Toxicology of dienogest

Drugs of Today

Volumn 35, Issue SUPPL. C, 1999, Pages 13-26

  Zimmermann, H ^a   Hoffmann, H ^a   Mathieu, M ^b   Oettel, M ^a  

^a BAYER PHARMA AG   (Germany)

^b Laboratoire Innothera   (France)

Author keywords

[No Author keywords available]

Indexed keywords

DIENOGEST;

ACUTE TOXICITY; AMES TEST; AREA UNDER THE CURVE; CHRONIC TOXICITY; DRUG CARCINOGENICITY; EMBRYOTOXICITY; ESTROGEN ACTIVITY; GENOTOXICITY; HUMAN; MICRONUCLEUS TEST; MUTAGEN TESTING; NONHUMAN; REPRODUCTIVE TOXICITY; REVIEW; TERATOGENICITY; TOXICITY TESTING; TOXICOKINETICS;

EID: 0032802404     PISSN: 16993993     EISSN: 16994019     Source Type: Journal    
DOI: None     Document Type: Review

References (43)

1. Oettel, M., Bervoas-Martin, B., Elger, W. et al. A 19-norprogestin without 17alpha-ethinyl group. I: DNG from a pharmacokinetic point of view. Drugs of Today 1995, 31: 499-516.
2. Oettel, M., Carol, W., Elger, W. et al. A 19-norprogestin without 17α-ethinyl group. II: DNG from a pharmacodynamic point of view. Drugs of Today 1995, 31: 517-36.
3. Tkocz, R., Hillesheim, H.G., Schmidt, G., Hoffmann, H. Serum lipoprotein changes in female rats treated with progesterone or synthetic gestagens alone or in combination with estradiol. I. Total and fractionated cholesterol and lipoprotein pattern. Exp Clin Endocrinol 1988, 91: 319-26.
4. Tkocz, R., Hillesheim, H.G., Schmidt, G., Hoffmann, H. Serum lipoprotein changes in female rats treated with progesterone alone or in combination with estradiol. II. Serum triglycerides and hepatic triglyceride release. Exp Clin Endocrinol 1988, 92: 7-12.
5. Hillesheim, H.G., Hoffmann, H. Data on acute toxicity of the progestin STS 557. Exper Clin Endocrinol 1983, 81: 175-8.
6. 50 values in newborn and adult animals. Toxicol Appl Pharmacol 1971, 18: 185-207.
7. Günzel, P. Methode der tierexperimentellen Verträglichkeitsprüfung von hormonalen Kontrazeptiva. In: Methodik der Steroidtoxikologie. Plotz, E.J., Haller, J. (Eds.). Thieme Verlag: Stuttgart 1971, 1-6.
8. Hoffmann, H. DNG - 28-31 Day Toxicity Study in the Female Beagle Dog by Oral Administration. Jenapharm Company documentation 1977.
9. Stade, K. DNG - 6 Month Toxicity Study in the Rat by Oral Administration. Jenapharm Company documentation 1978.
10. Hoffmann, H., Hillesheim, H.G., Güttner, J., Stade, K., Merbt, E.-M., Holle, K. Long term toxicological studies on the progestin STS 557. Exper Clin Endocrinol 1983, 81: 179-96.
11. Hillesheim, H.G., Hoffmann, H. DNG - 6 Month Toxicity Study in Beagle Dogs by Oral Administration. Jenapharm Company documentation 1980.
12. Hillesheim, H.G., Hoffmann, H., Güttner, J., Oettel, M. Toxicity of the progestagen STS 557 compared to levonorgestrel in Beagles after oral administration for 6 months. Arch Toxicol 1983, Suppl 5: 221-4.
13. Hoffmann, H., Zimmermann, H., Hillesheim, H.G. et al. Pharmakologisch-toxikologisches Wirkprofil von Dienogest. In: Dienogest. Präklinik und Klinik eines Gestagens. Teichmann, A.T. (Ed.), W. de Gruyter: Berlin 2. Auflage 1995, 59-72.
14. Stewart, J.S. DNG - Preliminary Toxicity Study by Oral (Gavage) Administration to CD-1 Mice for 13 Weeks. Jenapharm Company documentation 1996.
15. Richard, J. Reproductive Function and Fertility Study by Oral Route in Female Rats. Jenapharm Company documentation 1993.
16. Lehmann, M., Putz, B., Poggel, H.A. Experimental toxicity studies with contraceptive steroids and their relevance for human risk estimation. In: Advances in Applied Toxicology. Dayan, A.D., Paine, A.J. (Eds.). Taylor & Francis: London 1989, 51-79.
17. Hendrickx, A.G., Binkerd, P.E. Teratogenicity studies in of sex hormones. In: Safety Requirements for Contraceptive Steroids. Michal, F. (Ed.). University Press: Cambridge 1989, 289-322.
18. Richard, J. Embryotoxicity/Teratogenicity Study by Oral Route in Rats. Jenapharm Company documentation 1993.
19. Richard, J. Embryotoxicity/Teratogenicity Study by Oral Route in Rabbits. Jenapharm Company documentation 1993.
20. Klaus, S. Prenatal toxic effect of STS 557. Exp Clin Endocrinol 1983, 81: 197-205.
21. Heinecke, H., Köhler, D. Prenatal toxic effects of STS 557. Exp Clin Endocrinol 1983, 81: 206-9.
22. Strecke, J., Oettel, M., Tiroke, I., Ohme, E. Influence of neonatally administered gestagens on fertility in rat. In: Hormones and Brain Development. Dörner, K., Kawakami, M.(Eds.). Elsevier/North-Holland Biomed Press: Amsterdam 1978, 205-13.
23. Oettel, M., Kurischko, A., Strecke, J., Koch, M. Embryotoxic effects of post-coital fertility inhibiting steroids. Archiv Toxicol Suppl 1980, 4: 248-51.
24. Wollny, H.E. Salmonella Typhimurium Reverse Mutation Assay with DNG. Jenapharm Company documentation 1995.
25. Marzin, D. Mutation Assay at the TK Locus in L5178Y Mouse Lymphoma Cells Using a Microtiter Cloning Technique. Jenapharm Company documentation 1994.
26. Marzin, D. Test for Chromosome Aberrations by in vitro Human Lymphocyte Metaphase Analysis. Jenapharm Company documentation 1995.
27. Völkner, W. Micronucleus Assay in Bone Marrow Cells of the Mouse with DNG. Jenapharm Company documentation 1995.
28. Jemilev, Z., Komor, A., Strecke, J., Oettel, M., Schubert, K. Chromosome analysis after treatment of pregnant baboons with potential postovulatoric fertility inhibiting steroids in the mothers and their offspring. Zentralbl Gynäkol 1981, 103: 1215-19.
29. Schöneich, J., Becker, K., Braun, R. Investigations on the mutagenic activity of STS 557. Exp Clin Endocrinol 1983, 81: 210-16.
30. Strecke, J., Komor, A., Jemilew, Z., Schubert, K. Chromosome analysis on female baboons after treatment with STS 557 or Levonorgestrel. Zentralbl Gynäkol 1985, 107: 304-7.
31. Völkner, W. Unscheduled DNA synthesis in primary hepatocytes of female rats in vitro with DNG. Jenapharm Company documentation 1995.
32. Ward, P. DNG - Measurement of Unscheduled DNA Synthesis in Rat Hepatocytes in Vitro (JPH04894). Jenapharm Company documentation 1995.
33. Völkner, W. In Vivo/in Vitro Unscheduled DNA Synthesis in Rat Hepatocytes (JPH05495). Jenapharm Company documentation 1996.
34. Oesterle, D., Deml, E. Prüfung der initiierenden Wirksamkeit von Dienogest und Chlormadinonacetat im Rat Liver Foci Bioassay. In: Dienogest. Präklinik und Klinik eines Gestagens. Teichmann, A.T. (Ed.). W. de Gruyter: Berlin 2. Auflage 1995, 73-8.
35. Deml, E., Schwarz, R., Oesterle, D. Initiation of enzyme-altered foci by the synthetic steroid cyproterone acetate in rat liver foci bioassay. Carcinogenesis 1993, 14: 1229-31.
36. Sykes, A.K. An Assessment of Fixed Material from a Study in Rats. Addendum to Final Report. Jenapharm Company documentation 1993.
37. Elger, W., Schneider, B. Kontrollierte Studie zum Vergleich der uterotropen Wirkung von DNG, Norethisteronazetat und Levonorgestrel bei ovarektomierten Ratten im Uteruswachstumtest. Jenapharm Company documentation 1993.
38. Eletreby, M.F., Beier, S., Günzel, P. Comparative endocrine pharmacodynamics of contraceptive steroids. In: Safety Requirements for Contraceptive Steroids. Michel, F. (Ed.). University Press: Cambridge 1989, 179-92
39. Neumann, F., Elger, W. Kritische Überlegungen zu den biologischen Grundlagen von Toxizitätsstudien mit Steroid-(Sexual-)hormonen. In: Methodik der Steroidtoxikologie. Plotz, E.J., Haller, J. (Eds.). G. Thieme Verlag: Stuttgart 1971, 6-48.
40. Stewart, J.S. Dienogest. Oncogenicity Study by Oral (Gavage) Administration to CD-1 Mice for 104 Weeks. Jenapharm Company documentation 1998.
41. Elger, W., Gran, H., Schneider, B. Determination of Hormonally Active Dose Levels of DNG at Oral Administration in Ovariectomized Mice: Dose Finding for Cancerogenicity Studies in Mice. Jenapharm Company documentation 1995.
42. Hobe, G., Schön, R., Frankenberg, G., Schade, W., Schubert, K. Urinary metabolites of the new progestagen STS 557 (17α-cyanomethyl-17-hydroxy-4,9-estradien-3-one) in the dog and rat. Steroids 1983, 41: 23-32
43. Jordan, A. FDA requirements for non-clinical testing of contraceptive steroids. Contraception 1992, 46: 499-509.