Antiovulatory and postcoital antifertility activity of the antiprogestin CDB-2914 when administered as single, multiple, or continuous doses to rats

Contraception

Volumn 58, Issue 2, 1998, Pages 129-136

  Reel, Jerry R ^a,c   Hild Petito, Sheri ^a   Blye, Richard P ^b  

^a NATIONAL INSTITUTES OF HEALTH   (United States)

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

^c BIOQUAL INC   (United States)

Author keywords

Antagonist; Anti implantation; Contraception; Endometrium

Indexed keywords

17ALPHA ACETOXY 11BETA (4 DIMETHYLAMINOPHENYL) 19 NORPREGNA 4,9 DIENE 3,20 DIONE; ANTIGESTAGEN; MIFEPRISTONE; POSTCOITUS CONTRACEPTIVE AGENT; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL TISSUE; ARTICLE; CONTRACEPTION; CONTROLLED STUDY; DELAYED IMPLANTATION; DOSE RESPONSE; DRUG POTENCY; FEMALE; NONHUMAN; ORAL DRUG ADMINISTRATION; OVULATION INHIBITION; PREGNANCY RATE; RAT;

ANIMALS; CONTRACEPTIVES, POSTCOITAL, SYNTHETIC; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG ADMINISTRATION SCHEDULE; FEMALE; FERTILITY; MIFEPRISTONE; NORPREGNADIENES; OVULATION; PREGNANCY; RATS; RATS, SPRAGUE-DAWLEY;

EID: 0032144512     PISSN: 00107824     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0010-7824(98)00067-5     Document Type: Article

References (36)

1. Glasier A., Thong K.J., Dewar M., Mackie M., Baird D.J. Mifepristone (RU486) compared with high-dose estrogen and progestogen for emergency postcoital administration. N Engl J Med. 327:1992;1041-1044.
2. Glasier A. Emergency postcoital contraception. N Engl J Med. 337:1997;1058-1064.
3. Blye R.P. The effect of estrogens and related substances on embryonic viability. Raspe G. Advances in Biosciences 4. Schering Symposium on Mechanisms Involved in Conception. 1970;323-343 Pergamon Press/Vieweg, Braunschweig.
4. Blye R.P. The use of estrogens as postcoital contraceptive agents. Am J Obstet Gynecol. 116:1973;1044-1050.
5. Dixon G.W., Schlesselman J.J., Ory H.W., Blye R.P. Ethinyl estradiol and conjugated estrogens as postcoital contraceptives. JAMA. 244:1980;1336-1339.
6. Ledger W.L., Sweeting V.M., Hillier H., Baird D.J. Inhibition of ovulation by low-dose mifepristone (RU486). Hum Reprod. 7:1992;945-950.
7. Ling W.Y., Wrixon W., Zayid I., Acorn T., Popat R., Wilson E. Mode of action of dl-norgestrel and ethinylestradiol combination in postcoital contraception. II. Effect of postovulatory administration on ovarian function and endometrium. Fertil Steril. 39:1983;292-297.
8. Rowlands S., Kubba A.A., Guillebaud J., Bounds W.A. A possible mechanism of action of danazol and an ethinyl/norgestrel combination used as postcoital contraceptive agents. Contraception. 33:1986;539-545.
9. Swahn M.-L., Westlund P., Johannisson E., Bygdeman M. Effect of postcoital conceptive methods on the endometrium and the menstrual cycle. Acta Obstet Gynecol Scand. 75:1996;738-744.
10. Liu J.H., Garzo G., Morris S., Stuenkel C., Ulmann A., Yen S.S.C. Disruption of follicular maturation and delay of ovulation after administration of the antiprogesterone RU486. J Clin Endocrinol Metab. 65:1987;1135-1140.
11. Swahn M.-L., Bygdeman M., Cekan S., Xing S., Masironi B., Johannisson E. The effect of RU486 administered during the early luteal phase on bleeding pattern, hormonal parameters and endometrium. Hum Reprod. 5:1990;402-408.
12. Gemzell-Danielsson K., Swahn M.-L., Svalander P., Bygdeman M. Early luteal phase treatment with mifepristone (RU486) for fertility regulation. Hum Reprod. 8:1993;870-873.
13. Croxatto H.B., Salvatierra A.M., Croxatto H.D., Fuentealba B. Effects of continuous treatment with low dose mifepristone throughout one menstrual cycle. Hum Reprod. 8:1993;201-207.
14. Gemzell-Danielsson K., Swahn M.-L., Westlund P., Johannisson E., Seppälä M., Bygdeman M. Effect of low daily doses of mifepristone on ovarian function and endometrial development. Hum Reprod. 12:1997;124-131.
15. Psychoyos A., Prapas I. Inhibition of egg development and implantation in rats after postcoital administration of the progesterone antagonist RU486. J Reprod Fertil. 80:1987;487-491.
16. Roblero L.S., Croxatto H.B. Effect of RU486 on development and implantation of rat embryos. Mol Reprod Develop. 29:1991;342-346.
17. Dao B., Vanage G., Marshall A., Bardin C.W., Koide S.S. Anti-implantation activity of antiestrogens and mifepristone. Contraception. 54:1996;253-258.
18. Batista M.C., Bristow T.L., Mathews J., Stokes W.S., Loriaux D.L., Nieman L.K. Daily administration of the progesterone antagonist RU486 prevents implantation in the cycling guinea pig. Am J Obstet Gynecol. 165:1991;82-86.
19. Ghosh D., Sengupta J., Hendrickx A.G. Effect of single-dose, early luteal phase administration of mifepristone (RU486) on implantation stage endometrium in the rhesus monkey. Hum Reprod. 11:1996;2026-2035.
20. Nayak N.R., Ghosh D., Lasley B.L., Sengupta J. Anti-implantation activity of luteal phase mifepristone administration is not mimicked by prostaglandin synthesis inhibitor or prostaglandin analogue in the rhesus monkey. Contraception. 55:1997;103-114.
21. Batista M.C., Cartledge T.P., Zellmer A.W., et al. Delayed endometrial maturation induced by daily administration of the antiprogestin RU486 a potential new contraceptive strategy . Am J Obstet Gynecol. 167:1992;60-65.
22. Gemzell-Danielsson K., Svalander P., Swahn M.-L., Johannisson E., Bygdeman M. Effects of a single post-ovulatory dose of RU486 on endometrial maturation in the implantation phase. Hum Reprod. 9:1994;2398-2404.
23. Cameron S.T., Critchley H.O.D., Thong K.J., Buckley C.H., Williams A.R., Baird D.J. Effects of daily low dose mifepristone on endometrial maturation and proliferation. Hum Reprod. 11:1996;2518-2526.
24. Guide for the Care and Use of Laboratory Animals. 1996;National Research Council, National Academy Press, Washington, DC.
25. Heikinheimo O. Clinical pharmacokinetics of mifepristone. Clin Pharmacokinet. 33:1997;7-17.
26. Ringstrom S.J., Szabo M., Kilen S.M., Saberi S., Knox K.L., Schwartz N.B. The antiprogestins RU486 and ZK98299 affect follicle-simulating hormone secretion differentially on estrus, but not on proestrus. Endocrinology. 138:1997;2286-2290.
27. Elger W., Beier S., Chwalisz K., et al. Studies on the mechanisms of action of progesterone antagonists. J Steroid Biochem. 25:1986;835-845.
28. Schubert C., Donath J., Michna H., Nishino Y. The antiovulatory activity of progesterone antagonists is not correlated to their antiprogestational potency in the rat. J Steroid Biochem Molec Biol. 59:1996;75-82.
29. Klein-Hitpass L., Cato A.C.B., Henderson D., Ryffel G.U. Two types of antiprogestins identified by their differential action in transcriptionally active extracts from T47D cells. Nucleic Acids Res. 19:1991;1227-1234.
30. Horwitz K. The molecular biology of RU486. Is there a role for antiprogestins in the treatment of breast cancer? Endocr Rev. 13:1992;146-163.
31. Satorius C.A., Tung L., Takimoto G.S., Horwitz K.B. Antagonist-occupied human progesterone receptors bound to DNA are functionally switched to transcriptional agonists by cAMP. J Biol Chem. 268:1993;9262-9266.
32. Delabre K., Guiochon-Mantel A., Milgrom E. In vivo evidence against the existence of antiprogestins disrupting receptor binding to DNA. Proc Natl Acad Sci USA. 90:1993;4421-4425.
33. Truss M., Bartsch J., Beato M. Antiprogestins prevent progesterone receptor binding to hormone responsive elements in vivo. Proc Natl Acad Sci USA. 91:1994;11333-11337.
34. Teutsch G., Philibert D. History and perspectives of antiprogestins from the chemist's point of view. Hum Reprod. 9:(suppl 1):1994;12-31.
35. Tarantal A.F., Hendrickx A.G., Matlin S.A., et al. Effects of two antiprogestins on early pregnancy in the long-tailed macaque (Macaca fascicularis). Contraception. 54:1996;107-115.
36. Passaro M., Piquion J., Mullen N., Sutherland D., Alexander N., Nieman L. Safety and luteal phase effects of the antiprogestin CDB-2914 in normally cycling women. Endocrine Society Abstracts. 227:1997;1-370.