更新于：2024-05-05
Dienogest
地诺孕素
更新于：2024-05-05
概要
基本信息
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 德国 (1991-12-11), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C20H25NO2 |
InChIKeyAZFLJNIPTRTECV-FUMNGEBKSA-N |
CAS号65928-58-7 |
关联
101
项与 地诺孕素 相关的临床试验A Bioequivalence study of a randomized, open-label, single dose, two-way crossover design with two-period, two treatment and two-sequence of Dienogest Tablet (2 mg) relative to Originator Dienogest Tablet (2 mg) in healthy Thai female volunteers under fasting condition.
An open label randomized clinical trial to compare the efficacy of Dienogest versus combined oral contraceptive pills (OCPs) using visual analog scale (VAS) for relief of pain associated with Endometriosis - nil
Comparison between Dienogest and GnRH agonist on pregnancy outcome of infertile endometriosis women after laparoscopy
100 项与 地诺孕素 相关的临床结果
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100 项与 地诺孕素 相关的转化医学
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100 项与 地诺孕素 相关的专利（医药）
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786
项与 地诺孕素 相关的文献（医药）2024-03-01Reproductive Biology
Serum miRNA as a predictive biomarker for ovarian reserve after endometrioma-cystectomy
Article
作者: Nakamura, Tomoko ; Bayasura ; Yokoi, Akira ; Nakanishi, Natsuki ; Yoshida, Kosuke ; Iwase, Akira ; Muraoka, Ayako ; Sonehara, Reina ; Osuka, Satoko ; Kajiyama, Hiroaki ; Kitagawa, Masami ; Yabuki, Atsushi ; Miyake, Natsuki
Ovarian endometrioma (OE) is a common gynecological disease that is often treated with surgery and hormonal treatment. However, ovarian cystectomy can impair the ovarian reserve (OR). Previously, we showed that perioperative administration of dienogest (DNG) is an effective option for OR preservation. However, there were differences in the extent of OR preservation among patients following perioperative DNG treatment. In the current study, we performed a global examination of serum microRNAs (miRNAs) to identify accurate biomarkers that predict post-operative restoration of OR following perioperative DNG treatment. We also sought to identify specific miRNAs related to the anti-Müllerian hormone (AMH). miRNA sequencing was performed on serum samples obtained from twenty-seven patients who received perioperative DNG treatment. Candidate miRNAs were selected by comparing patients whose ORs were restored postoperatively (responder group, n = 7) with those whose ORs were not (non-responder group, n = 7). miR-370-3p and miR-1307-3p were significantly upregulated in the responder group, whereas miR-27b-3p was upregulated in the non-responder group. The pretreatment value of each miRNA could predict DNG responsiveness for OR following ovarian cystectomy (area under the curve [AUC] > 0.8). The quantitative polymerase chain reaction (qPCR) revealed only miR-1307-3p was found to be significantly upregulated in the responder group (P < 0.05). In addition, we identified miR-139-3p, miR-140-3p, and miR-629-5p as AMH-associated miRNAs. The transition of AMH showed a correlation with miR-139-3p (P < 0.05, r = -0.76). The miRNAs identified herein represent potential serum biomarkers of clinical value in predicting OR prior to DNG treatment.
2024-03-01European Journal of Obstetrics & Gynecology and Reproductive Biology
Dienogest attenuates STAT3 activation in ovarian endometriotic cysts
Article
作者: Choi, JongYeob ; Choi, DooSeok ; Jo, MinWha ; Lee, Dong-Yun ; Kim, Sung Eun ; Lee, EunYoung
OBJECTIVE:
Recent studies have suggested that endometriosis could be the result of excessive activation of signal transducer and activator of transcription 3 (STAT3), which is associated with the regulation of essential cellular mechanisms such as proliferation, invasion, and apoptosis. That finding implies that regulating STAT3 activation could play a key role in treating endometriosis. In the present study, we aimed to evaluate whether the anti-endometriotic effects of dienogest is mediated by the regulation of STAT3 activation.
STUDY DESIGN:
STAT3 activation was evaluated in normal endometrial and ovarian endometriotic tissues obtained from patients with/without preoperative dienogest treatment. A subsequent in vitro analysis with endometriotic cyst stromal cells (ECSCs) was used to confirm the direct influence of dienogest in STAT3 activation.
RESULT:
STAT3 activation is significantly higher in endometriotic tissues from non-treated patients than in normal endometrial tissues, and that difference is reversed by preoperative administration of dienogest. Similarly, the inhibitory effects of dienogest on STAT3 activation are demonstrated by in vitro results showing that dienogest treatment significantly inhibits IL-6-stimulated STAT3 activation in cultured ECSCs. That inhibition was accompanied by decreased expression of proliferative (PCNA), invasive (MMP-2), and anti-apoptotic (BCL-2) proteins. Furthermore, downregulating STAT3 activity with siRNA decreased PCNA, MMP-2, and BCL-2 expression in IL-6-treated ECSCs.
CONCLUSION:
Dienogest inhibits STAT3 activation in ECSCs, which affects their proliferation, invasiveness, and apoptosis.
2024-02-01Contraception
Comparison of estrogenic components used for hormonal contraception
Review
作者: Stanczyk, Frank Z ; Archer, David F ; Foidart, Jean-Michel ; Winer, Sharon A
Attempts have been made over the years to replace ethinyl estradiol (EE) in combined oral contraceptives (COCs) with the less potent natural estrogen estradiol (E2), or its prodrug, E2 valerate (E2V), to improve their safety and tolerability. Recently, a COC incorporating a novel weak natural estrogen, estetrol (E4), combined with drospirenone, has become available. We present a comparative analysis of the three prevailing estrogens used in COCs, focusing on their structure-function relationships, receptor-binding affinity, potency, metabolism, pharmacokinetic parameters, and pharmacodynamics. The binding affinity of EE to estrogen receptor (ER)α is twice that of E2, whereas its affinity for ERβ is about one-half that of E2. E4 has a lower binding affinity for the ERs than E2. The high potency of EE is notable in its dramatic increase in estrogen-sensitive hepatic globulins and coagulation factors. EE and E2 undergo extensive and comparable metabolism, while E4 produces only a very limited number of metabolites. E4 has the highest bioavailability among the three estrogens, with E2 having <5%. Studies demonstrate consistent ovulation inhibition, although a higher dose of E4 (15 mg) in COCs is required to achieve follicular suppression compared to E2 (1-3 mg) and EE (0.01-0.035 mg). E2 and E4 in COCs may be less stimulatory of coagulant proteins than EE. Studies with E2/dienogest suggest a comparable risk of venous thromboembolism to EE/levonorgestrel, while data assessing risk with an E4-based COC are insufficient. Nevertheless, the E4-based formulation shows promise as a potential alternative to EE and E2 due to its lower potency and possibly fewer side effects.
100 项与 地诺孕素 相关的药物交易
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研发状态
| 适应症 | 最高研发状态 | 国家/地区 | 公司 |
|---|---|---|---|
| 怀孕 | 批准上市 | 德国 更多 | |
| 更年期综合症 | 批准上市 | 德国 更多 | |
| 子宫内膜异位症 | 批准上市 | 俄罗斯 更多 | |
| 痛经 | 批准上市 | 日本 更多 | |
| 子宫腺肌病 | 批准上市 | 日本 更多 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
N/A | 887 | 構鏇選憲衊築願積淵醖(齋襯構構艱構壓廠觸糧) = 簾願構襯衊憲鹽鬱醖簾 鏇獵窪製衊觸襯壓顧淵 (鑰範淵餘構願願遞顧製 ) | 积极 | 2022-02-02 | |||
N/A | 134 | (Group A) | 壓選壓築襯遞餘網窪糧(鏇簾鑰積窪窪淵蓋構鏇) = 蓋蓋廠製餘網選範築製 簾艱範願簾顧鑰壓窪憲 (蓋築壓餘願淵鹹窪積鬱 ) 更多 | 积极 | 2021-03-30 | ||
(Group B) | 壓選壓築襯遞餘網窪糧(鏇簾鑰積窪窪淵蓋構鏇) = 齋襯夢齋製鬱鏇製遞壓 簾艱範願簾顧鑰壓窪憲 (蓋築壓餘願淵鹹窪積鬱 ) 更多 | ||||||
临床3期 | 220 | 選願艱齋築鏇醖齋築範(遞餘遞鑰齋淵願膚顧鬱) = 遞壓糧壓積製鑰鹹廠糧 衊遞網膚餘膚獵積鹽廠 (觸製窪構鹹簾範艱淵蓋, 26.54) | 积极 | 2019-02-01 | |||
Placebo | 選願艱齋築鏇醖齋築範(遞餘遞鑰齋淵願膚顧鬱) = 餘糧繭繭鬱膚糧簾糧鹹 衊遞網膚餘膚獵積鹽廠 (觸製窪構鹹簾範艱淵蓋, 31.15) |
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