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Items: 1 to 50 of 249

1.

P-glycoprotein (ABCB1/MDR1) limits brain accumulation and Cytochrome P450-3A (CYP3A) restricts oral availability of the novel FGFR4 inhibitor fisogatinib (BLU-554).

Li W, Sparidans R, El-Lari M, Wang Y, Lebre MC, Beijnen JH, Schinkel AH.

Int J Pharm. 2019 Nov 20:118842. doi: 10.1016/j.ijpharm.2019.118842. [Epub ahead of print]

PMID:
31759109
2.

Metabolome Analysis Reveals Dermal Histamine Accumulation in Murine Dermatitis Provoked by Genetic Deletion of P-Glycoprotein and Breast Cancer Resistance Protein.

Hashimoto N, Nakamichi N, Nanmo H, Kimura KI, Masuo Y, Sakai Y, Schinkel AH, Sato S, Soga T, Kato Y.

Pharm Res. 2019 Sep 11;36(11):158. doi: 10.1007/s11095-019-2695-3.

PMID:
31512001
3.

Development and validation of an LC-MS/MS method with a broad linear dynamic range for the quantification of tivozanib in human and mouse plasma, mouse tissue homogenates, and culture medium.

Bruin MAC, Rosing H, Lucas L, Wang J, Huitema ADR, Schinkel AH, Beijnen JH.

J Chromatogr B Analyt Technol Biomed Life Sci. 2019 Sep 1;1125:121723. doi: 10.1016/j.jchromb.2019.121723. Epub 2019 Jul 18.

PMID:
31352204
4.

P-glycoprotein Limits Ribociclib Brain Exposure and CYP3A4 Restricts Its Oral Bioavailability.

Martínez-Chávez A, van Hoppe S, Rosing H, Lebre MC, Tibben M, Beijnen JH, Schinkel AH.

Mol Pharm. 2019 Sep 3;16(9):3842-3852. doi: 10.1021/acs.molpharmaceut.9b00475. Epub 2019 Aug 5.

PMID:
31329454
5.

Cytochrome P450 3A4, 3A5, and 2C8 expression in breast, prostate, lung, endometrial, and ovarian tumors: relevance for resistance to taxanes.

van Eijk M, Boosman RJ, Schinkel AH, Huitema ADR, Beijnen JH.

Cancer Chemother Pharmacol. 2019 Sep;84(3):487-499. doi: 10.1007/s00280-019-03905-3. Epub 2019 Jul 15. Review.

6.

P-glycoprotein (MDR1/ABCB1) controls brain accumulation and intestinal disposition of the novel TGF-β 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
7.

Development and validation of a bioanalytical method for the quantification of the CDK4/6 inhibitors abemaciclib, palbociclib, and ribociclib in human and mouse matrices using liquid chromatography-tandem mass spectrometry.

Martínez-Chávez A, Rosing H, Hillebrand M, Tibben M, Schinkel AH, Beijnen JH.

Anal Bioanal Chem. 2019 Aug;411(20):5331-5345. doi: 10.1007/s00216-019-01932-w. Epub 2019 Jun 17.

8.

Brain accumulation of osimertinib and its active metabolite AZ5104 is restricted by ABCB1 (P-glycoprotein) and ABCG2 (breast cancer resistance protein).

van Hoppe S, Jamalpoor A, Rood JJM, Wagenaar E, Sparidans RW, Beijnen JH, Schinkel AH.

Pharmacol Res. 2019 Aug;146:104297. doi: 10.1016/j.phrs.2019.104297. Epub 2019 Jun 5.

PMID:
31175939
9.

Bioanalytical assay for the novel TRK inhibitor selitrectinib in mouse plasma and tissue homogenates using liquid chromatography-tandem mass spectrometry.

Sparidans RW, Li W, Schinkel AH, Beijnen JH.

J Chromatogr B Analyt Technol Biomed Life Sci. 2019 Aug 1;1122-1123:78-82. doi: 10.1016/j.jchromb.2019.05.026. Epub 2019 May 27.

10.

Liquid chromatography-tandem mass spectrometric assay for the quantification of galunisertib in human plasma and the application in a pre-clinical study.

Tibben MM, Huijberts S, Li W, Schinkel AH, Gebretensae A, Rosing H, Beijnen JH.

J Pharm Biomed Anal. 2019 Sep 5;173:169-175. doi: 10.1016/j.jpba.2019.05.037. Epub 2019 May 21.

PMID:
31146172
11.

Quantification of FGFR4 inhibitor BLU-554 in mouse plasma and tissue homogenates using liquid chromatography-tandem mass spectrometry.

Dogan-Topal B, Li W, Schinkel AH, Beijnen JH, Sparidans RW.

J Chromatogr B Analyt Technol Biomed Life Sci. 2019 Mar 15;1110-1111:116-123. doi: 10.1016/j.jchromb.2019.02.017. Epub 2019 Feb 16.

12.

ABC transporters Mdr1a/1b, Bcrp1, Mrp2 and Mrp3 determine the sensitivity to PhIP/DSS-induced colon carcinogenesis and inflammation.

Durmus S, van der Valk M, Teunissen SF, Song JY, Wagenaar E, Beijnen JH, Schinkel AH.

Arch Toxicol. 2019 Mar;93(3):775-790. doi: 10.1007/s00204-019-02394-w. Epub 2019 Jan 30.

PMID:
30701287
13.

Oral coadministration of elacridar and ritonavir enhances brain accumulation and oral availability of the novel ALK/ROS1 inhibitor lorlatinib.

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

Eur J Pharm Biopharm. 2019 Mar;136:120-130. doi: 10.1016/j.ejpb.2019.01.016. Epub 2019 Jan 17.

PMID:
30660696
14.

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
15.

Quantitative bioanalytical assay for the tropomyosin receptor kinase inhibitor larotrectinib in mouse plasma and tissue homogenates using liquid chromatography-tandem mass spectrometry.

Sparidans RW, Wang Y, Schinkel AH, Schellens JHM, Beijnen JH.

J Chromatogr B Analyt Technol Biomed Life Sci. 2018 Dec 1;1102-1103:167-172. doi: 10.1016/j.jchromb.2018.10.023. Epub 2018 Oct 30.

16.

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
17.

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
18.

Bioanalytical liquid chromatography-tandem mass spectrometric assay for the quantification of the ALK inhibitors alectinib, brigatinib and lorlatinib in plasma and mouse tissue homogenates.

Sparidans RW, Li W, Schinkel AH, Schellens JHM, Beijnen JH.

J Pharm Biomed Anal. 2018 Nov 30;161:136-143. doi: 10.1016/j.jpba.2018.08.038. Epub 2018 Aug 19.

PMID:
30149189
19.

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.

20.

Bioanalytical assay for the quantification of the ALK inhibitor lorlatinib in mouse plasma using liquid chromatography-tandem mass spectrometry.

Spatari C, Li W, Schinkel AH, Ragno G, Schellens JHM, Beijnen JH, Sparidans RW.

J Chromatogr B Analyt Technol Biomed Life Sci. 2018 Apr 15;1083:204-208. doi: 10.1016/j.jchromb.2018.03.014. Epub 2018 Mar 9.

21.

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
22.

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
23.

Liquid chromatography-tandem mass spectrometric assay for the quantitative determination of the tyrosine kinase inhibitor quizartinib in mouse plasma using salting-out liquid-liquid extraction.

Retmana IA, Wang J, Schinkel AH, Schellens JHM, Beijnen JH, Sparidans RW.

J Chromatogr B Analyt Technol Biomed Life Sci. 2017 Sep 1;1061-1062:300-305. doi: 10.1016/j.jchromb.2017.07.034. Epub 2017 Jul 23.

24.

What next? Preferably development of drugs that are no longer transported by the ABCB1 and ABCG2 efflux transporters.

van Hoppe S, Schinkel AH.

Pharmacol Res. 2017 Sep;123:144. doi: 10.1016/j.phrs.2017.05.015. Epub 2017 May 31. No abstract available.

PMID:
28578203
25.

Ochratoxin A transport by the human breast cancer resistance protein (BCRP), multidrug resistance protein 2 (MRP2), and organic anion-transporting polypeptides 1A2, 1B1 and 2B1.

Qi X, Wagenaar E, Xu W, Huang K, Schinkel AH.

Toxicol Appl Pharmacol. 2017 Aug 15;329:18-25. doi: 10.1016/j.taap.2017.05.022. Epub 2017 May 19.

PMID:
28532671
26.

Hepatic uptake of conjugated bile acids is mediated by both sodium taurocholate cotransporting polypeptide and organic anion transporting polypeptides and modulated by intestinal sensing of plasma bile acid levels in mice.

Slijepcevic D, Roscam Abbing RLP, Katafuchi T, Blank A, Donkers JM, van Hoppe S, de Waart DR, Tolenaars D, van der Meer JHM, Wildenberg M, Beuers U, Oude Elferink RPJ, Schinkel AH, van de Graaf SFJ.

Hepatology. 2017 Nov;66(5):1631-1643. doi: 10.1002/hep.29251. Epub 2017 Sep 29.

27.

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
28.

P-Glycoprotein in skin contributes to transdermal absorption of topical corticosteroids.

Hashimoto N, Nakamichi N, Yamazaki E, Oikawa M, Masuo Y, Schinkel AH, Kato Y.

Int J Pharm. 2017 Apr 15;521(1-2):365-373. doi: 10.1016/j.ijpharm.2017.02.064. Epub 2017 Feb 24.

PMID:
28242377
29.

The impact of Organic Anion-Transporting Polypeptides (OATPs) on disposition and toxicity of antitumor drugs: Insights from knockout and humanized mice.

Durmus S, van Hoppe S, Schinkel AH.

Drug Resist Updat. 2016 Jul;27:72-88. doi: 10.1016/j.drup.2016.06.005. Epub 2016 Jun 25. Review.

PMID:
27449599
30.

Liquid chromatography-tandem mass spectrometric assay for ponatinib and N-desmethyl ponatinib in mouse plasma.

Sparidans RW, Kort A, Schinkel AH, Schellens JH, Beijnen JH.

J Chromatogr B Analyt Technol Biomed Life Sci. 2016 Jun 15;1023-1024:24-9. doi: 10.1016/j.jchromb.2016.04.049. Epub 2016 May 2.

PMID:
27179188
31.

Liquid chromatography-tandem mass spectrometric assay for the tyrosine kinase inhibitor afatinib in mouse plasma using salting-out liquid-liquid extraction.

Sparidans RW, van Hoppe S, Rood JJ, Schinkel AH, Schellens JH, Beijnen JH.

J Chromatogr B Analyt Technol Biomed Life Sci. 2016 Feb 15;1012-1013:118-23. doi: 10.1016/j.jchromb.2016.01.025. Epub 2016 Jan 21.

PMID:
26826475
32.

Liquid chromatography-tandem mass spectrometric assay for the simultaneous determination of the irreversible BTK inhibitor ibrutinib and its dihydrodiol-metabolite in plasma and its application in mouse pharmacokinetic studies.

Rood JJM, van Hoppe S, Schinkel AH, Schellens JHM, Beijnen JH, Sparidans RW.

J Pharm Biomed Anal. 2016 Jan 25;118:123-131. doi: 10.1016/j.jpba.2015.10.033. Epub 2015 Oct 27.

PMID:
26540627
33.

Preclinical Mouse Models To Study Human OATP1B1- and OATP1B3-Mediated Drug-Drug Interactions in Vivo.

Durmus S, Lozano-Mena G, van Esch A, Wagenaar E, van Tellingen O, Schinkel AH.

Mol Pharm. 2015 Dec 7;12(12):4259-69. doi: 10.1021/acs.molpharmaceut.5b00453. Epub 2015 Oct 29.

PMID:
26474710
34.

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
35.

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
36.

Ritonavir inhibits intratumoral docetaxel metabolism and enhances docetaxel antitumor activity in an immunocompetent mouse breast cancer model.

Hendrikx JJ, Lagas JS, Song JY, Rosing H, Schellens JH, Beijnen JH, Rottenberg S, Schinkel AH.

Int J Cancer. 2016 Feb 1;138(3):758-69. doi: 10.1002/ijc.29812. Epub 2015 Sep 21.

37.

Down-regulation of OATP1B proteins correlates with hyperbilirubinemia in advanced cholestasis.

Sticova E, Lodererova A, van de Steeg E, Frankova S, Kollar M, Lanska V, Kotalova R, Dedic T, Schinkel AH, Jirsa M.

Int J Clin Exp Pathol. 2015 May 1;8(5):5252-62. eCollection 2015.

38.

Hepatocellular Shuttling and Recirculation of Sorafenib-Glucuronide Is Dependent on Abcc2, Abcc3, and Oatp1a/1b.

Vasilyeva A, Durmus S, Li L, Wagenaar E, Hu S, Gibson AA, Panetta JC, Mani S, Sparreboom A, Baker SD, Schinkel AH.

Cancer Res. 2015 Jul 1;75(13):2729-36. doi: 10.1158/0008-5472.CAN-15-0280. Epub 2015 May 7.

39.

Apical ABC transporters and cancer chemotherapeutic drug disposition.

Durmus S, Hendrikx JJ, Schinkel AH.

Adv Cancer Res. 2015;125:1-41. doi: 10.1016/bs.acr.2014.10.001. Epub 2015 Jan 8. Review.

PMID:
25640265
40.

P-gp and taxanes.

Hendrikx JJ, Beijnen JH, Schinkel AH.

Oncoscience. 2014 Jun 19;1(7):478-9. eCollection 2014. No abstract available.

41.

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
42.

Brain organic cation transporter 2 controls response and vulnerability to stress and GSK3β signaling.

Couroussé T, Bacq A, Belzung C, Guiard B, Balasse L, Louis F, Le Guisquet AM, Gardier AM, Schinkel AH, Giros B, Gautron S.

Mol Psychiatry. 2015 Jul;20(7):889-900. doi: 10.1038/mp.2014.86. Epub 2014 Aug 5.

PMID:
25092247
43.

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
44.

Evaluation of organic anion transporting polypeptide 1B1 and 1B3 humanized mice as a translational model to study the pharmacokinetics of statins.

Salphati L, Chu X, Chen L, Prasad B, Dallas S, Evers R, Mamaril-Fishman D, Geier EG, Kehler J, Kunta J, Mezler M, Laplanche L, Pang J, Rode A, Soars MG, Unadkat JD, van Waterschoot RA, Yabut J, Schinkel AH, Scheer N.

Drug Metab Dispos. 2014 Aug;42(8):1301-13. doi: 10.1124/dmd.114.057976. Epub 2014 May 22.

PMID:
24855184
45.

Human OATP1B1, OATP1B3 and OATP1A2 can mediate the in vivo uptake and clearance of docetaxel.

Iusuf D, Hendrikx JJ, van Esch A, van de Steeg E, Wagenaar E, Rosing H, Beijnen JH, Schinkel AH.

Int J Cancer. 2015 Jan 1;136(1):225-33. doi: 10.1002/ijc.28970. Epub 2014 Jun 3.

46.

Quantification of taxanes in biological matrices: a review of bioanalytical assays and recommendations for development of new assays.

Hendrikx JJ, Rosing H, Schinkel AH, Schellens JH, Beijnen JH.

Bioanalysis. 2014 Apr;6(7):993-1010. doi: 10.4155/bio.14.48. Review.

PMID:
24806907
47.

Oral co-administration of elacridar and ritonavir enhances plasma levels of oral paclitaxel and docetaxel without affecting relative brain accumulation.

Hendrikx JJ, Lagas JS, Wagenaar E, Rosing H, Schellens JH, Beijnen JH, Schinkel AH.

Br J Cancer. 2014 May 27;110(11):2669-76. doi: 10.1038/bjc.2014.222. Epub 2014 Apr 29.

48.

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.

49.

Liquid chromatography-tandem mass spectrometric assay for the multikinase inhibitor regorafenib in plasma.

Luethi D, Durmus S, Schinkel AH, Schellens JH, Beijnen JH, Sparidans RW.

Biomed Chromatogr. 2014 Oct;28(10):1366-70. doi: 10.1002/bmc.3176. Epub 2014 Mar 12.

PMID:
24619951
50.

In vivo disposition of doxorubicin is affected by mouse Oatp1a/1b and human OATP1A/1B transporters.

Durmus S, Naik J, Buil L, Wagenaar E, van Tellingen O, Schinkel AH.

Int J Cancer. 2014 Oct 1;135(7):1700-10. doi: 10.1002/ijc.28797. Epub 2014 Mar 4.

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