinib mesylate Internal Medicine Journal 39 2009 408 411
33. D.L. Johnston, T.A. Alonzo, R.B. Gerbing, B.J. Lange, and W.G. Woods Risk factors and therapy for isolated central nervous system relapse of pediatric acute myeloid leukemia Journal of Clinical Oncology 23 2005 9172 9178
34. J.F. Leis, D.E. Stepan, P.T. Curtin, J.M. Ford, B. Peng, and S. Schubach 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) Leukemia and Lymphoma 45 2004 695 698 (Pubitemid 38256028)
35. K. Porkka, P. Koskenvesa, T. Lundan, J. Rimpilainen, S. Mustjoki, and R. Smykla Dasatinib crosses the blood-brain barrier and is an efficient therapy for central nervous system Philadelphia chromosome-positive leukemia Blood 112 2008 1005 1012