Circulating concentrations of the antiprogestins CDB-2914 and mifepristone in the female rhesus monkey following various routes of administration

Human Reproduction

Volumn 15, Issue 5, 2000, Pages 1100-1106

  Larner, J M ^a,c   Reel, J R ^a   Blye, R P ^b  

^a BIOQUAL INC   (United States)

^b EUNICE KENNEDY SHRIVER NATIONAL INSTITUTE OF CHILD HEALTH AND HUMAN DEVELOPMENT   (United States)

^c ALEXION PHARMACEUTICALS   (United States)

Author keywords

Antiprogestin; Bioavailability; Contraception; Protein binding; Rhesus monkey

Indexed keywords

17ALPHA ACETOXY 11BETA (4 DIMETHYLAMINOPHENYL) 19 NORPREGNA 4,9 DIENE 3,20 DIONE; ALPHA1 GLYCOPROTEIN; ANTIGESTAGEN; MIFEPRISTONE; PROGESTERONE; SEX HORMONE BINDING PROTEIN; TRANSCORTIN; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; CONCENTRATION (PARAMETERS); DRUG BIOAVAILABILITY; FEMALE; HORMONAL CONTRACEPTION; NONHUMAN; ORAL CONTRACEPTION; PLASMA PROTEIN BINDING; RHESUS MONKEY;

ANIMALIA; MACACA MULATTA;

EID: 0034093492     PISSN: 02681161     EISSN: None     Source Type: Journal    
DOI: 10.1093/humrep/15.5.1100     Document Type: Article

References (28)

1. Altman, D.G. (1991) Practical Statistics for Medical Research. Chapman & Hall, London, pp. 309-315.
2. Cook, C.E., Lee, Y-.W., Wani, M.C. et al. (1994) Effects of D-ring substituents on antiprogestational (antagonist) and progestational (agonist) activity of 11β-aryl steroids. Hum. Reprod., 9 (Suppl. 1), 32-39.
3. Deraedt, R., Bonnat, C., Busigny, M. et al. (1985) Pharmacokinetics of RU 486. In Baulieu, E.E. and Segal, S. (eds), The Antiprogestin Steroid RU 486 and Human Fertility Control. Plenum Press, New York, pp. 103-122.
4. Fotherby, K. (1995) Levonorgestrel: clinical pharmacokinetics. Clin. Pharmacokinet., 28, 203-215.
5. Grimaldi, B., Barre, J. and Tillement, J.-P. (1992) Les rôles respectifs des liaisons aux protéines sanguines et tissulaires de la mifépristone (RU486) dans sa distribution quantitative dans l'organisme. C.R. Acad. Sci. (Paris) III, 315, 93-99.
6. Hammond, G.L. and Lähteenmäki, P.L.A. (1983) A versatile method for the determination of serum cortisol binding globulin and sex hormone binding globulin binding capacities. Clin. Chim. Acta, 132, 101-110.
7. Heikinheimo, O. (1997) Clinical pharmacokinetics of mifepristone. Clin. Pharmacokinet., 33, 7-17.
8. Heikinheimo, O., Kontula, K., Croxatto, H. et al. (1987a) Plasma concentrations and receptor binding of RU 486 and its metabolites in humans. J. Steroid Biochem., 26, 279-284.
9. Heikinheimo, O., Lähteenmäki, P.L.A., Koivunen, E. et al. (1987b) Metabolism and serum binding of RU 486 in women after various single doses. Hum. Reprod., 2, 379-385.
10. Heikinheimo, O., Haukkamma, M. and Lähteenmäki, P.L.A. (1989) Distribution of RU 486 and its demethylated metabolites in humans. J. Clin. Endocrinol. Metab., 68, 270-275.
11. Heikinheimo, O., Pesonen, U., Huupponen, R. et al. (1994) Hepatic metabolism and distribution of mifepristone and its metabolites in rats. Hum. Reprod., 9 (Suppl. 1), 40-46.
12. 3H-Labelled RU 38486: characterization of binding sites in human uterine cytosol. J. Clin. Chem. Clin. Biochem., 23, 265-276.
13. Hild-Petito, S., Blye, R.P., Larner, J.M. and Reel, J.R. (1996) Biological activity profile of the antiprogestin, CDB-2914 (11β-[4-N,N-dimethylaminophenyl]-17α-acetoxy-19-norpregna-4,9-diene- 2,20-dione). 29th Annual Meeting of the Society for the Study of Reproduction, Abstract 310.
14. Holford, N. (1990) In PROPHET: Public Procedures. Bolt, Beranek and Newman, Inc., Cambridge, MA, pp. 150-178.
15. Juchem, M. and Pollow, K. (1990) Binding of oral contraceptive progestogens to serum proteins and cytoplasmic receptor. Am. J. Obstet. Gynecol., 163, 2171-2183.
16. Kekkonen, R., Heikinheimo, O., Mandelin, E. et al. (1996) Pharmacokinetics of mifepristone after low oral doses. Contraception, 54, 229-234.
17. Lähteenmäki, P., Heikinheimo, O., Croxatto, H. et al. (1987) Pharmacokinetics and metabolism of RU 486. J. Steroid Biochem., 27, 859-863.
18. Moguilewsky, M. and Philibert, D. (1985) Biochemical profile of RU 486. In Baulieu, E.E. and Segal, S. (eds), The Antiprogestin Steroid RU 486 and Human Fertility Control. Plenum Press, New York, pp. 87-97.
19. National Research Council (1996) Guide for the Care and Use of Laboratory Animals. Institute of Laboratory Animal Resources Commission on Life Sciences, National Academy Press, Washington DC.
20. Niswender, G.D., Akbar, A.S. and Nett, T.M. (1975) Use of specific antibodies for quantification of steroid hormones. Methods Enzymol., 36, 16-34.
21. Passaro, M., Piquion, J., Mullen, N. et al. (1997) Safety and luteal phase effects of the antiprogestin CDB-2914 in normally cycling women. The Endocrine Society Abstracts, PI-370, 227.
22. Reel, J.R., Humphrey, R.R., Shih, Y.-H. et al. (1979) Competitive progesterone antagonists: receptor binding and biologic activity of testosterone and 19-nortestosterone derivatives. Fertil. Steril., 31, 552-561.
23. Reel, J.R., Hild-Petito, S. and Blye, R.P. (1998) Anti-ovulatory and postcoital antifertility activity of the antiprogestin CDB-2914 when administered as single, multiple, or continuous doses to rats. Contraception. 58, 129-136.
24. Spitz, I.M. and Bardin, C.W. (1993) Clinical pharmacology of RU 486 - an antiprogestin and antiglucocorticoid. Contraception, 48, 403-444.
25. Tarantal, A.F., Hendrickx, A.G., Matlin, S.A. et al. (1996) Effects of two antiprogestins on early pregnancy in the long-tailed macaque (Macaca fascicularis). Contraception, 54, 107-115.
26. Teutsch, G. and Philibert, D. (1994) History and perspectives of antiprogestins from the chemist's point of view. Hum. Reprod., 9 (Suppl. 1), 12-31.
27. Vaitukaitis, J., Robbins, J.B., Neischlag, E. et al. (1971) A method for producing specific antisera with small doses of immunogen. J. Clin. Endocrinol., 33, 988-991.
28. Westphal, U. (1986) Steroid-Protein Interactions II. Springer-Verlag, Berlin, pp. 1-7; 26-44.