Metabolism of levormeloxifene, a selective oestrogen receptor modulator, in the Sprague-Dawley rat, Cynomolgus monkey and postmenopausal woman

Xenobiotica

Volumn 30, Issue 2, 2000, Pages 201-217

  Mountfield, R J ^a   Panduro, A M ^b   Wassmann, O ^b   Thompson, M ^b   John, B ^c   Van Der Merbel, N ^d  

^a F HOFFMANN LA ROCHE LTD   (Switzerland)

^b NOVO NORDISK A S   (Denmark)

^c HLS Ltd   (United Kingdom)

^d PRA International USA   (Netherlands)

Author keywords

[No Author keywords available]

Indexed keywords

CENTCHROMAN; DRUG METABOLITE; SELECTIVE ESTROGEN RECEPTOR MODULATOR;

ADULT; ANIMAL EXPERIMENT; ARTICLE; DRUG BLOOD LEVEL; DRUG ELIMINATION; DRUG EXCRETION; DRUG FECES LEVEL; DRUG METABOLISM; DRUG URINE LEVEL; FEMALE; HUMAN; HUMAN EXPERIMENT; LIVER; MALE; MONKEY; NONHUMAN; NORMAL HUMAN; OXIDATION; POSTMENOPAUSE; RAT;

ANIMALIA; MACACA FASCICULARIS;

EID: 0034002828     PISSN: 00498254     EISSN: None     Source Type: Journal    
DOI: 10.1080/004982500237785     Document Type: Article

References (10)

1. Antunes, C. M. F., Strolley, P. D., Rosenshein, N. B., Davies, J. L., Tonascia, J. A., Brown, C., Burnett, L., Rutledge, A., Pokempner, M. and Garcia, R., 1979, Endometrial cancer and estrogen use: report of a large case-control study. New England Journal of Medicine, 300, 9-13.
2. Bain, S., Shalmi, M. and Korsgaard, N., 1997, Levormeloxifene, a non-steroidal estrogen receptor therapeutic, prevents bone loss, reduces serum cholesterol and has differentiated uterine effects in the ovariectomised rat. Maturita, 27 (suppl. 1), 144.
3. Black, L. J., Sato, M., Rowley, E. R., Magee, D, E., Bekele, A., Williams, D. C., Cullinan, G. J., Bendele, R., Kaufmann, R. F., Bensch, W. R., Frolik, C. A., Termine, J. D. and Bryant, H. U., 1994, Raloxifene prevents bone loss and reduces serum cholesterol without causing uterine hypertrophy in ovariectomised rats. Journal of Clinical Investigation, 93, 63-69.
4. Holm, P., Korsgaard, N., Shalmi, M., Andersen, H. L., Hougaard, P., Skouby, S. O. and Stender, S., 1997b, Significant reduction of the antiatherogenic effect of estrogen by long-term inhibition of nitric oxide synthesis in cholesterol-clamped rabbits. Journal of Clinical Investigation, 100, 821-828.
5. Holm, P., Shalmi, M., Korsgaard, N., Guldhammer, B., Skouby, S. O. and Stender, S., 1997a, A partial estrogen receptor agonist with strong antiatherogenic properties without noticeable effect on reproductive tissue in cholesterol-fed female and male rabbits. Arteriosclerosis, Thrombosis, and Vascular Biology, 17, 2264-2272.
6. Hulley, S., Grady, D., Bush, T., Furberg, C., Herrington, D., Riggs, B., Vittinghoff, E. for the Heart and Estrogen/Progestin Replacement Study (HERS) Research Group, 1998, Randomized trial of estrogen plus progestin for secondary prevention of coronary heart disease in the postmenopausal woman. Journal of the American Medical Association, 280, 605-613.
7. Ke, H. Z., Simmons, H. A., Pirie, C. M., Crawford, D. T. and Thompson, D. D., 1995, Droloxifene, a new estrogen antagonist/agonist, prevents bone loss in ovariectomized rats. Endocrinology, 136, 2435-2441.
8. Lobo, R. A., Pickar, J. H., Wild, R. A., Walsh, B. and Hirvonen, E., 1994, Metabolic impact of adding medroxyprogesterone acetate to conjugated estrogen therapy in the postmenopausal woman. Obstetrics and Gynecology, 84, 987-995.
9. Remie, R., Rensema, J. W., Havinga, R. and Kuipers, F., 1991, The permanent bile fistula rat model. In Progress in Pharmacology and Clinical Pharmacology, 8/4 (Stuttgart: Gustav Fischer), pp. 127-145.
10. Witt, D. M. and Lousberg, T. R., 1997, Controversies surrounding estrogen use in the postmenopausal woman. Annals of Pharmacotherapy, 31, 745-755.