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Items: 1 to 20 of 120

1.

P-Glycoprotein (MDR1/ABCB1) Restricts Brain Penetration of the Bruton's Tyrosine Kinase Inhibitor Ibrutinib, While Cytochrome P450-3A (CYP3A) Limits Its Oral Bioavailability.

van Hoppe S, Rood JJM, Buil L, Wagenaar E, Sparidans RW, Beijnen JH, Schinkel AH.

Mol Pharm. 2018 Nov 5;15(11):5124-5134. doi: 10.1021/acs.molpharmaceut.8b00702. Epub 2018 Oct 10.

PMID:
30247919
2.

P-glycoprotein and breast cancer resistance protein restrict brigatinib brain accumulation and toxicity, and, alongside CYP3A, limit its oral availability.

Li W, Sparidans RW, Wang Y, Lebre MC, Beijnen JH, Schinkel AH.

Pharmacol Res. 2018 Nov;137:47-55. doi: 10.1016/j.phrs.2018.09.020. Epub 2018 Sep 22.

PMID:
30253203
3.

P-glycoprotein (MDR1/ABCB1) and Breast Cancer Resistance Protein (BCRP/ABCG2) limit brain accumulation of the FLT3 inhibitor quizartinib in mice.

Wang J, Gan C, Retmana IA, Sparidans RW, Li W, Lebre MC, Beijnen JH, Schinkel AH.

Int J Pharm. 2019 Feb 10;556:172-180. doi: 10.1016/j.ijpharm.2018.12.014. Epub 2018 Dec 12.

PMID:
30553002
4.

P-glycoprotein (MDR1/ABCB1) restricts brain accumulation and cytochrome P450-3A (CYP3A) limits oral availability of the novel ALK/ROS1 inhibitor lorlatinib.

Li W, Sparidans RW, Wang Y, Lebre MC, Wagenaar E, Beijnen JH, Schinkel AH.

Int J Cancer. 2018 Oct 15;143(8):2029-2038. doi: 10.1002/ijc.31582. Epub 2018 Jul 10.

PMID:
29744867
5.

Brain and Testis Accumulation of Regorafenib is Restricted by Breast Cancer Resistance Protein (BCRP/ABCG2) and P-glycoprotein (P-GP/ABCB1).

Kort A, Durmus S, Sparidans RW, Wagenaar E, Beijnen JH, Schinkel AH.

Pharm Res. 2015 Jul;32(7):2205-16. doi: 10.1007/s11095-014-1609-7. Epub 2015 Jan 8.

PMID:
25563977
6.

Brain Accumulation of Ponatinib and Its Active Metabolite, N-Desmethyl Ponatinib, Is Limited by P-Glycoprotein (P-GP/ABCB1) and Breast Cancer Resistance Protein (BCRP/ABCG2).

Kort A, van Hoppe S, Sparidans RW, Wagenaar E, Beijnen JH, Schinkel AH.

Mol Pharm. 2017 Oct 2;14(10):3258-3268. doi: 10.1021/acs.molpharmaceut.7b00257. Epub 2017 Sep 19.

PMID:
28880088
7.

P-glycoprotein (MDR1/ABCB1) and Breast Cancer Resistance Protein (BCRP/ABCG2) affect brain accumulation and intestinal disposition of encorafenib in mice.

Wang J, Gan C, Sparidans RW, Wagenaar E, van Hoppe S, Beijnen JH, Schinkel AH.

Pharmacol Res. 2018 Mar;129:414-423. doi: 10.1016/j.phrs.2017.11.006. Epub 2017 Nov 14.

PMID:
29155017
8.

P-glycoprotein, CYP3A, and Plasma Carboxylesterase Determine Brain Disposition and Oral Availability of the Novel Taxane Cabazitaxel (Jevtana) in Mice.

Tang SC, Kort A, Cheung KL, Rosing H, Fukami T, Durmus S, Wagenaar E, Hendrikx JJ, Nakajima M, van Vlijmen BJ, Beijnen JH, Schinkel AH.

Mol Pharm. 2015 Oct 5;12(10):3714-23. doi: 10.1021/acs.molpharmaceut.5b00470. Epub 2015 Sep 15.

PMID:
26317243
9.

Brain accumulation of the EML4-ALK inhibitor ceritinib is restricted by P-glycoprotein (P-GP/ABCB1) and breast cancer resistance protein (BCRP/ABCG2).

Kort A, Sparidans RW, Wagenaar E, Beijnen JH, Schinkel AH.

Pharmacol Res. 2015 Dec;102:200-7. doi: 10.1016/j.phrs.2015.09.003. Epub 2015 Sep 8.

PMID:
26361725
10.

Effects of cytochrome P450 3A (CYP3A) and the drug transporters P-glycoprotein (MDR1/ABCB1) and MRP2 (ABCC2) on the pharmacokinetics of lopinavir.

van Waterschoot RA, ter Heine R, Wagenaar E, van der Kruijssen CM, Rooswinkel RW, Huitema AD, Beijnen JH, Schinkel AH.

Br J Pharmacol. 2010 Jul;160(5):1224-33. doi: 10.1111/j.1476-5381.2010.00759.x.

11.

Increased oral availability and brain accumulation of the ALK inhibitor crizotinib by coadministration of the P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) inhibitor elacridar.

Tang SC, Nguyen LN, Sparidans RW, Wagenaar E, Beijnen JH, Schinkel AH.

Int J Cancer. 2014 Mar 15;134(6):1484-94. doi: 10.1002/ijc.28475. Epub 2013 Oct 3.

12.

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.

Durmus S, Sparidans RW, Wagenaar E, Beijnen JH, Schinkel AH.

Mol Pharm. 2012 Nov 5;9(11):3236-45. doi: 10.1021/mp3003144. Epub 2012 Oct 18.

PMID:
23020847
13.

Breast cancer resistance protein (BCRP/ABCG2) and P-glycoprotein (P-gp/ABCB1) transport afatinib and restrict its oral availability and brain accumulation.

van Hoppe S, Sparidans RW, Wagenaar E, Beijnen JH, Schinkel AH.

Pharmacol Res. 2017 Jun;120:43-50. doi: 10.1016/j.phrs.2017.01.035. Epub 2017 Mar 10.

PMID:
28288939
14.

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.

Tang SC, Lagas JS, Lankheet NA, Poller B, Hillebrand MJ, Rosing H, Beijnen JH, Schinkel AH.

Int J Cancer. 2012 Jan 1;130(1):223-33. doi: 10.1002/ijc.26000. Epub 2011 Apr 7.

15.

P-glycoprotein, CYP3A, and plasma carboxylesterase determine brain and blood disposition of the mTOR Inhibitor everolimus (Afinitor) in mice.

Tang SC, Sparidans RW, Cheung KL, Fukami T, Durmus S, Wagenaar E, Yokoi T, van Vlijmen BJ, Beijnen JH, Schinkel AH.

Clin Cancer Res. 2014 Jun 15;20(12):3133-45. doi: 10.1158/1078-0432.CCR-13-1759. Epub 2014 Apr 11.

16.

Breast cancer resistance protein (BCRP/ABCG2) and P-glycoprotein (P-GP/ABCB1) restrict oral availability and brain accumulation of the PARP inhibitor rucaparib (AG-014699).

Durmus S, Sparidans RW, van Esch A, Wagenaar E, Beijnen JH, Schinkel AH.

Pharm Res. 2015 Jan;32(1):37-46. doi: 10.1007/s11095-014-1442-z. Epub 2014 Jun 25.

PMID:
24962512
17.

P-glycoprotein (MDR1/ABCB1) controls brain accumulation and intestinal disposition of the novel TGF-╬▓ signaling pathway inhibitor galunisertib.

Li W, Tibben M, Wang Y, Lebre MC, Rosing H, Beijnen JH, Schinkel AH.

Int J Cancer. 2019 Jul 15. doi: 10.1002/ijc.32568. [Epub ahead of print]

PMID:
31304590
18.

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.

PMID:
21282407
19.

Brain accumulation of dasatinib is restricted by P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and can be enhanced by elacridar treatment.

Lagas JS, van Waterschoot RA, van Tilburg VA, Hillebrand MJ, Lankheet N, Rosing H, Beijnen JH, Schinkel AH.

Clin Cancer Res. 2009 Apr 1;15(7):2344-51. doi: 10.1158/1078-0432.CCR-08-2253. Epub 2009 Mar 10.

20.

PET-CT imaging with [(18)F]-gefitinib to measure Abcb1a/1b (P-gp) and Abcg2 (Bcrp1) mediated drug-drug interactions at the murine blood-brain barrier.

Vlaming ML, L├Ąppchen T, Jansen HT, Kivits S, van Driel A, van de Steeg E, van der Hoorn JW, Sio CF, Steinbach OC, DeGroot J.

Nucl Med Biol. 2015 Nov;42(11):833-41. doi: 10.1016/j.nucmedbio.2015.07.004. Epub 2015 Jul 15.

PMID:
26264927

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