Preclinical pharmacokinetics of paclitaxel and docetaxel

Anti-Cancer Drugs

Volumn 9, Issue 1, 1998, Pages 1-17

  Sparreboom, Alex ^d   Van Tellingen, Olaf ^a   Nooijen, Willem J ^a   Beijnen, Jos H ^b,c  

^a NETHERLANDS CANCER INSTITUTE   (Netherlands)

^b SLOTERVAART HOSPITAL   (Netherlands)

^c UTRECHT UNIVERSITY   (Netherlands)

^d ERASMUS MC CANCER INSTITUTE   (Netherlands)

Author keywords

Docetaxel; Paclitaxel; Pharmacokinetics

Indexed keywords

ALCOHOL; CREMOPHOR; CYCLODEXTRIN; DOCETAXEL; LIPOSOME; PACLITAXEL; POLYSORBATE 80; PRODRUG; TAXANE DERIVATIVE;

ANIMAL EXPERIMENT; ANIMAL TISSUE; CANCER INHIBITION; DOSE RESPONSE; DRUG DESIGN; DRUG DISTRIBUTION; DRUG ELIMINATION; DRUG FORMULATION; DRUG MECHANISM; DRUG PROTEIN BINDING; DRUG SOLUBILITY; INTRAPERITONEAL DRUG ADMINISTRATION; LIVER MICROSOME; MOUSE; NONHUMAN; ORAL DRUG ADMINISTRATION; PRIORITY JOURNAL; REVIEW; SOLID TUMOR; SUBCUTANEOUS DRUG ADMINISTRATION;

EID: 0031910064     PISSN: 09594973     EISSN: None     Source Type: Journal    
DOI: 10.1097/00001813-199801000-00001     Document Type: Review

References (171)

1. Wani MC, Taylor HL, Wall ME, et al. Plant antitumor agents. VI: the isolation and structure of taxol, a novel antileukemic and antitumor agent from Taxus brevifolia. J Am Chem Soc 1971; 93: 2325-7.
2. Horwitz SB, Cohen D, Rao S, et al. Taxol: mechanisms of action and resistance. J Natl Cancer Inst 1993; 15: 55-61.
3. Schiff PB, Fant J, Horwitz SB. Promotion of microtubule assembly in vitro by taxol. Nature 1979; 22: 665-7.
4. Schiff PB, Horwitz SB. Taxol stabilizes microtubules in mouse fibroblasts cells. Proc Natl Acad Sci USA 1980; 77: 1561-5.
5. Huizing MT, Sewberath Misser VH, Pieters RC, et al. Taxanes: a new class of antitumor agents. Cancer Invest 1995; 13: 381-404.
6. McGuire WP, Rowinsky EK, Rosenhein EB, et al. Taxol: a unique antineoplastic agent with significant activity in advanced ovarian epithelial neoplasms. Ann Intern Med 1989; 111: 273-9.
7. Holmes FA, Walters RS, Theriault RL, et al. Phase II trial of taxol, an active drug in the treatment of metastatic breast cancer. J Natl Cancer Inst 1991; 83: 1797-805.
8. Murphy WK, Fossella FV, Winn RJ, et al. Phase II study of taxol in patients with untreated advanced non-small cell lung cancer. J Natl Cancer Inst 1993; 85: 384-8.
9. Colin M, Guénard D, Guéritte-Voegelein F, et al. Taxol derivatives, their preparation and pharmaceutical compositions containing them. Rhône-Poulenc Sante. US patent 4814470 (granted March 21, 1989; priority date, July 17, 1986).
10. Ringel I, Horwitz SB. Studies with RP 56976 (Taxotere): a semisynthetic analogue of Taxol. J Natl Cancer Inst 1991; 83: 288-91.
11. Verweij J, Clavel M, Chevalier B. Paclitaxel (Taxol®) and docetaxel (Taxotere®): not simply two of a kind. Ann Oncol 1994; 5: 495-506.
12. Spencer CM, Faulds C. Paclitaxel: a review of its pharmacodynamic and pharmacokinetic properties and therapeutic potential in the treatment of cancer. Drugs 1994; 48: 794-847.
13. Rowinsky EK, Ross C, Donehower RC. Paclitaxel. N Engl J Med 1995; 332: 1004-14.
14. Rowinsky EK, Donehower RC. The clinical pharmacology and use of antimi-crotubule agents in cancer chemotherapeutics. Pharmacol Rev 1991; 52: 35-84.
15. Pazdur R, Kudelka AP, Kavanagh JJ, et al. The taxoids: paclitaxel (Taxol®) and docetaxel (Taxotere®). Cancer Treat Rev 1993; 19: 351-86.
16. Rowinsky EK, Cazenave IA, Donehower RC. Taxol: a novel investigational antineoplastic agent. J Natl Cancer Inst 1990; 82: 1247-59.
17. Mathew AE, Mejillano MR, Nath JP, et al. Synthesis and evaluation of some water-soluble prodrugs and derivatives of taxol with antitumor activity. J Med Chem 1992; 34: 145-51.
18. Straubinger RM, Sharma A, Sharma US, et al. Pharmacology and antitumor effect of novel paclitaxel formulations. In: Georg GI, ed. Taxane anticancer agents: basic science and current status. Washington, DC: American Chemical Society 1995: 111-42.
19. Swindell CS, Krauss NE, Horwitz SB, et al. Biologically active taxol analogues with deleted A-ring side chain substituents and variable C-2′ configurations. J Med Chem 1991; 34: 1176-83.
20. Sharma US, Balasubramanian SV, Straubinger RM. Pharmaceutical and physical properties of paclitaxel (Taxol) complexus with cyclodextrins. J Pharm Sci 1995; 84: 1223-30.
21. Adams JD, Flora KD, Goldspiel BR, et al. Taxol (paclitaxel): a history of pharmaceutical development and current pharmaceutical concerns. J Natl Cancer Inst Monogr 1993; 15: 189-94.
22. Rose WC. Preclinical antitumor activity of taxanes. In: Suffness M, ed. Taxol: science and applications. Boca Raton, FL: CRC Press 1995: 209-21.
23. Rose WC. Taxol: a review of its preclinical in vivo antitumor activity. Anti-Cancer Drugs 1992; 31: 311-21.
24. Meerum Terwogt JM, Nuijen B, Ten Bokkel Huinink WW, et al. Alternative formulations of paclitaxel. Cancer Treat Rev 1997; 23: 87-96.
25. Lorenz W, Riemann HJ, Schmal A. Histamine release in dogs by Cremophor EL and its derivatives: oxyethylated oleic acid is the most effective constituent. Agent Actions 1977; 7: 63-7.
26. Dorr RT. Pharmacology and toxicology of Cremophor EL diluent. Ann Pharmacother 1994; 28: S11-4.
27. Weiss RB, Donehower RC, Wiernik PH, et al. Hypersensitivity reactions from taxol. J Clin Oncol 1990; 8: 1263-69.
28. Theis JG, Liau-Chu M, Chan HS, et al. Anaphylactoid reactions in children receiving high-dose intravenous cyclosporine for reversal of tumor resistance: the causative role of improper dissolution of Cremophor EL. J Clin Oncol 1995; 13: 2508-16.
29. Bissery MC, Guénard D, Guéritte-Voegelein F, et al. Experimental antitumor activity of Taxotere (RP56976; NSC628503), a taxol analogue. Cancer Res 1991; 51: 4845-52.
30. Chevallier B, Fumoleau P, Kerbrat P, et al. Docetaxel is a major cytotoxic drug for the treatment of advanced breast cancer: a phase II trial of the clinical screening cooperative group of the European Organization for Research and Treatment of Cancer. J Clin Oncol 1995; 13: 314-22.
31. Burris H, Irvin R, Kuhn J, et al. Phase I clinical trial of Taxotere administered as either a 2-hour or 6-hour intravenous infusion. J Clin Oncol 1993; 11: 950-8.
32. Pazdur R, Newman RA, Newman B, et al. Phase I trial of Taxotere: five-day schedule. J Natl Cancer Inst 1992; 84: 1781-8.
33. Francis PA, Rigas JR, Kris MG, et al. Phase II trial of docetaxel in patients with stage III and IV non-small cell lung cancer. J Clin Oncol 1994; 12: 1232-7.
34. Woodcock DM, Jefferson S, Linsenmeyer ME, et al. Reversal of the multidrug resistance phenotype with Cremophor EL, a common vehicle for water-insoluble vitamins and drugs. Cancer Res 1990; 50: 4199-203.
35. Schuurhuis GJ, Broxterman HJ, Pinedo HM, et al. The polyoxyethylene castor oil Cremophor EL modifies multidrug resistance. Br J Cancer 1991; 62: 591-4.
36. Friche E, Jensen PB, Sehested M, et al. The solvents Cremophor EL and Tween 80 modulate daunorubicin resistance in the multidrug resistant Ehrlich ascites tumor. Cancer Commun 1990; 90: 297-303.
37. Ross DD, Wooten PJ, Tong Y, et al. Synergistic reversal of multidrug-resistance phenotype in acute myeloid cells by cyclosporin A and Cremophor EL. Blood 1994; 83: 1337-47.
38. Chervinsky DS, Brecher ML, Hoelcle. Cremophor EL enhances taxol efficacy in a multi-drug resistant C1300 neuroblastoma cell line. Anticancer Res 1993; 13: 93-101.
39. Webster LK, Linsenmeyer ME, Millward MJ, et al. Measurement of Cremophor EL following taxol: plasma levels sufficient to reverse drug exclusion mediated by the multidrug resistant phenotype. J Natl Cancer Inst 1993; 85: 1685-90.
40. Millward MJ, Webster LK, Rischin D, et al. Plasma concentrations of polysorbate 80 (Tween 80) in patients following docetaxel (Taxotere®) or etoposide. Ann Oncol 1996; 7: S95 (abstr).
41. Rischin D, Webster LK, Millward MJ, et al. Cremophor pharmacokinetics in patients receiving 3-, 6-, and 24-hour infusions of paclitaxel. J Natl Cancer Inst 1996; 88: 1297-301.
42. Webster LK, Linsenmeyer ME, Rischin D, et al. Plasma concentrations of polysorbate 80 measured in patients following administration of docetaxel or etoposide. Cancer Chemother Pharmacol 1996; 39: 557-60.
43. 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.
44. Sparreboom A, Van Asperen J, Mayer U, et al. Limited bioavailability and active epithelial excretion of paclitaxel (Taxol) caused by P-glycoprotein in the intestine. Proc Natl Acad Sci USA 1997; 94: 2031-5.
45. Sparreboom A, Van Asperen J, Van Tellingen O, et al. Pharmacokinetics of paclitaxel in mdr1a P-glycoprotein deficient mice after intravenous and oral administration. Ann Oncol 1996; 7: S91 (abstr).
46. Watanabe T, Nakayama Y, Naito M, et al. Cremophor EL reversed multidrug resistance in vitro but not in tumor-bearing mouse models. Anti-Cancer Drugs 1996; 7: 825-32.
47. Monsarrat B, Mariel E, Cros S, et al. Isolation and identification of three major metabolites of taxol in rat bile. Drug Metab Dispos 1990; 18: 895-901.
48. Tarr BD, Yalkowsky SH. Enhanced intestinal absorption of cyclosporine in rats through the reduction of emulsion droplet size. J Parenteral Sci Technol 1987; 41: 31-7.
49. Tarr BD, Sambandan TG, Yalkowsky SH. A new parenteral emulsion for the administration of taxol. Pharm Res 1987; 4: 162-5.
50. Bartoli MH, Biotard M, Fessi H, et al. In vitro and in vivo antitumoral activity of free and encapsulated taxol. J Microencapsulation 1990; 7: 191-7.
51. Riondel J, Jacrot M, Fessi H, et al. Effects of free and liposome-encapsulated taxol on two brain tumors xenografted into nude mice. In vivo 1992; 6: 23-7.
52. Rafaeloff R, Husain SR, Rahman A, et al. Liposomes-encapsulated Taxol is an effective modality to circumvent multidrug resistance phenotype. Proc Am Ass Cancer Res 1992; 33: 482 (abstr).
53. Straubinger RM, Sharma A, Murray M, et al. Novel taxol formulations: taxol-containing liposomes. J Natl Cancer Inst Monogr 1993; 15: 69-78.
54. Sharma A, Mayhew E, Straubinger RM. Antitumor effect of taxol-containing liposomes in a taxol-resistant murine tumor model. Cancer Res 1993; 54: 5877-81.
55. Cabanes A, Briggs KE, Gokhale PG, et al. Pharmacokinetics, tissue distribution and in vivo toxicity of liposome-encapsulated taxol. Proc Am Ass Cancer Res 1996; 37: 370 (abstr).
56. Sharma A, Sharma US, Straubinger RM. Paclitaxel-liposomes for local treat-ment of intraperitoneal P388 leukemia. Cancer Lett 1996; 107: 265-72.
57. Sharma A, Straubinger RM, Ojima I, et al. Antitumor efficacy of taxane liposomes on a human ovarian tumor xenograft in nude athymic mice. J Pharm Sci 1995; 84: 1400-4.
58. Sharma A, Mayhew E, Bolcsak L, et al. Activity of paclitaxel liposome formulations against human ovarian tumor xenografts. Int J Cancer 1997; 71: 103-7.
59. Sharma A, Straubinger RM. Novel taxol formulations: preparation and characterization of taxol-containing liposomes. Pharm Res 1994; 11: 889-96.
60. Bangham A, Standish M, Watkins J. J Mol Biol 1965; 13: 238-41.
61. Peres-Soler R, Lopez-Berestein G, Lautersztain J, et al. Phase I and pharmacological study of liposome-entrapped cis-bis-neodecanoato-trans-R,R-1,2-diamino-cyclohexane platinum(II). Cancer Res 1990; 50: 4254-9.
62. Wiernik PH, Schwartz EL, Strauman JJ, et al. Phase I clinical and pharmacokinetic study of taxol. Cancer Res 1987; 47: 2486-93.
63. Markman M, Rowinsky EK, Hakes T, et al. Phase I trial of intraperitoneal taxol: a Gynecologic Oncology Group study. J Clin Oncol 1992; 10: 1485-91.
64. Francis P, Rowinsky EK, Hakes T, et al. Phase I trial of weekly intraperitoneal taxol in patients with residual ovarian carcinoma: a Gynecologic Oncology Group study. J Clin Oncol 1995; 13: 2961-70.
65. Schweikert KM, Sullivan TM, Shaw ME, et al. Bioequivalence of nanodispersed (Cremophor-free) vs. Cremophor-containing formulations of paclitaxel in beagle dogs. Proc Am Ass Cancer Res 1996; 37: 2302 (abstr).
66. Sharma D, Chelvi TP, Kaur J, et al. Novel taxol formulations: PVP nanoparticle-encapsulated taxol for drug delivery in cancer therapy. Oncol Res 1996; 8: 281-6.
67. Dordunoo SK, Jackson JK, Arsenault AL, et al. Taxol encapsulation in poly(ε-caprolactone) microspheres. Cancer Chemotber Pharmacol 1995; 36: 279-84.
68. Lundberg BB. A submicron lipid emulsion coated with amphipathic polyethylene glycol for parenteral administration of paclitaxel (taxol). J Pharm Pharmacol 1997; 49: 16-21.
69. Zhang X, Jackson JK, Burt HM. Development of amphiphilic diblock copolymers as micellar carriers of paclitaxel. Int J Pharm 1996; 132: 195-206.
70. Zhang X, Burt HM, Von Hoff DD, et al. An investigation of the antitumour activity and biodistribution of polymeric micellar paclitaxel. Cancer Chemother Pharmacol 1997; 40: 81-6.
71. Burt HM, Jackson JK, Bains SK, et al. Controlled delivery of taxol from microspheres composed of a blend of ethylene-vinyl acetate copolymer and poly(d,l-lactic acid). Cancer Lett 1995; 88: 73-9.
72. Wenk MR, Fahr A, Reszka R, et al. Paclitaxel partitioning into lipid bilayers. J Pharm Sci 1996; 85: 228-31.
73. Cserhati T, Forgacs E. Use of principal component analysis for the study of the retention behavior of anticancer drugs on a β-cyclodextrin polymer-coated silica column. J Chromatogr A 1996; 728: 67-73.
74. Cserhati T. Interaction of carboxymethyl-γ-cyclodextrin with anticancer drugs studied by charge-transfer thin-layer chromatography. Biomed Chromatogr 1994; 8: 267-72.
75. Nicolaou KC, Dai WM, Guy RK. Chemistry and biology of taxol. Angew Chem Int Ed Engl 1994; 33: 15-44.
76. Kingston DGI. Taxol: the chemistry and structure-activity relationships of a novel anticancer agent. Trends Biotechnol 1994; 12: 222-7.
77. Rose WC, Clark JL, Lee FYF, et al. Preclinical antitumor activity of water-soluble paclitaxel derivatives. Cancer Chemother Pharmacol 1997; 39: 486-92.
78. Pesenti E, Franzetti C, Basioli G, et al. Synthesis and biological activity of water soluble polymer-bound taxol derivatives. Proc Am Ass Cancer Res 1995; 36: 307 (abstr).
79. Vyas DM, Wong H, Croswell AR, et al. Synthesis and antitumor evaluation of water soluble taxol phosphates. Bioorg Med Chem Lett 1993; 3: 1357-64.
80. Ueda Y, Mikkilineni A, Knipe JO, et al. Novel water soluble phosphate prodrugs of taxol possessing in vivo antitumor activity. Bioorg Med Chem Lett 1993; 3: 1761-8.
81. Vyas DM, Ueda Y, Wong H, et al. Phosphatase-activated prodrugs of paclitaxel. In: Georg GI, ed. Taxane anticancer agents: basic science and current status. Washington, DC: American Chemical Society 1995: 124-43.
82. Hamel E, Linn CM, Johns DG. Tubulin-dependent biochemical assay for the antineoplastic agent taxol and applications to measurements of the drug in the serum. Cancer Treat Rep 1982; 66: 1381-6.
83. Lin CM, Jiang YQ, Chaudhary AG, et al. A convenient tubulin-based quantitative assay for paclitaxel (Taxol) derivatives more effective in inducing assembly than the parent compound. Cancer Chemother Pharmacol 1996; 38: 136-40.
84. Brown T, Havlin K, Weiss G, et al. A phase I trial of taxol given by 6-hour intravenous infusion. J Clin Oncol 1991; 9: 1261-7.
85. Grem JL, Tutsch KD, Simon KJ, et al. Phase I study of taxol administered as a short IV infusion daily for 5 days. Cancer Treat Rep 1987; 71: 1179-84.
86. Longnecker SM, Donehower RC, Cates AE, et al. High performance liquid chromatographic assay for taxol (NSC125973) in human plasma and urine: application to pharmacokinetics in a phase I trial. Cancer Treat Rep 1986; 71: 53-9.
87. Rowinsky EK, Burke PJ, Karpe JE, et al. Phase I study of taxol in refractory adult acute leukemia. Cancer Res 1989; 49: 4640-7.
88. Rowinsky EK, Gilbert M, McGuire WP, et al. Sequences of taxol and cisplatin: a phase I and pharmacologic study. J Clin Oncol 1991; 9: 1692-703.
89. Song D, Au LS. Isocratic high-performance liquid chromatographic assay of taxol in biological fluids and tissues using automated column switching. J Chromatogr B 1995; 663: 337-45.
90. Willey TA, Bekos EJ, Gaver RC, et al. A high-performance liquid chromatographic procedure for the quantitative determination of paclitaxel in plasma. J Chromatogr B 1993; 621: 231-6.
91. Huizing MT, Sparreboom A, Rosing H, et al. Quantification of paclitaxel metabolites in human plasma. J Chromatogr B 1995; 674: 261-8.
92. Huizing MT, Rosing H, Keung ACF, et al. High performance liquid chromatographic procedures for the quantitative determination of paclitaxel (Taxol) in human urine: a comparison between a liquid-liquid extraction and a solid-phase extraction as sample pretreatment. J Chromatogr B 1995; 664: 373-82.
93. Vergniol JC, Bruno R, Montay G, et al. Determination of Taxotere in human plasma by a semi-automated high-performance liquid chromatographic method. J Chromatogr B 1993; 582: 273-8.
94. Jamis-Dow CA, Klecker RW, Katki AG, et al. Metabolism of taxol by human and rat liver in vitro: a screen for interactions and interspecies differences. Cancer Chemother Pharmacol 1995; 36: 107-14.
95. Ohtsu T, Sasahi Y, Tamura T, et al. Clinical pharmacokinetics and pharmacodynamics of paclitaxel: a 3-hour infusion versus a 24-hour infusion. Clin Cancer Res 1995; 1: 599-606.
96. El Yazigi A, Yusuf A. Expedient liquid chromatographic assay for paclitaxel in plasma after its administration to cancer patients. Ther Drug Monit 1995; 17: 511-7.
97. Loos WJ, Verweij J, Nooter K, et al. Sensitive determination of docetaxel in human plasma by liquid-liquid extraction and reversed-phase high-performance liquid chromatography. J Chromatogr B 1997; 693: 437-41.
98. Sparreboom A, De Bruijn P, Loos WJ, et al. Determination of paclitaxel in human plasma using single solvent extraction prior to isocratic reversed-phase high-performance liquid chromatography with ultraviolet detection. J Chromatogr B 1997; in press.
99. Leslie J, Kujawa JM, Eddington ND, et al. Stability problems with taxol in mouse plasma during analysis by liquid chromatography. J Pharm Biomed Anal 1993; 11: 1349-52.
100. Mase H, Hiraoka M, Suzuki A, et al. Determination of new anticancer drug, paclitaxel, in biological fluids by high performance liquid chromatography. Yakugaku Zasshi 1994; 114: 351-5.
101. Sharma A, Conway WD, Straubinger RM. Reverse-phase high-performance liquid chromatographic determination of taxol in mouse plasma. J Chromatogr B 1994; 655: 315-9.
102. Sparreboom A, Van Tellingen O, Nooijen WJ, et al. Determination of paclitaxel and metabolites in mouse plasma, tissues, urine and feces by semi-automated reversed-phase high-performance liquid chromatography. J Chromatogr 1995; 664: 383-91.
103. Bitch F, Ma W, McDonald F, et at. Analysis of taxol and related diterpenoids from cell culture by liquid chromatography-electrospray mass spectrometry. J Chromatogr A 1993; 615: 273-80.
104. Royer I, Alvinerie P, Ho LK, et al. Paclitaxel metabolites in human plasma and urine: identification of 6a-hydroxytaxol, 7-epitaxol and taxol hydrolysis products using liquid chromatography/atmospheric pressure chemical ionization mass spectrometry. Rapid Commun Mass Spectr 1995; 9: 495-502.
105. Poon GK, Wade J, Bloomer J, et al. Rapid screening of taxol metabolites in human microsomes by liquid chromatography/electrospray ionization-mass spectrometry. Rapid Commun Mass Spectr 1996; 10: 1165-8.
106. Hempel G, Lehmkuhl D, Krumpelmann S, et al. Determination of paclitaxel in biological fluids by micellar electrokinetic chromatography. J Chromatogr A 1996; 745: 173-9.
107. Grothaus PG, Raybould TJG, Bignami GS, et al. n enzyme immunoassay for the determination of taxol and taxanes in Taxus sp. tissue and human plasma. J Immunol Meth 1993; 158: 5-15.
108. Leu JG, Chen BX, Schiff PB, et al. Characterization of polyclonal and monoclonal anti-taxol antibodies and measurement of taxol in plasma. Cancer Res 1993; 53: 1388-91.
109. Spriggs DR, Tondini C. Taxol administered as a 120-hour infusion. Invest New Drugs 1992; 10: 275-8.
110. Wilson WH, Berg SL, Bryant G, et al. Phase I/II study of taxol 96-hour infusion in refractory lymphoma and breast cancer: Pharmacodynamics and analysis of multidrug resistance. J Clin Oncol 1994; 12: 1621-30.
111. Fujita H, Okamoto M, Takao A, et al. Pharmacokinetics of paclitaxel in experimental animals. Part 1. Blood levels. Gan to Kagaku Ryoho 1994; 21: 653-8.
112. 1 mice. Cancer Chemother Pharmacol 1994; 34: 465-71.
113. Sparreboom A, Van Tellingen O, Nooijen WJ, et al. Tissue distribution, metabolism and excretion of paclitaxel in mice. Anti-Cancer Drugs 1996; 7: 78-87.
114. 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.
115. Sonnichsen DS, Hurwitz CA, Pratt CB, et al. Saturable pharmacokinetics and paclitaxel pharmacodynamics in children with solid tumors. J Clin Oncol 1994; 12: 532-8.
116. Gianni L, Kearns CM, Capri G, et al. Nonlinear pharmacokinetics and metabolism of paclitaxel and its pharmacokinetic/pharmacodynamic relationships in humans. J Clin Oncol 1995; 13: 180-90.
117. Hurwitz CA, Relling MV, Weitman SD, et al. Phase I trial of paclitaxel in children with refractory solid tumors: a Pediatric Oncology Group study. J Clin Oncol 1994; 11: 2324-9.
118. Woodburn K, Chang CK, Lee S, et al. Biodistribution and PDT efficacy of a ketochlorin photosensitizer as a function of the delivery vehicle. Photochem Photobiol 1994; 60: 154-9.
119. Sykes E, Woodburn K, Decker D, et al. Effects of Cremophor EL on distribution of Taxol to serum lipoproteins. Br J Cancer 1994; 70: 401-4.
120. Woodburn K, Kessel D. The alteration of plasma lipoproteins by Cremophor EL. J Photochem Photobiol 1994; 22: 197-201.
121. Webster LK, Cosson EJ, Stokes KH, et al. Effect of the paclitaxel vehicle, Cremophor EL, on the pharmacokinetics of doxorubicin and doxorubicinol in mice. Br J Cancer 1996; 73: 522-4.
122. Gianni L, Vigano L, Locatelli A, et al. Human pharmacokinetic characterization and in vitro study of the interaction between doxorubicin and paclitaxel in patients with breast cancer. J Clin Oncol 1997; 15: 1906-15.
123. Colombo T, Gonzalez Paz O, Zucchetti M, et al. Paclitaxel induces significant changes in epidoxorubicin distribution in mice. Ann Oncol 1996; 7: 801-5.
124. Ellis AG, Crinis NA, Webster LK. Inhibition of etoposide elimination in the isolated perfused rat liver by Cremophor EL and Tween 80. Cancer Chemother Pharmacol 1996; 38: 81-7.
125. Kurlansky PA, Sadeghi AM, Michler RE, et al. J Heart Transplant 1986; 5: 312-5.
126. Innocenti F, Danesi R, Di Paolo A, et al. Plasma and tissue disposition of paclitaxel (taxol) after intraperitoneal administration in mice. Drug Metab Dispos 1995; 23: 713-7.
127. Adler JD, Jarvis KP, Marsh KC, et al. Preclinical in vivo efficacy of two 9-dihydrotaxane analogues against human and murine tumours. Br J Cancer 1996; 73: 560-5.
128. Van Asperen J, Van Tellingen O, Sparreboom A, et al. Enhanced oral bioavailability of paclitaxel in mice treated with the P-glycoprotein blockers SDZ PSC 833 or cyclosporin A. Proc Am Ass Cancer Res 1997; 38: 5 (abstr).
129. Van Asperen J, Van Tellingen O, Sparreboom A, et al. Enhanced oral bioavailability of paclitaxel in mice treated with the P-glycoprotein blocker SDZ PSC 833. Br J Cancer 1997; 76: 1181-3.
130. Gaver RC, Deeb G, Willey TA, et al. The disposition of paclitaxel (taxol) in the rat. Proc Am Ass Cancer Res 1993; 34: 390 (abstr).
131. Bissery MC, Renard A, Montay G, et al. Taxotere: Antitumor activity and pharmacokinetics in mice. Proc Am Ass Cancer Res 1991; 32: 401 (abstr).
132. Bissery MC, Nohynek G, Sanderink GJ, et al. Docetaxel (Taxotere®), a review of preclinical and clinical experience. 1. Preclinical experience. Anti-Cancer Drugs 1995; 6: 339-55.
133. Bissery MC, Renard A, Montay G, et al. Preclinical pharmacology and toxicology of Taxotere (RP56976, NSC628503). In: 7th NCI-EORTC Symp on New Drugs in Cancer Therapy, Amsterdam, March 1992; abstr 251.
134. Bruno R, Sanderink GJ. Pharmacokinetics and metabolism of Taxotere® (docetaxel). Cancer Surv 1993; 17: 305-17.
135. 1-acid glycoprotein. Res Commun Chem Pathol Pharmacol 1993; 80: 337-44.
136. Wild MD, Walle UK, Walle T. Extensive and saturable accumulation of paclitaxel by the human platelet. Cancer Chemother Pharmacol 1995; 36: 41-5.
137. Gout PW, Wijcik LL, Beer CT. Differences between vinblastine and vincristine in distribution in the blood of rats and binding by platelets and malignant cells. Eur J Cancer 1978; 14: 1167-71.
138. Kelton JG, McDonald JWD, Barr RM, et al. The reversible binding of vinblastine to platelets: implications for therapy. Blood 1981; 57: 431-9.
139. 3H]vinblastine by red blood platelets in vitro: effects of colchicine and vincristine. Biochem Pharmacol 1972; 21: 1609-14.
140. 14 radiolabelled Taxotere (RPR56976, NSC628503) in cancer patients. Proc Am Ass Cancer Res 1993; 34: 373 (abstr).
141. 3H]-paclitaxel in rats: a quantitative autoradiographic study. Cancer Chemother Pharmacol 1995; 37: 173-8.
142. 14C-paclitaxel in the rat. Proc Am Ass Cancer Res 1994; 35: 426 (abstr).
143. 3H]Taxol in the Sprague-Dawley rat. Drug Metab Dispos 1994; 22: 254-8.
144. Fujita H, Okamoto M, Takao A, et al. Pharmacokinetics of paclitaxel in experimental animals. Part 2. Tissue distribution. Gan to Kagaku Ryoho 1994; 21: 659-64.
145. Glantz MJ, Choy H, Kearns CM, et al. Paclitaxel disposition in plasma and central nervous systems of humans and rats with brain tumors. J Natl Cancer Inst 1995; 87: 1077-81.
146. Monsarrat B, Alvinerie P, Gares M, et al. Hepatic metabolism and biliary excretion of taxol. Cell Pharmacol 1993; 1: 77-81.
147. Monsarrat B, Alvinerie P, Dubois P, et al. Hepatic metabolism and biliary excretion of taxol in rats and humans. J Natl Cancer Inst Monogr 1993; 15: 39-46.
148. Walle T, Kumar GN, McMillan JM, et al. Taxol metabolism in rat hepatocytes. Biochem Pharmacol 1993; 46: 1661-4.
149. Monsarrat B, Royer I, Wright M, et al. Biotransformation of taxoids by human cytochromes P450: structure-activity relationships. Bull Cancer 1997; 84: 125-33.
150. Anderson CD, Wang J, Kumar GN, et al. Dexamethasone induction of taxol metabolism in the rat. Drug Metab Dispos 1995; 23: 1286-90.
151. Sparreboom A, Huizing MT, Boesen JJB, et al. Isolation, purification and biological activity of mono- and dihydroxylated paclitaxel metabolites from human faeces. Cancer Chemother Pharmacol 1995; 36: 299-304.
152. Kumar GN, Oatis JE, Thornburg KR, et al. 6α-Hydroxytaxol: isolation and identification of the major metabolite of taxol in human liver microsomes. Drug Metab Dispos 1994; 22: 177-9.
153. Harris JW, Katki A, Anderson LW, et al. Isolation, structural determination and biological activity of 6αhydroxytaxol. The principal metabolite of Taxol. J Med Chem 1994; 37: 706-9.
154. Kumar GN, Ray S, Walle T, et al. Comparative in vitro cytotoxic effects of taxol and its major human metabolite 6α-hydroxytaxol. Cancer Chemother Pharmacol 1995; 36: 129-33.
155. Rahman A, Korzekwa KR, Grogan J, et al. Selective biotransformation of Taxol to 6α-hydroxytaxol by human cytochrome P450 2C8. Cancer Res 1994; 54: 5543-6.
156. Walle T. Assays for CYP2C8- and CYP3A4-mediated metabolism of taxol in vivo and in vitro. Methods Enzymol 1996; 272: 145-51.
157. Kumar GN, Walle UK, Walle T. Cytochrome P450 3A-mediated human liver microsomal taxol 6α-hydroxylation. J Pharmacol Exp Ther 1994; 268: 1160-5.
158. Cresteil T, Monsarrat B, Alvinerie P, et al. Taxol metabolism by human liver microsomes: identification of isozymes involved in its biotransformation. Cancer Res 1994; 54: 386-92.
159. 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.
160. 2 receptor antagonists that differ in P450 modulation activity: comparative effects on paclitaxel clearance rates and neutropenia. Cancer Chemotber Pharmacol 1995; 36: 227-32.
161. Sonnichsen DS, Liu Q, Schuetz EG, et al. Variability in human cytochrome P450 paclitaxel metabolism. J Pharmacol Exp Ther 1995; 275: 566-75.
162. Gaillard C, Monsarrat B, Vuilhorgne M, et al. Docetaxel (Taxotere) metabolism in the rat. Proc Am Ass Cancer Res 1994; 35: 428 (abstr).
163. Monegier B, Gaillard C, Sable S, et al. Structures of the major human metabolites of docetaxel (RP 56976, Taxotere®). Tetrahedron Lett 1994; 35: 3715-8.
164. Vuilhorgne M, Gaillard C, Sanderink GJ. Metabolism of docetaxel. ACS Symp Ser 1995; 583: 98-110.
165. Sparreboom A, Van Tellingen O, Scherrenburg EJ, et al. Isolation, purification and biological activity of major docetaxel metabolites from human feces. Drug Metab Dispos 1996; 24: 655-8.
166. Commerçon A, Bourzat JD, Bézard D, et al. Partial synthesis of major human metabolites of docetaxel (RP 56976-Taxotere®). Tetrahedron 1994; 50: 10289-98.
167. Zhou-Pan XR, Marre F, Zhou XJ, et al. Preliminary characterization of taxotere metabolism by using human liver microsomal fractions. Cell Pharmacol 1993; 1: S119 (abstr).
168. Royer I, Monsarrat B, Sonnier M, et al. Metabolism of docetaxel by human cytochromes P450: interactions with paclitaxel and other antineoplastic drugs. Cancer Res 1996; 56: 58-65.
169. Marre F, Sanderink GJ, De Sousa G, et al. Hepatic biotransformation of docetaxel (Taxotere) in vitro: involvement of the CYP3A subfamily in humans. Cancer Res 1996; 56: 1296-302.
170. Walle T, Walle UK, Kumar GN, et al. Taxol metabolism and disposition in cancer patients. Drug Metab Dispos 1995; 23: 506-12.
171. Marlard M, Gaillard C, Sanderink GJ, et al. Kinetics, distribution, metabolism, and excretion of radiolabelled Taxotere in mice and dogs. Proc Am Ass Cancer Res 1993; 34: 393 (abstr).