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In vitro characterization of axitinib interactions with human efflux and hepatic uptake transporters: implications for disposition and drug interactions.

Reyner EL, Sevidal S, West MA, Clouser-Roche A, Freiwald S, Fenner K, Ullah M, Lee CA, Smith BJ.

Drug Metab Dispos. 2013 Aug;41(8):1575-83. doi: 10.1124/dmd.113.051193. Epub 2013 May 31.


Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics.

Poller B, Iusuf D, Sparidans RW, Wagenaar E, Beijnen JH, Schinkel AH.

Drug Metab Dispos. 2011 May;39(5):729-35. doi: 10.1124/dmd.110.037317. Epub 2011 Jan 31.


Characterization of efflux transporters involved in distribution and disposition of apixaban.

Zhang D, He K, Herbst JJ, Kolb J, Shou W, Wang L, Balimane PV, Han YH, Gan J, Frost CE, Humphreys WG.

Drug Metab Dispos. 2013 Apr;41(4):827-35. doi: 10.1124/dmd.112.050260. Epub 2013 Feb 4.


Multiple human isoforms of drug transporters contribute to the hepatic and renal transport of olmesartan, a selective antagonist of the angiotensin II AT1-receptor.

Yamada A, Maeda K, Kamiyama E, Sugiyama D, Kondo T, Shiroyanagi Y, Nakazawa H, Okano T, Adachi M, Schuetz JD, Adachi Y, Hu Z, Kusuhara H, Sugiyama Y.

Drug Metab Dispos. 2007 Dec;35(12):2166-76. Epub 2007 Sep 6.


Interaction Studies of Resolvin E1 Analog (RX-10045) with Efflux Transporters.

Cholkar K, Trinh HM, Vadlapudi AD, Wang Z, Pal D, Mitra AK.

J Ocul Pharmacol Ther. 2015 May;31(4):248-55. doi: 10.1089/jop.2014.0144. Epub 2015 Apr 6.


Lack of Interactions Between an Antisense Oligonucleotide with 2'-O-(2-Methoxyethyl) Modifications and Major Drug Transporters.

Yu RZ, Warren MS, Watanabe T, Nichols B, Jahic M, Huang J, Burkey J, Geary RS, Henry SP, Wang Y.

Nucleic Acid Ther. 2016 Apr;26(2):111-7. doi: 10.1089/nat.2015.0588. Epub 2016 Mar 9.


In vitro evaluation of potential drug interactions mediated by cytochrome P450 and transporters for luseogliflozin, an SGLT2 inhibitor.

Chino Y, Hasegawa M, Fukasawa Y, Mano Y, Bando K, Miyata A, Nakai Y, Endo H, Yamaguchi JI.

Xenobiotica. 2017 Apr;47(4):314-323. doi: 10.1080/00498254.2016.1193913. Epub 2016 Jun 20.


Evaluation of the endothelin receptor antagonists ambrisentan, bosentan, macitentan, and sitaxsentan as hepatobiliary transporter inhibitors and substrates in sandwich-cultured human hepatocytes.

Lepist EI, Gillies H, Smith W, Hao J, Hubert C, St Claire RL 3rd, Brouwer KR, Ray AS.

PLoS One. 2014 Jan 30;9(1):e87548. doi: 10.1371/journal.pone.0087548. eCollection 2014.


A new intestinal cell culture model to discriminate the relative contribution of P-gp and BCRP on transport of substrates such as imatinib.

Graber-Maier A, Gutmann H, Drewe J.

Mol Pharm. 2010 Oct 4;7(5):1618-28. doi: 10.1021/mp100040f. Epub 2010 Aug 11.


In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.

Reese MJ, Savina PM, Generaux GT, Tracey H, Humphreys JE, Kanaoka E, Webster LO, Harmon KA, Clarke JD, Polli JW.

Drug Metab Dispos. 2013 Feb;41(2):353-61. doi: 10.1124/dmd.112.048918. Epub 2012 Nov 6.


Zinc finger nuclease-mediated gene knockout results in loss of transport activity for P-glycoprotein, BCRP, and MRP2 in Caco-2 cells.

Sampson KE, Brinker A, Pratt J, Venkatraman N, Xiao Y, Blasberg J, Steiner T, Bourner M, Thompson DC.

Drug Metab Dispos. 2015 Feb;43(2):199-207. doi: 10.1124/dmd.114.057216. Epub 2014 Nov 11.


TKI combination therapy: strategy to enhance dasatinib uptake by inhibiting Pgp- and BCRP-mediated efflux.

D'Cunha R, Bae S, Murry DJ, An G.

Biopharm Drug Dispos. 2016 Oct;37(7):397-408. doi: 10.1002/bdd.2022. Epub 2016 Sep 13.


Raltegravir has a low propensity to cause clinical drug interactions through inhibition of major drug transporters: an in vitro evaluation.

Rizk ML, Houle R, Chan GH, Hafey M, Rhee EG, Chu X.

Antimicrob Agents Chemother. 2014;58(3):1294-301. doi: 10.1128/AAC.02049-13. Epub 2013 Dec 2.


Small intestinal efflux mediated by MRP2 and BCRP shifts sulfasalazine intestinal permeability from high to low, enabling its colonic targeting.

Dahan A, Amidon GL.

Am J Physiol Gastrointest Liver Physiol. 2009 Aug;297(2):G371-7. doi: 10.1152/ajpgi.00102.2009. Epub 2009 Jun 18.


Effects of aripiprazole and its active metabolite dehydroaripiprazole on the activities of drug efflux transporters expressed both in the intestine and at the blood-brain barrier.

Nagasaka Y, Oda K, Iwatsubo T, Kawamura A, Usui T.

Biopharm Drug Dispos. 2012 Sep;33(6):304-15. doi: 10.1002/bdd.1801. Epub 2012 Aug 18.


Effect of the ATP-binding cassette drug transporters ABCB1, ABCG2, and ABCC2 on erlotinib hydrochloride (Tarceva) disposition in in vitro and in vivo pharmacokinetic studies employing Bcrp1-/-/Mdr1a/1b-/- (triple-knockout) and wild-type mice.

Marchetti S, de Vries NA, Buckle T, Bolijn MJ, van Eijndhoven MA, Beijnen JH, Mazzanti R, van Tellingen O, Schellens JH.

Mol Cancer Ther. 2008 Aug;7(8):2280-7. doi: 10.1158/1535-7163.MCT-07-2250.


Biochemical interaction of anti-HCV telaprevir with the ABC transporters P-glycoprotein and breast cancer resistance protein.

Fujita Y, Noguchi K, Suzuki T, Katayama K, Sugimoto Y.

BMC Res Notes. 2013 Nov 6;6:445. doi: 10.1186/1756-0500-6-445.

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