Effects of tesmilifene, a substrate of CYP3A and an inhibitor of P-glycoprotein, on the pharmacokinetics of intravenous and oral docetaxel in rats

Journal of Pharmacy and Pharmacology

Volumn 62, Issue 8, 2010, Pages 1084-1088

  Choi, Young H ^a,b   Suh, Jung H ^a   Lee, Joo H ^a,c   Cho, Il H ^d   Lee, Myung G ^a  

^a Seoul National University   (South Korea)

^b Dongguk University   (South Korea)

^c Kyung Hee University   (South Korea)

^d Shinpoong Pharmaceutical Co   (South Korea)

Author keywords

docetaxel; P glycoprotein; pharmacokinetics; rats; tesmilifene

Indexed keywords

BUTYL PARABEN; DOCETAXEL; GLYCOPROTEIN P INHIBITOR; PACLITAXEL; TESMILIFENE;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; COMPARATIVE STUDY; CONTROLLED STUDY; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG EFFECT; DRUG HALF LIFE; DRUG INHIBITION; DRUG METABOLISM; DRUG TRANSPORT; ENZYME SUBSTRATE; FIRST PASS EFFECT; GASTROINTESTINAL ABSORPTION; MALE; MEAN RESIDENCE TIME; NONHUMAN; PROTEIN FAMILY; RAT; TIME TO MAXIMUM PLASMA CONCENTRATION;

ADMINISTRATION, ORAL; ANIMALS; ANTINEOPLASTIC AGENTS; AREA UNDER CURVE; BIOTRANSFORMATION; CYTOCHROME P-450 CYP3A; DRUG INTERACTIONS; INJECTIONS, INTRAVENOUS; MALE; METABOLIC CLEARANCE RATE; P-GLYCOPROTEIN; PHENYL ETHERS; RATS; RATS, SPRAGUE-DAWLEY; TAXOIDS;

EID: 77954899250     PISSN: 00223573     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.2042-7158.2010.01129.x     Document Type: Article

References (24)

1. DeMario MD, Ratain MJ. Oral chemotherapy: rationale and future directions. J Clin Oncol 1998 16 : 2557 2567.
2. Sparreboom A et al. Limited oral bioavailability and active epithelial secretion of paclitaxel caused by P-glycoprotein in the intestine. Proc Natl Acad Sci USA 1997 92 : 2031 2035.
3. Rowinsky EK et al. Clinical pharmacology and metabolism of taxol (paclitaxel): update. Ann Oncol 1994 5 : S7 S16.
4. van Waterschoot RA et al. Absence of both cytochrome P450 3A and P-glycoprotein dramatically increases docetaxel oral bioavailability and risk of intestinal toxicity. Cancer Res 2009 69 : 8996 9002.
5. Malingré MM et al. Coadministration of cyclosporine strongly enhances the oral bioavailability of docetaxel. J Clin Oncol 2001 19 : 1160 1166.
6. Marchettini P et al. Docetaxel: pharmacokinetics and tissue levels after intraperitoneal and intravenous administration in a rat model. Cancer Chemother Pharmacol 2002 49 : 499 503.
7. Schiff PB et al. Promotion of microtubule assembly in vitro by taxol. Nature 1979 277 : 665.
8. Sparreboom A et al. Preclinical pharmacokinetics of paclitaxel and docetaxel. Anticancer Drugs 1998 9 : 1 17.
9. Marre F et al. Hepatic biotransformation of docetaxel (Taxotere®) in vitro: involvement of the CYP3A subfamily in humans. Cancer Res 1996 56 : 1296 1302.
10. Thummel KE. Gut instincts: CYP3A4 and intestinal drug metabolism. J Clin Invest 2007 117 : 3173 3176.
11. Ben Reguiga M et al. Bioavailability and tissular distribution of docetaxel, a P-glycoprotein substrate, are modified by interferon-alpha in rats. J Pharm Pharmacol 2007 59 : 401 408.
12. Brandes LJ et al. N,N-diethyl-2-[4-(phenylmethyl)-phenyoxy] ethanamine (DPPE), a chemopotentiating agent and cytoprotective agent in clinical trials: interaction with histamine at cytochrome P450 3A4 and other isozymes that metabolize antineoplastic drugs. Cancer Chemother Pharmacol 2000 45 : 298 304.
13. Chevallier B et al. A prognostic score in histological node negative breast cancer. Br J Cancer 1990 61 : 436 440.
14. Wacher VJ et al. Overlapping substrate specificities and tissue distribution of cytochrome P450 3A and P-glycoprotein: implications for drug delivery and activity in cancer chemotherapy. Mol Carcinog 1995 13 : 129.
15. Menendez AT et al. Mechanism of action of DPPE, a chemosensitizing agent. Proc Am Assoc Cancer Res 1998 39 : 3462 (abstract).
16. Choi YH et al. Dose-independent pharmacokinetics of metformin in rats: hepatic and gastrointestinal first-pass effects. J Pharm Sci 2006 95 : 2543 2552.
17. Gibaldi M, Perrier D. Pharmacokinetics, 2nd edn. New York: MarcelDekker, 1982.
18. Chiou WL. Critical evaluation of the potential error in pharmacokinetic studies using the linear trapezoidal rule method for the calculation of the area under the plasma level-time curve. J Pharmacokinet Biopharm 1978 6 : 539 546.
19. Sandström M et al. The pharmacokinetics of epirubicin and docetaxel in combination in rats. Cancer Chemother Pharmacol 1999 44 : 469 474.
20. Delin MA et al. Effects of N,N-diethyl-2-[4-(phenylmethyl)phenoxy] ethanamine on the blood-brain barrier permeability in the rat. Eur J Pharmacol 2000 387 : 63 72.
21. Bruono R et al. Pharmacokinetics and metabolism of taxotere™ (Docetaxel). Cancer Surveys 1993 17 : 305 313.
22. Davies B, Morris T. Physiological parameters in laboratory animals and humans. Pharm Res 1993 10 : 1093 1095.
23. Lo YH. Phospholipids as multidrug resistance modulators of the transport of epirubicin in human intestinal epithelial Caco-2 cell layers and everted gut sacs of rats. Biochem Pharmacol 2000 60 : 1381 1390.
24. Lee MG, Chiou WL. Evaluation of potential causes for the incomplete bioavailability of furosemide: gastric first-pass metabolism. J Pharmacokinet Biopharm 1983 11 : 623 640.