Metabolism of thalidomide in liver microsomes of mice, rabbits, and humans

Journal of Pharmacology and Experimental Therapeutics

Volumn 310, Issue 2, 2004, Pages 571-577

  Lu, Jun ^a   Helsby, Nuala ^a   Palmer, Brian D ^a   Tingle, Malcolm ^b   Baguley, Bruce C ^a   Kestell, Philip ^a   Ching, Lai Ming ^a  

^a UNIVERSITY OF AUCKLAND   (New Zealand)

^b UNIVERSITY OF AUCKLAND   (New Zealand)

Author keywords

[No Author keywords available]

Indexed keywords

DRUG METABOLITE; GLUTAMINE DERIVATIVE; PHTHALOYLISOGLUTAMINE; THALIDOMIDE; THALIDOMIDE 5 O GLUCURONIDE; UNCLASSIFIED DRUG;

ANIMAL TISSUE; ANTINEOPLASTIC ACTIVITY; ARTICLE; CONTROLLED STUDY; DRUG HALF LIFE; DRUG HYDROXYLATION; DRUG MECHANISM; DRUG METABOLISM; HUMAN; HUMAN TISSUE; IN VITRO STUDY; IN VIVO STUDY; INFLAMMATION; LIQUID CHROMATOGRAPHY; LIVER MICROSOME; MASS SPECTROMETRY; MOUSE; NONHUMAN; PRIORITY JOURNAL; RABBIT; SPECIES DIFFERENTIATION;

ANIMALS; HUMANS; MICE; MICE, INBRED C57BL; MICROSOMES, LIVER; RABBITS; SPECIES SPECIFICITY; THALIDOMIDE;

EID: 3342996710     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: 10.1124/jpet.104.067793     Document Type: Article

References (27)

1. Ando Y, Fuse E, and Figg WD (2002a) Thalidomide metabolism by the CYP2C subfamily. Clin Can Res 8:1964-1973.
2. Ando Y, Price DK, Dahut WL, Cox MC, Reed E, and Figg WD (2002b) Pharmacogenetic associations of CYP2C19 genotype with in vivo metabolisms and pharmacological effects of thalidomide. Cancer Biol Ther 1:669-673.
3. Barfield M, Spear RJ, and Sternhell S (1975) Interproton spin-spin coupling across a dual path in 2,5-dihydrofurans and phthalans. J Am Chem Soc 97:5160-5167.
4. Calabrese L and Fleischer AB (2000) Thalidomide: current and potential clinical applications. Am J Med 108:487-495.
5. Chung F, Lu J, Palmer BD, Kestell P, Browett P, Baguley BC, Tingle MD and Ching LM (2004) Thalidomide pharmacokinetics and metabolite formation in mice, rabbits and multiple myeloma patients. Clin Cancer Res, in press.
6. Chung F, Wang LCS, Kestell P, Baguley BC, and Ching LM (2004) Modulation of thalidomide pharmacokinetics by cyclophosphamide or 5,6-dimethylxanthenone-4- acetic acid (DXAA) in mice: the role of tumour necrosis factor. Cancer Chemother Pharmacol 53:377-383.
7. Eisen TG (2000) Thalidomide in solid tumors: the London experience. Oncology (Huntington) 14:17-20.
8. Eriksson T, Bjorkman S, Roth B, Bjork H, and Hoglund P (1998) Hydroxylated metabolites of thalidomide: formation in-vitro and in-vivo in man. J Pharm Pharmacol 50:1409-1416.
9. Faigle JW (1962) The metabolic fate of thalidomide. Experientia 18:389-397.
10. Figg WD, Raje S, Bauer KS, Tompkins A, Venzon D, Bergan R, Chen A, Hamilton M, Pluda J, and Reed E (1999) Pharmacokinetics of thalidomide in an elderly prostate cancer population. J Pharm Sci 88:121-125.
11. Gordon GB, Spielberg SP, Blake DA, and Balasubramanian V (1981) Thalidomide teratogenesis: evidence for a toxic arene oxide metabolite. Proc Natl Acad Sci USA 78:2545-2548.
12. Keberle H, Faigle JW, Fritz H, Knusel F, Loustalot P, and Schmid K (1965) Theories on the mechanism of action of thalidomide, in Embryopathic Activity of Drugs (Robson JM, Sullivan FM, and Smith RL eds) pp 210-233, J. & A. Churchill Ltd., London.
13. Lenz W (1962) Thalidomide and congenital abnormalities. Lancet 1:45.
14. Lu J, Palmer BD, Kestell P, Browett P, Baguley BC, Muller G, and Ching LM (2003) Thalidomide metabolites in mice and patients with multiple myeloma. Clin Cancer Res 9:1680-1688.
15. McBride W (1961) Thalidomide and congenital abnormalities. Lancet 2:1358.
16. Scheffler MR, Colburn W, Kook KA, and Thomas SD (1999) Thalidomide does not alter estrogen-progesterone hormone single dose pharmacokinetics. Clin Pharmacol Ther 65:483-490.
17. Schumacher H, Blake DA, and Gillette JR (1968) Disposition of thalidomide in rabbits and rats. J Pharmacol Exp Ther 160:201-211.
18. Schumacher H, Smith RL, and Williams RT (1965) The metabolism of thalidomide: the fate of thalidomide and some of its hydrolysis products in various species. Br J Pharmacol 25:338-351.
19. Sheskin J (1965) Further observation with thalidomide in lepra reactions. Leprosy Rev 36:183-187.
20. Singhal S, Mehta J, Desikan R, Ayers D, Roberson P, Eddlemon P, Munshi N, Anaissie E, Wilson C, Dhodapkar M, et al. (1999) Antitumor activity of thalidomide in refractory multiple myeloma. N Engl J Med 341:1565-1571.
21. Smith PK, Krohn RI, Hermanson GT, Mallia AK, Garter FH, Provenzano MD, Fujimoto EK, Goeke NM, Olson BJ, and Klenk DC (1985) Measurement of protein using bichinchoninic acid. Anal Biochem 150:76-85.
22. Smith RL, Fabro S, Schumacher H, and Williams RT (1965) Studies on the relationship between the chemical structure and embryotoxic activity of thalidomide and related compound, in Embryopathic Activity of Drugs (Robson JM, Sullivan FM, and Smith RL eds) pp 195-209, J. & A. Churchill Ltd., London.
23. Teo SK, Sabourin PJ, O'Brien K, Kook KA, and Thomas SD (2000) Metabolism of thalidomide in human microsomes, cloned human cytochrome P-450 isozymes and Hansen's disease patients. J Biochem Toxicol 14:140-147.
24. Torano JS, Verbon A, and Guchelaar HJ (1999) Quantitative determination of thalidomide in human serum with high-performance liquid chromatography using protein precipitation with trichloroacetic acid and ultraviolet detection. J Chromatogr Biomed Appl 734:203-210.
25. Trapnell CB, Donahue SR, Collins JM, Flockhart DA, Thacker D, and Abernethy DR (1998) Thalidomide does not alter the pharmacokinetics of ethinyl estradiol and norethindrone. Clin Pharmacol Ther 64:597-602.
26. Williams RT, Schumacher H, Fabro S, and Smith RL (1965) The chemistry and metabolism of thalidomide, in Embryopathic Activity of Drugs (Robson JM, Sullivan FM, and Smith RL eds) pp 167-193, J. & A. Churchill Ltd., London.
27. Zwingenberger K and Wnendt S (1996) Immunomodulation by thalidomide: systematic review of the literature and of unpublished observations. J Inflamm 46:177-211.