Population pharmacokinetics of orally administered paclitaxel formulated in Cremophor EL

British Journal of Clinical Pharmacology

Volumn 59, Issue 3, 2005, Pages 325-334

  De Jonge, Milly E ^a,b   Huitema, Alwin D R ^a   Schellens, Jan H M ^a   Rodenhuis, Sjoerd ^a   Beijnen, Jos H ^a  

^a NETHERLANDS CANCER INSTITUTE   (Netherlands)

^b SLOTERVAART HOSPITAL   (Netherlands)

Author keywords

Cremophor EL; Oral administration; Paclitaxel; Population pharmacokinetics

Indexed keywords

CARBOPLATIN; CREMOPHOR; CYCLOPHOSPHAMIDE; CYCLOSPORIN A; PACLITAXEL; THIOTEPA;

ADULT; AGED; ARTICLE; CANCER; CONTROLLED STUDY; DOSE RESPONSE; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG DOSE REGIMEN; DRUG ELIMINATION; DRUG FORMULATION; FEMALE; GASTROINTESTINAL ABSORPTION; HUMAN; MAJOR CLINICAL STUDY; MALE; PRIORITY JOURNAL;

ABSORPTION; ADULT; AGED; ANTINEOPLASTIC AGENTS, PHYTOGENIC; BIOLOGICAL AVAILABILITY; DOSE-RESPONSE RELATIONSHIP, DRUG; GLYCEROL; HUMANS; MIDDLE AGED; PACLITAXEL; SURFACE-ACTIVE AGENTS; VEHICLES;

EID: 15244361780     PISSN: 03065251     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1365-2125.2004.02325.x     Document Type: Article

References (41)

1. Rowinski EK, Donehower RC. Paclitaxel (Taxol) N Engl J Med 1995; 332: 1004-14.
2. Huizing MT, Sewberath Misser VH, Pieters RC, et al. Taxanes: a new class of antitumor agents. Cancer Invest 1995; 13: 381-404.
3. Webster LK, Woodcock DM, Rischin D, et al. Cremophor. Pharmacological activity of an 'inert' solubiliser. J Oncol Pharm Prac 1997; 3: 186-92.
4. Van Zuylen L, Karlsson MO, Verweij J, et al. Pharmacokinetic modelling of paclitaxel encapsulation in Cremophor EL micelles. Cancer Chemother Pharmacol 2001; 47: 309-18.
5. Van Tellingen O, Huizing MT, Nannan Panday VR, et al. Cremophor EL causes (pseudo-) non-linear pharmacokinetics of paclitaxel in patients. Br J Cancer 1999; 81: 330-5.
6. Sparreboom A, Van Tellingen O, Nooijen WJ, et al. Nonlinear pharmacokinetics of paclitaxel in mice results from the pharmaceutical vehicle Cremophor EL. Cancer Res 1996; 56: 2112-5.
7. Sparreboom A, Van Zuylen L, Brouwer E, et al. Cremophor EL-mediated alteration of paclitaxel distribution in human blood: clinical pharmacokinetic implications. Cancer Res 1999; 59: 1454-7.
8. Sparreboom A, Van Asperen J, Mayer U, et al. Limited oral bioavailability and active epithelial excretion of paclitaxel (Taxol) caused by P-glycoprotein in the intestine. Proc Matl Acad Sci USA 1997; 94: 2031-5.
9. Monsarrat B, Alvinerie P, Wright M, et al. Hepatic metabolism and biliary excretion of Taxol in rats and humans. J Natl Cancer Inst Monogr 1993; 15: 39-46.
10. Harris JW, Katki A, Anderson LW, et al. Isolation, structural determination, and biological activity of 6 alpha-hydroxytaxol, the principal human metabolite of taxol. J Med Chem 1994; 37: 706-9.
11. Sparreboom A, Huizing MT, Boesen JJB, et al. Isolation, purification and biological activity of mono- and dihydroxylated paclitaxel (Taxol) metabolites from human faeces. Cancer Chemother Pharmacol 1995; 36: 299-304.
12. Kumar HN, Ray S, Walle T, et al. Comparative in vitro cytotoxic effects of taxol and its major human metabolites 6α-hydroxytaxol Cancer Chemother Pharmacol 1995; 36: 129-35.
13. Harris JW, Rahman A, Kim BR, et al. Metabolism of Taxol by human hepatic microsomes and liver slices: participation of cytochrome P450 3A4 and an unknown P450 enzyme. Cancer Res 1994; 54: 4026-35.
14. Cresteil T, Monsarrat B, Alvinerie P, et al. Taxol metabolism by human liver microsomes: identification of cytochrome P450 isozymes involved in its biotransformation. Cancer Res 1994; 54: 386-92.
15. Rahman A, Korzekwa KR, Grogan J, et al. Selective biotransformation of taxol to 6alpha-hydroxytaxol by human cytochrome P450 2C8. Cancer Res 1994; 54: 5543-6.
16. Wandel C, Kim RB, Kajiji S, et al. P-glycoprotein and cytochrome P-450 3A inhibition: dissociation of inhibitory potencies. Cancer Res 1999; 59: 3944-8.
17. Meerum Terwogt JM, Malingré MM, Beijnen JH, et al. Co-administration of oral cyclosporin A enables oral therapy with paclitaxel. Clin Cancer Res 1999; 5: 3379-84.
18. Meerum Terwogt JM, Beijnen JH, Ten Bokkel Huinink WW, et al. Co-administration of oral cyclosporin A enables oral therapy with paclitaxel. Lancet 1998; 352: 285.
19. Van Asperen J, Van Tellingen O, Van Der Valk MA, et al. Enhanced oral absorption and decreased elimination of paclitaxel in mice cotreated with cyclosporin A. Clin Cancer Res 1998; 4: 2293-7.
20. Bardelmeijer HA, Ouwehand M, Malingré MM, et al. Entrapment by Cremophor EL decreases the absorption of paclitaxel from the gut. Cancer Chemother Pharmacol 2002; 49: 119-25.
21. Malingré MM, Schellens JHM, Van Tellingen O, et al. The co-solvent Cremophor EL limits adsorption of orally administered paclitaxel in cancer patients. Br J Cancer 2001; 85: 1472-7.
22. Britten CD, Baker SD, Denis LJ, et al. Oral paclitaxel and concurrent cyclosporin A. Targeting clinically relevant systemic exposure to paclitaxel. Clin Cancer Res 2000; 6: 3459-68.
23. Malingré MM, Meerum Terwogt JM, Beijnen JH, et al. A phase I pharmacokinetic study of oral paclitaxel. J Clin Oncol 2000; 18: 2468-75.
24. Malingré MM, Beijnen JH, Rosing H, et al. A phase I and pharmacokinetic study of bi-daily dosing of oral paclitaxel in combination with cyclosporin A. Cancer Chemother Pharmacol 2001; 47: 347-54.
25. Malingré MM, Beijnen JH, Rosing H, et al. The effect of different doses of cyclosporin A on the systemic exposure of orally administered paclitaxel. Anticancer Drugs 2001; 12: 351-8.
26. Huizing MT, Sparreboom A, Rosing H, et al. Quantification of paclitaxel metabolites in human plasma by high-performance liquid chromatography. J Chromatogr B 1995; 674: 261-8.
27. Beal SL, Sheiner LB. NONMEM Users' Guide. University of California at San Fransisco, San Fransisco: NONMEM Project Group; 1998.
28. Wade JR, Kelman AW, Howie CA, Whiting B. Effect of misspecification of the absorption process on subsequent estimation in population analysis. J Pharmacokinet Biopharm 1993; 21: 209-22.
29. Jonsson EN, Karlsson MO. X-pose - an S-PLUS based population pharmacokinetic/pharmacodynamic model building aid for NONMEM. Comput Meth Programs Biomed 1999; 58: 51-64.
30. Malingré MM, Schellens JHM, Van Tellingen O, et al. Metabolism and excretion of paclitaxel after oral administration in combination with cyclosporine A and after i.v. administration. Anticancer Drugs 2000; 11: 813-20.
31. Karlsson MO, Molnar V, Freijs A, et al. Pharmacokinetic models for the saturable distribution of paclitaxel. Drug Metab Dispos 1999; 27: 1220-3.
32. Van Den Bongard HJGD. Development and validation of a population pharmacokinetic model of paclitaxel in cancer patients. Clinical Pharmacokinetics of Anticancer Agents. Focus on E7070, methotrexate and paclitaxel. Thesis University Utrecht, 2002.
33. Gianni L, Kearns CM, Giani A, et al. Nonlinear pharmacokinetics and metabolism of paclitaxel and its pharmacokinetic/pharmacodynamic relationships in humans. J Clin Oncol 1995; 13: 180-90.
34. Henningsson A, Karlsson MO, Viganò L, et al. Mechanism-based pharmacokinetic model for paclitaxel. J Clin Oncol 2001; 19: 4065-73.
35. Cabanes A, Briggs KE, Gokhale PC, et al. Comparative in vivo studies with paclitaxel and liposome-encapsulated paclitaxel. Int J Oncol 1998; 12: 1035-49.
36. Wild MD, Walle UK, Walle T. Extensive and saturable accumulation of paclitaxel by the human platelet. Cancer Chemother Pharmacol 1995; 36: 41-4.
37. Kruijtzer CMF, Schellens JHM, Mezger J, et al. Phase II and pharmacologic study of weekly oral paclitaxel plus cyclosporine in patients with advanced non-small-cell lung cancer. J Clin Oncol 2002; 20: 4508-16.
38. Kruijtzer CMF, Boot H, Beijnen JH, et al. Weekly oral paclitaxel as first-line treatment in patients with advanced gastric cancer. Ann Oncol 2003; 14: 197-204.
39. Huizing MT, Keung ACF, Rosing H, et al. Pharmacokinetics of paclitaxel and metabolites in a randomized comparative study in platinum-pretreated ovarian cancer patients. J Clin Oncol 1993; 11: 2127-35.
40. Huizing MT, Giaccone G, Van Warmerdam LJC, et al. Pharmacokinetics of paclitaxel and carboplatin in a dose escalating and dose-sequencing study in patients with non-small-cell lung cancer. J Clin Oncol 1997; 15: 317-29.
41. Fogli S, Danesi R, De Braud F, et al. Drug distribution and pharmacokinetic/pharmacodynamic relationship of paclitaxel and gemcitabine in patients with non-small-cell lung cancer. Ann Oncol 2001; 12: 1553-9.