دورية أكاديمية
Development of the selective progesterone receptor modulator CDB-2914 for clinical indications.
| العنوان: | Development of the selective progesterone receptor modulator CDB-2914 for clinical indications. |
|---|---|
| المؤلفون: | Blithe DL; Department of Health and Human Services, National Institute of Child Health and Human Development, National Institutes of Health Building 61E, Room 8B13, Bethesda, MD 20892, USA. blithed@nih.gov, Nieman LK, Blye RP, Stratton P, Passaro M |
| المصدر: | Steroids [Steroids] 2003 Nov; Vol. 68 (10-13), pp. 1013-7. |
| نوع المنشور: | Clinical Trial; Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Elsevier Country of Publication: United States NLM ID: 0404536 Publication Model: Print Cited Medium: Print ISSN: 0039-128X (Print) Linking ISSN: 0039128X NLM ISO Abbreviation: Steroids Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: New York Ny : Elsevier Original Publication: San Francisco. |
| مواضيع طبية MeSH: | Norpregnadienes/*pharmacokinetics, Contraceptive Agents/chemistry ; Contraceptive Agents/pharmacokinetics ; Dose-Response Relationship, Drug ; Endometrium/drug effects ; Female ; Humans ; Menstrual Cycle/drug effects ; Norpregnadienes/chemistry ; Ovary/drug effects ; Ovulation/drug effects ; Placebos ; Progesterone/metabolism ; Time Factors |
| مستخلص: | CDB-2914 (17 alpha-acetoxy-11 beta-[4-N,N-dimethylaminophenyl]-19-norpregna-4,9-diene-3,20-dione) is a 19-norprogesterone derivative that acts as an antagonist in progesterone-responsive tissues. It binds to progesterone receptors A and B with high affinity. After oral dosing in humans, CDB-2914 serum levels peak at 60-90 min. CDB-2914 binds to serum proteins and is cleared slowly. Doses of 1, 10 and 50 mg exhibit proportional increases in peak serum levels, but serum levels from higher doses, 100 and 200 mg, are not dose-dependent, suggesting saturation of carrier sites. The biological effects of CDB-2914 vary according to time of the menstrual cycle that the drug is given. In the mid-follicular phase, CDB-2914 (50 mg) inhibits follicular development and delays ovulation and menses. At 100 mg, in some cases the original follicle ceases development and a new follicle is recruited. Endometrial maturation is delayed at all doses tested (10, 50, 100 mg). Given at mid-luteal phase, there was a dose-dependent effect on menses, with higher doses (100-200 mg) resulting in earlier menses. On average, CDB-2914 tends to lengthen the menstrual cycle by approximately 1-2 days although the amount of delay varies with timing in the menstrual cycle and dose. |
| المشرفين على المادة: | 0 (Contraceptive Agents) 0 (Norpregnadienes) 0 (Placebos) 4G7DS2Q64Y (Progesterone) 6J5J15Q2X8 (ulipristal) |
| تواريخ الأحداث: | Date Created: 20031212 Date Completed: 20040817 Latest Revision: 20190823 |
| رمز التحديث: | 20221213 |
| DOI: | 10.1016/s0039-128x(03)00118-1 |
| PMID: | 14667994 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 0039-128X |
|---|---|
| DOI: | 10.1016/s0039-128x(03)00118-1 |