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

British Journal of Cancer

Volumn 110, Issue 11, 2014, Pages 2669-2676

  Hendrikx, J J M A ^a,b   Lagas, J S ^a   Wagenaar, E ^b   Rosing, H ^a   Schellens, J H M ^b,c   Beijnen, J H ^a,c   Schinkel, A H ^b  

^a SLOTERVAART HOSPITAL   (Netherlands)

^b NETHERLANDS CANCER INSTITUTE   (Netherlands)

^c UTRECHT UNIVERSITY   (Netherlands)

Author keywords

cytochrome P4503A (CYP3A4); docetaxel; oral bioavailability; P glycoprotein (P gp MDR1); paclitaxel

Indexed keywords

CYTOCHROME P450 3A4; DOCETAXEL; ELACRIDAR; PACLITAXEL; RITONAVIR;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; BIOAVAILABILITY; CONTROLLED STUDY; DRUG ACCUMULATION; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG EXPOSURE; DRUG INHIBITION; DRUG METABOLISM; DRUG UPTAKE; ENZYME SPECIFICITY; HUMAN; LIQUID CHROMATOGRAPHY; MOUSE; NONHUMAN; PLASMA CONCENTRATION-TIME CURVE; PRIORITY JOURNAL; RELATIVE BRAIN ACCUMULATION; TANDEM MASS SPECTROMETRY; TIME TO MAXIMUM PLASMA CONCENTRATION;

ACRIDINES; ADMINISTRATION, ORAL; ANIMALS; ANTINEOPLASTIC COMBINED CHEMOTHERAPY PROTOCOLS; AREA UNDER CURVE; BRAIN; HUMANS; MALE; MICE; MICE, KNOCKOUT; PACLITAXEL; RITONAVIR; TAXOIDS; TETRAHYDROISOQUINOLINES; TISSUE DISTRIBUTION;

EID: 84901592917     PISSN: 00070920     EISSN: 15321827     Source Type: Journal    
DOI: 10.1038/bjc.2014.222     Document Type: Article

References (37)

1. Bardelmeijer HA, Beijnen JH, Brouwer KR, Rosing H, Nooijen WJ, Schellens JH, van Tellingen O (2000) Increased oral bioavailability of paclitaxel by GF120918 in mice through selective modulation of P-glycoprotein. Clin Cancer Res 6: 4416-4421.
2. Bardelmeijer HA, Ouwehand M, Beijnen JH, Schellens JH, van Tellingen O (2004) Efficacy of novel P-glycoprotein inhibitors to increase the oral uptake of paclitaxel in mice. Invest New Drugs 22: 219-229.
3. Bardelmeijer HA, Ouwehand M, Buckle T, Huisman MT, Schellens JH, Beijnen JH, van Tellingen O (2002) Low systemic exposure of oral docetaxel in mice resulting from extensive first-pass metabolism is boosted by ritonavir. Cancer Res 62: 6158-6164.
4. Bosch TM, Meijerman I, Beijnen JH, Schellens JH (2006) Genetic polymorphisms of drug-metabolising enzymes and drug transporters in the chemotherapeutic treatment of cancer. Clin Pharmacokinet 45: 253-285.
5. di Masi A, De Marinis E, Ascenzi P, Marino M (2009) Nuclear receptors CAR and PXR: Molecular, functional, and biomedical aspects. Mol Aspects Med 30: 297-343.
6. Glaeser H, Fromm MF (2008) Animal models and intestinal drug transport. Exp Opin Drug Metab Toxicol 4: 347-361.
7. Gligorov J, Lotz JP (2004) Preclinical pharmacology of the taxanes: implications of the differences. Oncologist 9(Suppl 2): 3-8.
8. Gottesman MM, Ambudkar SV (2001) Overview: ABC transporters and human disease. J Bioenerg Biomembr 33: 453-458.
9. Hendrikx JJ, Lagas JS, Rosing H, Schellens JH, Beijnen JH, Schinkel AH (2013) P-glycoprotein and cytochrome P450 3A act together in restricting the oral bioavailability of paclitaxel. Int J Cancer 132: 2439-2447.
10. Jabir RS, Naidu R, Annuar MA, Ho GF, Munisamy M, Stanslas J (2012) Pharmacogenetics of taxanes: impact of gene polymorphisms of drug transporters on pharmacokinetics and toxicity. Pharmacogenomics 13: 1979-1988.
11. Jiang H, Tao W, Zhang M, Pan S, Kanwar JR, Sun X (2010) Low-dose metronomic paclitaxel chemotherapy suppresses breast tumors and metastases in mice. Cancer Invest 28: 74-84.
12. Kalvass JC, Polli JW, Bourdet DL, Feng B, Huang SM, Liu X, Smith QR, Zhang LK, Zamek-Gliszczynski MJ (2013) Why clinical modulation of efflux transport at the human blood-brain barrier is unlikely: the ITC evidence-based position. Clin Pharmacol Ther 94: 80-94.
13. Kemper EM, van Zandbergen AE, Cleypool C, Mos HA, BoogerdW, Beijnen JH, van Tellingen O (2003) Increased penetration of paclitaxel into the brain by inhibition of P-Glycoprotein. Clin Cancer Res 9: 2849-2855.
14. Koolen SL. Intravenous-to-oral switch in anticancer chemotherapy. Focus on taxanes and gemcitabine. Dissertation, Utrecht University: Utrecht, The Netherlands, 2011.
15. Koolen SL, Beijnen JH, Schellens JHM (2010a) Intravenous-to-oral switch in anticancer chemotherapy: a focus on docetaxel and paclitaxel. Clin Pharmacol Ther 87: 126-129.
16. Koolen SL, Oostendorp RL, Beijnen JH, Schellens JHM, Huitema AD (2010b) Population pharmacokinetics of intravenously and orally administered docetaxel with or without co-administration of ritonavir in patients with advanced cancer. Br J Clin Pharmacol 69: 465-474.
17. Kuppens IE, van Maanen MJ, Rosing H, Schellens JHM, Beijnen JH (2005) Quantitative analysis of docetaxel in human plasma using liquid chromatography coupled with tandem mass spectrometry. Biomed Chromatogr 19: 355-361.
18. Lagas JS, Vlaming ML, van Tellingen O, Wagenaar E, Jansen RS, Rosing H, Beijnen JH, Schinkel AH (2006) Multidrug resistance protein 2 is an important determinant of paclitaxel pharmacokinetics. Clin Cancer Res 12: 6125-6132.
19. Malingre MM, Beijnen JH, Rosing H, Koopman FJ, Jewell RC, Paul EM, ten Bokkel Huinink WW, Schellens JH (2001) Co-administration of GF120918 significantly increases the systemic exposure to oral paclitaxel in cancer patients. Br J Cancer 84: 42-47.
20. Marchetti S, Stuurman FE, Koolen SL, Moes JJ, Hendrikx JJ, Thijssen B, Huitema AD, Nuijen B, Rosing H, Keessen M, Voest EE, Mergui-Roelvink M, Beijnen JH, Schellens JH (2012) Phase I study of weekly oral docetaxel (ModraDoc001) plus ritonavir in patients with advanced solid tumors. ASCO Meeting Abstracts 30: 2550.
21. Meerum Terwogt JM, Beijnen JH, ten Bokkel Huinink WW, Rosing H, Schellens JH (1998) Co-administration of cyclosporin enables oral therapy with paclitaxel. Lancet 352: 285.
22. Oostendorp RL, Huitema A, Rosing H, Jansen RS, Ter Heine R, Keessen M, Beijnen JH, Schellens JHM (2009) Coadministration of ritonavir strongly enhances the apparent oral bioavailability of docetaxel in patients with solid tumors. Clin Cancer Res 15: 4228-4233.
23. Paine MF, Hart HL, Ludington SS, Haining RL, Rettie AE, Zeldin DC (2006) The human intestinal cytochrome P450 'pie'. Drug Metab Dispos 34: 880-886.
24. Quinney SK, Malireddy SR, Vuppalanchi R, Hamman MA, Chalasani N, Gorski JC, Hall SD (2013) Rate of onset of inhibition of gut-wall and hepatic CYP3A by clarithromycin. Eur J Clin Pharmacol 69: 439-448.
25. Schellens JHM, Malingre MM, Kruijtzer CM, Bardelmeijer HA, van Tellingen O, Schinkel AH, Beijnen JH (2000) Modulation of oral bioavailability of anticancer drugs: from mouse to man. Eur J Pharm Sci 12: 103-110.
26. Sparreboom A, van Asperen J, Mayer U, Schinkel AH, Smit JW, Meijer DK, Borst P, Nooijen WJ, Beijnen JH, van Tellingen O (1997) Limited oral bioavailability and active epithelial excretion of paclitaxel (Taxol) caused by P-glycoprotein in the intestine. Proc Natl Acad Sci USA 94: 2031-2035.
27. Stokvis E, Ouwehand M, Nan LG, Kemper EM, van Tellingen O, Rosing H, Beijnen JH (2004) A simple and sensitive assay for the quantitative analysis of paclitaxel in human and mouse plasma and brain tumor tissue using coupled liquid chromatography and tandem mass spectrometry. J Mass Spectrom 39: 1506-1512.
28. Stuurman FE, Nuijen B, Beijnen JH, Schellens JH (2013) Oral anticancer drugs: mechanisms of low bioavailability and strategies for improvement. Clin Pharmacokinet 52: 399-414.
29. Thelen K, Dressman JB (2009) Cytochrome P450-mediated metabolism in the human gut wall. J Pharm Pharmacol 61: 541-558.
30. Vaishampayan U, Parchment RE, Jasti BR, Hussain M (1999) Taxanes: an overview of the pharmacokinetics and pharmacodynamics. Urology 54: 22-29.
31. van Asperen J, van Tellingen O, Sparreboom A, Schinkel AH, Borst P, Nooijen WJ, Beijnen JH (1997) Enhanced oral bioavailability of paclitaxel in mice treated with the P-glycoprotein blocker SDZ PSC 833. Br J Cancer 76: 1181-1183.
32. van Asperen J, van Tellingen O, van der Valk MA, Rozenhart M, Beijnen JH (1998) Enhanced oral absorption and decreased elimination of paclitaxel in mice cotreated with cyclosporin A. Clin Cancer Res 4: 2293-2297.
33. van Herwaarden AE, Wagenaar E, van der Kruijssen CM, van Waterschoot RA, Smit JW, Song JY, van der Valk MA, van Tellingen O, van der Hoorn JW, Rosing H, Beijnen JH, Schinkel AH (2007) Knockout of cytochrome P450 3A yields new mouse models for understanding xenobiotic metabolism. J Clin Invest 117: 3583-3592.
34. van Waterschoot RA, Lagas JS, Wagenaar E, van der Kruijssen CM, van Herwaarden AE, Song JY, Rooswinkel RW, van Tellingen O, Rosing H, Beijnen JH, Schinkel AH (2009) Absence of both cytochrome P450 3A and P-glycoprotein dramatically increases docetaxel oral bioavailability and risk of intestinal toxicity. Cancer Res 69: 8996-9002.
35. Wojnowski L (2004) Genetics of the variable expression of CYP3A in humans. Ther Drug Monit 26: 192-199.
36. Wu H, Xin Y, Zhao J, Sun D, Li W, Hu Y, Wang S (2011) Metronomic docetaxel chemotherapy inhibits angiogenesis and tumor growth in a gastric cancer model. Cancer Chemother Pharmacol 68: 879-887.
37. Xu C, Li CY, Kong AN (2005) Induction of phase I, II and III drug metabolism/transport by xenobiotics. Arch Pharm Res 28: 249-268.