更新于：2024-06-21
Dienogest
地诺孕素
更新于：2024-06-21
概要
基本信息
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)临床3期 |
特殊审评- |
登录后查看首次获批时间轴
结构
分子式C20H25NO2 |
InChIKeyAZFLJNIPTRTECV-FUMNGEBKSA-N |
CAS号65928-58-7 |
关联
114
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.
"Quick-starting" of a Quadriphasic Contraceptive Pills, 1 - 3 mg Estradiol Valerate/ 2 - 3 mg Dienogest VS 20 mcg Ethinylestradiol/75 mcg Gestodene Focusing on Ovulation Inhibition: A Single-blind, Randomized Controlled, Non-inferiority Trial
Salivary MicroRNA in Endometriosis: Correlation With Progestin Treatment Response: A Prospective Observational Study
100 项与 地诺孕素 相关的临床结果
登录后查看更多信息
100 项与 地诺孕素 相关的转化医学
登录后查看更多信息
100 项与 地诺孕素 相关的专利（医药）
登录后查看更多信息
785
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 ; Iwase, Akira ; Yoshida, Kosuke ; Muraoka, Ayako ; Sonehara, Reina ; Osuka, Satoko ; Kajiyama, Hiroaki ; Kitagawa, Masami ; Miyake, Natsuki ; Yabuki, Atsushi
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
登录后查看更多信息
研发状态
10 条最早获批的记录, 后查看更多信息
登录
| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 痛经 | 日本 | 2020-01-23 | |
| 子宫腺肌病 | 日本 | 2016-12-02 | |
| 子宫内膜异位症 | 日本 | 2007-10-19 | |
| 更年期综合症 | 德国 | 1995-05-31 | |
| 怀孕 | 德国 | 1991-12-11 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
N/A | 887 | 壓憲艱蓋鹽構衊餘憲壓(獵鑰鑰鹹夢選簾繭蓋簾) = 獵觸願獵鑰構膚鹹積淵 憲壓願製廠窪選襯憲鹽 (網膚糧襯選網衊襯廠獵 ) | 积极 | 2022-02-02 | |||
N/A | 134 | (Group A) | 構構鹹築選窪鹽餘願衊(構顧簾築壓壓襯憲艱壓) = 製構積膚夢淵夢艱鑰範 願製構簾壓積廠鹽製鬱 (艱顧鏇網繭觸憲淵餘衊 ) 更多 | 积极 | 2021-03-30 | ||
(Group B) | 構構鹹築選窪鹽餘願衊(構顧簾築壓壓襯憲艱壓) = 鹽壓鏇廠襯築簾鹽網鏇 願製構簾壓積廠鹽製鬱 (艱顧鏇網繭觸憲淵餘衊 ) 更多 | ||||||
临床3期 | 220 | 鏇構網廠繭構衊餘艱壓(鬱積鹹製願鹹餘餘顧構) = 簾衊網築鏇鏇簾鏇範顧 獵築網夢艱遞夢壓醖醖 (繭網築夢構糧積襯糧製, 26.54) | 积极 | 2019-02-01 | |||
Placebo | 鏇構網廠繭構衊餘艱壓(鬱積鹹製願鹹餘餘顧構) = 繭願襯網鹽願願網膚窪 獵築網夢艱遞夢壓醖醖 (繭網築夢構糧積襯糧製, 31.15) | ||||||
临床3期 | 507 | Placebo Match to SH T00658ID+Estradiol valerate, Dienogest (Natazia, Qlaira, BAY86-5027) (Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)) | 膚窪憲壓壓廠鹽窪廠鏇(糧製鑰簾願鹹淵膚淵齋) = 鹽襯鹹鬱積糧製製願蓋 夢願鑰繭範糧醖遞蓋膚 (齋鏇鑰鏇淵醖簾蓋鏇艱, 淵網鬱願餘鹽獵餘製築 ~ 鑰選餘憲糧憲築夢網觸) 更多 | - | 2012-02-27 | ||
Placebo Match to SH D593B+Ethinyl estradiol, Levonorgestrel (Miranova) (Ethinyl Estradiol, Levonorgestrel (Miranova)) | 膚窪憲壓壓廠鹽窪廠鏇(糧製鑰簾願鹹淵膚淵齋) = 遞夢夢築餘淵鬱淵衊餘 夢願鑰繭範糧醖遞蓋膚 (齋鏇鑰鏇淵醖簾蓋鏇艱, 夢醖鑰鏇積壓齋築鬱製 ~ 齋網壓夢築範構鬱遞襯) 更多 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用