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更新于：2025-07-15
Menatetrenone
四烯甲萘醌
更新于：2025-07-15
概要
基本信息
原研机构- |
非在研机构 |
权益机构- |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国) |
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结构/序列
分子式C31H40O2 |
InChIKeyDKHGMERMDICWDU-GHDNBGIDSA-N |
CAS号863-61-6 |
关联
62
项与 四烯甲萘醌 相关的临床试验NCT06385275
The Role of Vitamin K on Knee Osteoarthritis Outcomes
CTR20250946
评估受试制剂四烯甲萘醌软胶囊（规格：15 mg）与参比制剂固力康®（规格：15 mg）在中国健康成年参与者空腹状态下的单中心、开放、随机、单剂量、四周期、两序列、完全重复交叉生物等效性试验
CTR20244462
评估受试制剂四烯甲萘醌软胶囊（规格：15mg）与参比制剂固力康®（规格：15mg）在中国健康成年受试者空腹和餐后状态下的单中心、开放、随机、单剂量、四周期、两序列、完全重复交叉生物等效性研究
100 项与 四烯甲萘醌 相关的临床结果
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100 项与 四烯甲萘醌 相关的转化医学
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100 项与 四烯甲萘醌 相关的专利（医药）
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1,914
项与 四烯甲萘醌 相关的文献（医药）2025-09-01PHYTOMEDICINE
Emodin-induced ERα degradation via SYVN1 alleviates vascular calcification by preventing HIF-1α deacetylation in chronic kidney disease
Article
作者: Wang, Xu ; Wu, Fupeng ; Hao, Yuxuan ; Chen, Yongyan ; Han, Xu ; Tan, Sheng ; Ye, Huijing ; Shen, Xiaoyan ; Hong, Yang
BACKGROUND:
Vascular calcification is a major cause of death in chronic kidney disease (CKD), with osteoblastic transdifferentiation of vascular smooth muscle cells (VSMCs) considered to be the crucial pathologic process. However, there remains a significant deficiency in effective prevention and treatment strategies.
PURPOSE:
In an in vitro calcification screening model, we observed an inhibitory activity of Emodin on osteoblastic transdifferentiation of VSMCs. In the present study, we therefore aimed to evaluate its efficacy in CKD-induced medial vascular calcification in vitro and in vivo, and to further explore the underlying mechanisms.
STUDY DESIGN:
A7R5 and MOVAS cells were treated with sodium phosphate to induce osteogenic transdifferentiation as in vitro models, while mice were fed with adenine and a high-phosphorus diet, and additionally received an intraperitoneal injection of 10,000 IU Vitamin D3 to induce chronic kidney disease (CKD) as an in vivo model. Vitamin K2 served as a positive control.
METHODS:
Alizarin Red S staining and VON-KOSSA staining were used to evaluate the effects of Emodin on osteogenic transdifferentiation. Western blotting, RT-qPCR and Von-Kossa staining were used to detect the effects of Emodin on aortic calcification in CKD mice in vivo. Chemical biology techniques including ITC, fluorescence titration, dual fluorescein reporter genes, CETSA, and DARTS, were used to detect the binding activity of Emodin to ERα and SYVN1. Immunoprecipitation, immunostaining, etc. were used to explore the mechanisms, and small molecule inhibitors and small RNA interference were used to verify the target of Emodin.
RESULTS:
Emodin could effectively inhibit the osteogenic transdifferentiation of A7R5 and MOVAS cells in vitro, and alleviate aortic calcification in CKD mice in vivo. Mechanism study revealed that Emodin could act as a molecular glue that binds directly to ERα and SYVN1 and enhances their interaction, thereby accelerating the ubiquitination degradation process of ERα. The decrease in ERα diminished the inhibition of ERα on the deacetylation of HIF-1α by SIRT6, thereby inhibiting VSMC osteogenic transdifferentiation and relieving the vascular cells calcification.
CONCLUSION:
Our study demonstrates that ERα has a non-genomic effect to inhibit the deacetylation of HIF-1α by SIRT6, which can be abrogated by Emodin through SYVN1-mediated ERα degradation. These results provide evidences for Emodin to serve as a candidate drug for controlling clinical vascular calcification in CKD.
2025-08-18Journal of the American Nutrition Association
Exploring Menatetrenone: Origin, Chemistry, Therapies and Delivery
Review
作者: Singh, Widhilika ; Kushwaha, Poonam ; Kushwaha, Shom Prakash
Menatetrenone (MK-4), a potent form of vitamin K2, has gained significant attention for its diverse therapeutic potential, particularly in bone health, cardiovascular protection, and metabolic disorders. This manuscript explores the origins and chemical structure of menatetrenone, highlighting its synthesis from dietary sources and its enzymatic conversion in the body. The review examines the extensive therapeutic applications of MK-4, focusing on its role in treating osteoporosis, diabetes, and cardiovascular diseases, along with emerging evidence of its anticancer and neuroprotective effects. Furthermore, the manuscript discusses innovative delivery systems, such as nanostructured lipid carriers and other advanced formulations, designed to enhance the bioavailability and therapeutic efficacy of menatetrenone. By addressing the challenges associated with its pharmacokinetics and exploring novel drug delivery strategies, this review provides a comprehensive overview of menatetrenone's therapeutic promise and outlines future directions for its clinical use.
2025-07-03Epigenomics
The epigenetic potential of vitamin K2 in brain health
Review
作者: Fuso, Andrea ; Maresz, Katarzyna ; Miraglia, Niccolò ; Neofytou, Ioannis E ; Kontogiorgos, Ioannis ; Jeanne, Jean-Francois ; Roumeliotis, Stefanos ; Cavallaro, Rosaria A
Vitamin K2 refers to a subfamily of vitamin K isoforms known as Menaquinones and, therefore, indicated as MK-n, the "n" indicating the number of isoprene units present in the side chain. Like the other members of the Vitamin K family, K2 is an enzymatic cofactor for the γ-glutamyl carboxylase (GGCX). This enzyme's substrates, which carboxylate glutamic acid residues, are known as Vitamin K-dependent proteins (VKDPs). Besides being involved in bone homeostasis, vitamin K exerts its primary function in the coagulation process. More recently, a function of Vitamin K also in brain homeostasis has been claimed. In addition to these so-called "canonical" effects, recent research highlights the possibility that Vitamin K, particularly Vitamin K2 May 2001have or induce epigenetic effects through the modulation of DNA methylation, histone modifications, and microRNAs expression. This evidence seems particularly relevant in brain diseases, where epigenetics is gaining a central role as a modulator of multiple diseases-associated molecular metabolisms. The present review examines the recent literature (PubMed) to collect evidence for the role of Vitamin K2 in neurodegenerative diseases with the goal of fostering interest in its epigenetic potential.
100 项与 四烯甲萘醌 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 绝经期后骨质疏松 | 中国 | 2013-07-21 | |
| 维生素K缺乏性出血 | 日本 | 2012-05-25 | |
| 维生素K缺乏性出血 | 日本 | 2012-05-25 | |
| 疼痛 | 中国 | 2010-06-29 | |
| 骨质疏松症 | 日本 | 1995-06-30 | |
| 出血 | 日本 | 1972-06-29 | |
| 低凝血酶原血症 | 日本 | 1972-06-29 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 肝细胞癌 | 临床3期 | 日本 | 2004-03-01 | |
| 脑出血 | 临床前 | 日本 | 2024-05-10 | |
| 白血病 | 临床前 | 日本 | 2007-11-16 |
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临床结果
临床结果
适应症
分期
评价
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N/A | 40 | Vitamin K2 (MK-7) 120 g/d | 襯淵簾簾觸顧鬱願衊糧(鹹淵壓築艱衊艱衊顧積) = 獵醖餘鹽膚網餘壓淵顧 積積淵構膚繭製鏇壓獵 (襯鏇獵鬱餘淵艱襯繭鏇 ) | 积极 | 2023-05-04 | ||
N/A | 389 | Vitamin K2 (720 μg/day) and Vitamin D (25 μg/day) | 糧壓艱鹹鹹構製獵範鹽(繭醖壓餘築蓋選製蓋繭) = 蓋願繭蓋積淵膚選齋廠 廠鹹鑰鬱憲製憲繭繭膚 (淵淵壓鑰齋窪積網壓淵 ) 更多 | - | 2022-08-28 | ||
糧壓艱鹹鹹構製獵範鹽(繭醖壓餘築蓋選製蓋繭) = 餘壓艱獵築憲蓋製選遞 廠鹹鑰鬱憲製憲繭繭膚 (淵淵壓鑰齋窪積網壓淵 ) 更多 | |||||||
N/A | matrix Gla protein (MGP) | 120 | 築壓鹽襯範獵衊鏇顧選(艱遞顧鬱蓋壓鹹窪齋築) = 艱鑰鏇顧繭鏇艱糧壓憲 簾蓋獵窪積鹽鹹選積範 (繭壓觸淵鑰衊糧鬱艱顧 ) | 积极 | 2022-05-03 | ||
築壓鹽襯範獵衊鏇顧選(艱遞顧鬱蓋壓鹹窪齋築) = 膚壓觸廠積網鏇築簾鬱 簾蓋獵窪積鹽鹹選積範 (繭壓觸淵鑰衊糧鬱艱顧 ) | |||||||
N/A | 46 | (Women with Postmenopausal Osteoporosis) | 繭鏇鬱鏇齋鹽襯壓糧壓(壓觸獵夢齋蓋範選網範) = 觸蓋鬱築壓選衊鬱選構 選鑰糧夢選蓋鹽觸醖餘 (餘觸夢繭願顧餘鹽鏇繭, 10.09) 更多 | - | 2022-03-24 | ||
(Postmenopausal Women without Osteoporosis) | 繭鏇鬱鏇齋鹽襯壓糧壓(壓觸獵夢齋蓋範選網範) = 鑰鹹積壓鹽廠遞顧夢範 選鑰糧夢選蓋鹽觸醖餘 (餘觸夢繭願顧餘鹽鏇繭, 6.94) 更多 | ||||||
N/A | 18 | Vitamin K2 (Menaquinone-7) 75 μg | 簾壓蓋憲艱築憲膚蓋選(壓獵餘製鹹築糧夢鹽顧) = 壓艱遞壓簾選製糧齋憲 顧壓鬱繭鹹蓋襯鏇醖淵 (廠顧餘齋鏇憲蓋鏇艱憲 ) 更多 | 不佳 | 2021-04-01 | ||
N/A | 血管钙化 uncarboxylated-MGP | 102 | Vitamin K2 supplementation (200μg/day) | 糧膚鑰艱繭鬱願鏇繭糧(淵繭鹹構鑰範選蓋範製) = 糧襯繭遞築醖窪憲築醖 範醖餘夢觸夢網繭鹹獵 (膚製糧鏇衊淵鬱選艱壓 ) 更多 | 不佳 | 2019-06-13 | |
(Control (no treatment)) | 糧膚鑰艱繭鬱願鏇繭糧(淵繭鹹構鑰範選蓋範製) = 蓋憲醖鹽襯餘艱艱夢壓 範醖餘夢觸夢網繭鹹獵 (膚製糧鏇衊淵鬱選艱壓 ) 更多 | ||||||
临床4期 | 50 | Vitamin K2 (menaquinone-7) | 鑰醖鹹獵夢選遞築願積(襯襯鑰獵齋願觸範獵鏇) = 醖顧襯蓋鬱蓋顧簾遞鏇 淵鹹艱齋衊選醖齋鬱築 (築廠鹹窪廠製窪壓夢築 ) | - | 2017-06-07 | ||
临床4期 | 血液透析并发症 dp-ucMGP | MGP | vitamin K2 | 50 | Vitamin K2 (menaquinone-7) | 艱積範壓艱糧範壓淵繭(醖窪願窪鹽艱築憲觸簾) = 鹹築積鬱糧簾襯選醖襯 蓋選積糧淵獵遞憲繭糧 (願淵鏇醖廠遞簾鑰選繭 ) | 积极 | 2017-05-26 | |
临床4期 | 42 | Vitamin K2 + cholecalciferol (K+D) | 鑰簾憲積網網壓構顧顧(窪簾糧艱選蓋鏇餘繭窪) = 鹽窪廠鬱壓餘獵淵廠遞 築夢艱窪繭願選窪範艱 (齋壓淵鹽遞艱遞醖糧襯 ) | - | 2015-01-01 | ||
Cholecalciferol (D) | 鑰簾憲積網網壓構顧顧(窪簾糧艱選蓋鏇餘繭窪) = 廠鬱製憲願鏇選鏇鑰壓 築夢艱窪繭願選窪範艱 (齋壓淵鹽遞艱遞醖糧襯 ) | ||||||
N/A | 慢性肾病 dp-ucMGP positive | MGP positive | osteocalcin | 42 | Vitamin K2 (menaquinone-7, MK-7) + cholecalciferol | 築襯鬱觸衊襯衊遞觸網(夢選簾網醖廠範製餘襯) = 淵鏇鏇齋顧糧廠餘淵願 築艱糧壓鏇艱獵網觸窪 (製膚鏇廠餘夢窪淵憲壓, 1077.1±507.7) 更多 | 积极 | 2014-05-01 | |
築襯鬱觸衊襯衊遞觸網(夢選簾網醖廠範製餘襯) = 獵醖齋網鏇觸醖艱淵壓 築艱糧壓鏇艱獵網觸窪 (製膚鏇廠餘夢窪淵憲壓, 793.9±400.3) 更多 |
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