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Barriers to Effective Drug Treatment for Brain Metastases: A Multifactorial Problem in the Delivery of Precision Medicine.

Kim M, Kizilbash SH, Laramy JK, Gampa G, Parrish KE, Sarkaria JN, Elmquist WF.

Pharm Res. 2018 Jul 12;35(9):177. doi: 10.1007/s11095-018-2455-9. Review.


Efficacy of the MDM2 inhibitor SAR405838 in glioblastoma is limited by poor distribution across the blood-brain barrier.

Kim M, Ma DJ, Calligaris D, Zhang S, Feathers RW, Vaubel RA, Meaux I, Mladek AC, Parrish KE, Jin F, Barriere C, Debussche L, Watters J, Tian S, Decker PA, Eckel-Passow JE, Kitange GJ, Johnson AJ, Parney IF, Anastasiadis PZ, Agar NYR, Elmquist WF, Sarkaria JN.

Mol Cancer Ther. 2018 Jul 3. pii: molcanther.0600.2017. doi: 10.1158/1535-7163.MCT-17-0600. [Epub ahead of print]


Pharmacokinetic Assessment of Cooperative Efflux of the Multitargeted Kinase Inhibitor Ponatinib Across the Blood-Brain Barrier.

Laramy JK, Kim M, Parrish KE, Sarkaria JN, Elmquist WF.

J Pharmacol Exp Ther. 2018 May;365(2):249-261. doi: 10.1124/jpet.117.246116. Epub 2018 Feb 12.


Brain Distribution of a Novel MEK Inhibitor E6201: Implications in the Treatment of Melanoma Brain Metastases.

Gampa G, Kim M, Cook-Rostie N, Laramy JK, Sarkaria JN, Paradiso L, DePalatis L, Elmquist WF.

Drug Metab Dispos. 2018 May;46(5):658-666. doi: 10.1124/dmd.117.079194. Epub 2018 Feb 2.


Is the blood-brain barrier really disrupted in all glioblastomas? A critical assessment of existing clinical data.

Sarkaria JN, Hu LS, Parney IF, Pafundi DH, Brinkmann DH, Laack NN, Giannini C, Burns TC, Kizilbash SH, Laramy JK, Swanson KR, Kaufmann TJ, Brown PD, Agar NYR, Galanis E, Buckner JC, Elmquist WF.

Neuro Oncol. 2018 Jan 22;20(2):184-191. doi: 10.1093/neuonc/nox175.


Restricted Delivery of Talazoparib Across the Blood-Brain Barrier Limits the Sensitizing Effects of PARP Inhibition on Temozolomide Therapy in Glioblastoma.

Kizilbash SH, Gupta SK, Chang K, Kawashima R, Parrish KE, Carlson BL, Bakken KK, Mladek AC, Schroeder MA, Decker PA, Kitange GJ, Shen Y, Feng Y, Protter AA, Elmquist WF, Sarkaria JN.

Mol Cancer Ther. 2017 Dec;16(12):2735-2746. doi: 10.1158/1535-7163.MCT-17-0365. Epub 2017 Sep 25.


Heterogeneous Binding and Central Nervous System Distribution of the Multitargeted Kinase Inhibitor Ponatinib Restrict Orthotopic Efficacy in a Patient-Derived Xenograft Model of Glioblastoma.

Laramy JK, Kim M, Gupta SK, Parrish KE, Zhang S, Bakken KK, Carlson BL, Mladek AC, Ma DJ, Sarkaria JN, Elmquist WF.

J Pharmacol Exp Ther. 2017 Nov;363(2):136-147. doi: 10.1124/jpet.117.243477. Epub 2017 Aug 28.


Drug delivery to melanoma brain metastases: Can current challenges lead to new opportunities?

Gampa G, Vaidhyanathan S, Sarkaria JN, Elmquist WF.

Pharmacol Res. 2017 Sep;123:10-25. doi: 10.1016/j.phrs.2017.06.008. Epub 2017 Jun 17.


Challenges in the delivery of therapies to melanoma brain metastases.

Gampa G, Vaidhyanathan S, Resman BW, Parrish KE, Markovic SN, Sarkaria JN, Elmquist WF.

Curr Pharmacol Rep. 2016 Dec;2(6):309-325. doi: 10.1007/s40495-016-0072-z. Epub 2016 Nov 9.


ABCG2 and ABCB1 Limit the Efficacy of Dasatinib in a PDGF-B-Driven Brainstem Glioma Model.

Mittapalli RK, Chung AH, Parrish KE, Crabtree D, Halvorson KG, Hu G, Elmquist WF, Becher OJ.

Mol Cancer Ther. 2016 May;15(5):819-29. doi: 10.1158/1535-7163.MCT-15-0093. Epub 2016 Feb 16.


Factors Influencing the Central Nervous System Distribution of a Novel Phosphoinositide 3-Kinase/Mammalian Target of Rapamycin Inhibitor GSK2126458: Implications for Overcoming Resistance with Combination Therapy for Melanoma Brain Metastases.

Vaidhyanathan S, Wilken-Resman B, Ma DJ, Parrish KE, Mittapalli RK, Carlson BL, Sarkaria JN, Elmquist WF.

J Pharmacol Exp Ther. 2016 Feb;356(2):251-9. doi: 10.1124/jpet.115.229393. Epub 2015 Nov 24.


Efficacy of PARP Inhibitor Rucaparib in Orthotopic Glioblastoma Xenografts Is Limited by Ineffective Drug Penetration into the Central Nervous System.

Parrish KE, Cen L, Murray J, Calligaris D, Kizilbash S, Mittapalli RK, Carlson BL, Schroeder MA, Sludden J, Boddy AV, Agar NY, Curtin NJ, Elmquist WF, Sarkaria JN.

Mol Cancer Ther. 2015 Dec;14(12):2735-43. doi: 10.1158/1535-7163.MCT-15-0553. Epub 2015 Oct 5.


CNS Anticancer Drug Discovery and Development Conference White Paper.

Levin VA, Tonge PJ, Gallo JM, Birtwistle MR, Dar AC, Iavarone A, Paddison PJ, Heffron TP, Elmquist WF, Lachowicz JE, Johnson TW, White FM, Sul J, Smith QR, Shen W, Sarkaria JN, Samala R, Wen PY, Berry DA, Petter RC.

Neuro Oncol. 2015 Nov;17 Suppl 6:vi1-26. doi: 10.1093/neuonc/nov169.


Strategies to improve delivery of anticancer drugs across the blood-brain barrier to treat glioblastoma.

Oberoi RK, Parrish KE, Sio TT, Mittapalli RK, Elmquist WF, Sarkaria JN.

Neuro Oncol. 2016 Jan;18(1):27-36. doi: 10.1093/neuonc/nov164. Epub 2015 Sep 10. Review.


Efflux transporters at the blood-brain barrier limit delivery and efficacy of cyclin-dependent kinase 4/6 inhibitor palbociclib (PD-0332991) in an orthotopic brain tumor model.

Parrish KE, Pokorny J, Mittapalli RK, Bakken K, Sarkaria JN, Elmquist WF.

J Pharmacol Exp Ther. 2015 Nov;355(2):264-71. doi: 10.1124/jpet.115.228213. Epub 2015 Sep 9.


Decreased affinity for efflux transporters increases brain penetrance and molecular targeting of a PI3K/mTOR inhibitor in a mouse model of glioblastoma.

Becker CM, Oberoi RK, McFarren SJ, Muldoon DM, Pafundi DH, Pokorny JL, Brinkmann DH, Ohlfest JR, Sarkaria JN, Largaespada DA, Elmquist WF.

Neuro Oncol. 2015 Sep;17(9):1210-9. doi: 10.1093/neuonc/nov081. Epub 2015 May 12.


Improving drug delivery to primary and metastatic brain tumors: strategies to overcome the blood-brain barrier.

Parrish KE, Sarkaria JN, Elmquist WF.

Clin Pharmacol Ther. 2015 Apr;97(4):336-46. doi: 10.1002/cpt.71. Epub 2015 Feb 18. Review.


The Efficacy of the Wee1 Inhibitor MK-1775 Combined with Temozolomide Is Limited by Heterogeneous Distribution across the Blood-Brain Barrier in Glioblastoma.

Pokorny JL, Calligaris D, Gupta SK, Iyekegbe DO Jr, Mueller D, Bakken KK, Carlson BL, Schroeder MA, Evans DL, Lou Z, Decker PA, Eckel-Passow JE, Pucci V, Ma B, Shumway SD, Elmquist WF, Agar NY, Sarkaria JN.

Clin Cancer Res. 2015 Apr 15;21(8):1916-24. doi: 10.1158/1078-0432.CCR-14-2588. Epub 2015 Jan 21.


Impact of BRAF mutation and BRAF inhibition on melanoma brain metastases.

Gummadi T, Zhang BY, Valpione S, Kim C, Kottschade LA, Mittapalli RK, Chiarion-Sileni V, Pigozzo J, Elmquist WF, Dudek AZ.

Melanoma Res. 2015 Feb;25(1):75-9. doi: 10.1097/CMR.0000000000000133.


Factors influencing the CNS distribution of a novel MEK-1/2 inhibitor: implications for combination therapy for melanoma brain metastases.

Vaidhyanathan S, Mittapalli RK, Sarkaria JN, Elmquist WF.

Drug Metab Dispos. 2014 Aug;42(8):1292-300. doi: 10.1124/dmd.114.058339. Epub 2014 May 29.


Sunitinib LC-MS/MS Assay in Mouse Plasma and Brain Tissue: Application in CNS Distribution Studies.

Oberoi RK, Mittapalli RK, Fisher J, Elmquist WF.

Chromatographia. 2013 Dec 1;76(23-24). doi: 10.1007/s10337-013-2528-1.


Pharmacokinetic assessment of efflux transport in sunitinib distribution to the brain.

Oberoi RK, Mittapalli RK, Elmquist WF.

J Pharmacol Exp Ther. 2013 Dec;347(3):755-64. doi: 10.1124/jpet.113.208959. Epub 2013 Oct 10.


Saturable active efflux by p-glycoprotein and breast cancer resistance protein at the blood-brain barrier leads to nonlinear distribution of elacridar to the central nervous system.

Sane R, Agarwal S, Mittapalli RK, Elmquist WF.

J Pharmacol Exp Ther. 2013 Apr;345(1):111-24. doi: 10.1124/jpet.112.199786. Epub 2013 Feb 8.


Development and evaluation of a novel microemulsion formulation of elacridar to improve its bioavailability.

Sane R, Mittapalli RK, Elmquist WF.

J Pharm Sci. 2013 Apr;102(4):1343-54. doi: 10.1002/jps.23450. Epub 2013 Jan 18.


Brain efflux index to investigate the influence of active efflux on brain distribution of pemetrexed and methotrexate.

Li L, Agarwal S, Elmquist WF.

Drug Metab Dispos. 2013 Mar;41(3):659-67. doi: 10.1124/dmd.112.049254. Epub 2013 Jan 7.


Brain metastases from renal cell carcinoma in the era of tyrosine kinase inhibitors.

Dudek AZ, Raza A, Chi M, Singhal M, Oberoi R, Mittapalli RK, Agarwal S, Elmquist WF.

Clin Genitourin Cancer. 2013 Jun;11(2):155-60. doi: 10.1016/j.clgc.2012.11.001. Epub 2012 Dec 21.


Mechanisms limiting distribution of the threonine-protein kinase B-RaF(V600E) inhibitor dabrafenib to the brain: implications for the treatment of melanoma brain metastases.

Mittapalli RK, Vaidhyanathan S, Dudek AZ, Elmquist WF.

J Pharmacol Exp Ther. 2013 Mar;344(3):655-64. doi: 10.1124/jpet.112.201475. Epub 2012 Dec 17.


Function of the blood-brain barrier and restriction of drug delivery to invasive glioma cells: findings in an orthotopic rat xenograft model of glioma.

Agarwal S, Manchanda P, Vogelbaum MA, Ohlfest JR, Elmquist WF.

Drug Metab Dispos. 2013 Jan;41(1):33-9. doi: 10.1124/dmd.112.048322. Epub 2012 Sep 26.


Active efflux of Dasatinib from the brain limits efficacy against murine glioblastoma: broad implications for the clinical use of molecularly targeted agents.

Agarwal S, Mittapalli RK, Zellmer DM, Gallardo JL, Donelson R, Seiler C, Decker SA, Santacruz KS, Pokorny JL, Sarkaria JN, Elmquist WF, Ohlfest JR.

Mol Cancer Ther. 2012 Oct;11(10):2183-92. doi: 10.1158/1535-7163.MCT-12-0552. Epub 2012 Aug 13.


Brain distribution and bioavailability of elacridar after different routes of administration in the mouse.

Sane R, Agarwal S, Elmquist WF.

Drug Metab Dispos. 2012 Aug;40(8):1612-9. doi: 10.1124/dmd.112.045930. Epub 2012 May 18.


Impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on the brain distribution of a novel BRAF inhibitor: vemurafenib (PLX4032).

Mittapalli RK, Vaidhyanathan S, Sane R, Elmquist WF.

J Pharmacol Exp Ther. 2012 Jul;342(1):33-40. doi: 10.1124/jpet.112.192195. Epub 2012 Mar 27.


Quantitative proteomics of transporter expression in brain capillary endothelial cells isolated from P-glycoprotein (P-gp), breast cancer resistance protein (Bcrp), and P-gp/Bcrp knockout mice.

Agarwal S, Uchida Y, Mittapalli RK, Sane R, Terasaki T, Elmquist WF.

Drug Metab Dispos. 2012 Jun;40(6):1164-9. doi: 10.1124/dmd.112.044719. Epub 2012 Mar 8.


Brain distribution of cediranib is limited by active efflux at the blood-brain barrier.

Wang T, Agarwal S, Elmquist WF.

J Pharmacol Exp Ther. 2012 May;341(2):386-95. doi: 10.1124/jpet.111.190488. Epub 2012 Feb 8.


Determination of cediranib in mouse plasma and brain tissue using high-performance liquid chromatography-mass spectrometry.

Wang T, Oberoi RK, Elmquist WF.

J Chromatogr B Analyt Technol Biomed Life Sci. 2011 Dec 15;879(32):3812-7. doi: 10.1016/j.jchromb.2011.10.025. Epub 2011 Oct 29.


Cardiac responses to the intrapericardial delivery of metoprolol: targeted delivery compared to intravenous administration.

Richardson ES, Rolfes C, Woo OS, Elmquist WF, Benditt DG, Iaizzo PA.

J Cardiovasc Transl Res. 2012 Aug;5(4):535-40. doi: 10.1007/s12265-011-9315-x. Epub 2011 Aug 30.


Breast cancer resistance protein and P-glycoprotein in brain cancer: two gatekeepers team up.

Agarwal S, Hartz AM, Elmquist WF, Bauer B.

Curr Pharm Des. 2011;17(26):2793-802. Review.


Delivery of molecularly targeted therapy to malignant glioma, a disease of the whole brain.

Agarwal S, Sane R, Oberoi R, Ohlfest JR, Elmquist WF.

Expert Rev Mol Med. 2011 May 13;13:e17. doi: 10.1017/S1462399411001888. Review.


pH-Dependent transport of pemetrexed by breast cancer resistance protein.

Li L, Sham YY, Bikadi Z, Elmquist WF.

Drug Metab Dispos. 2011 Sep;39(9):1478-85. doi: 10.1124/dmd.111.039370. Epub 2011 May 31.


OCT2 and MATE1 provide bidirectional agmatine transport.

Winter TN, Elmquist WF, Fairbanks CA.

Mol Pharm. 2011 Feb 7;8(1):133-42. doi: 10.1021/mp100180a. Epub 2010 Dec 3.


The role of the breast cancer resistance protein (ABCG2) in the distribution of sorafenib to the brain.

Agarwal S, Sane R, Ohlfest JR, Elmquist WF.

J Pharmacol Exp Ther. 2011 Jan;336(1):223-33. doi: 10.1124/jpet.110.175034. Epub 2010 Oct 15.


Distribution of gefitinib to the brain is limited by P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2)-mediated active efflux.

Agarwal S, Sane R, Gallardo JL, Ohlfest JR, Elmquist WF.

J Pharmacol Exp Ther. 2010 Jul;334(1):147-55. doi: 10.1124/jpet.110.167601. Epub 2010 Apr 26.


Organic cation uptake is enhanced in bcrp1-transfected MDCKII cells.

Pan G, Winter TN, Roberts JC, Fairbanks CA, Elmquist WF.

Mol Pharm. 2010 Feb 1;7(1):138-45. doi: 10.1021/mp900177r.


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

Chen Y, Agarwal S, Shaik NM, Chen C, Yang Z, Elmquist WF.

J Pharmacol Exp Ther. 2009 Sep;330(3):956-63. doi: 10.1124/jpet.109.154781. Epub 2009 Jun 2.


Substrate-dependent breast cancer resistance protein (Bcrp1/Abcg2)-mediated interactions: consideration of multiple binding sites in in vitro assay design.

Giri N, Agarwal S, Shaik N, Pan G, Chen Y, Elmquist WF.

Drug Metab Dispos. 2009 Mar;37(3):560-70. doi: 10.1124/dmd.108.022046. Epub 2008 Dec 4.


Investigation of the role of breast cancer resistance protein (Bcrp/Abcg2) on pharmacokinetics and central nervous system penetration of abacavir and zidovudine in the mouse.

Giri N, Shaik N, Pan G, Terasaki T, Mukai C, Kitagaki S, Miyakoshi N, Elmquist WF.

Drug Metab Dispos. 2008 Aug;36(8):1476-84. doi: 10.1124/dmd.108.020974. Epub 2008 Apr 28.


Interactions of pluronic block copolymers on P-gp efflux activity: experience with HIV-1 protease inhibitors.

Shaik N, Pan G, Elmquist WF.

J Pharm Sci. 2008 Dec;97(12):5421-33. doi: 10.1002/jps.21372.


P-glycoprotein-mediated active efflux of the anti-HIV1 nucleoside abacavir limits cellular accumulation and brain distribution.

Shaik N, Giri N, Pan G, Elmquist WF.

Drug Metab Dispos. 2007 Nov;35(11):2076-85. Epub 2007 Aug 20.

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