Nitroaspirin(Nitroaspirin) - 药物靶点：COX-1_专利_临床

概要

基本信息

药物类型

小分子化药

别名

M-NO-ASA、NO-ASA、NO-aspirin

+ [3]

靶点

COX-1

作用机制

COX-1抑制剂(环氧化酶-1抑制剂)、一氧化氮供体

治疗领域

神经系统疾病心血管疾病内分泌与代谢疾病

在研适应症-

非在研适应症

2型糖尿病间歇性跛行疼痛+ [1]

原研机构

Nicox SA

在研机构-

非在研机构

Nicox Research Institute Srl

Nicox SA

最高研发阶段终止临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构

分子式C16H13NO7

InChIKeyIOJUJUOXKXMJNF-UHFFFAOYSA-N

CAS号175033-36-0

关联

3

项与 Nitroaspirin 相关的临床试验

NCT01001260 / TerminatedN/AIIT

Biosynthesis of PGD2 in Vascular Injury

To investigate the biosynthesis of PGD2 during percutaneous transluminal coronary angioplasty (PTCA) procedure.

开始日期2007-08-01

申办/合作机构

University of Pennsylvania

NCT01256775 / Completed临床2期

A Multicenter, Double-blind, Randomized, Parallel Group Study to Assess the Effect of NCX4016 vs Placebo on Walking Distance in Patients With Peripheral Arterial Occlusive Disease at Leriche-Fontaine Stage II

Peripheral arterial disease (PAD) is almost invariably associated with a generalized atherosclerotic involvement of the arterial tree and endothelial dysfunction. Previous short term studies showed improvement of vascular reactivity and walking capacity in PAD patients by measures aimed at restoring Nitric Oxide (NO) production. NO is also known to prevent the progression of atherosclerosis. We wished to assess whether the prolonged administration of a NO-donating agent (NCX 4016) improves the functional capacity of PAD patients and affects the progression of atherosclerosis as assessed by carotid intima-media thickness (IMT).
Four hundred forty two patients with stable intermittent claudication were enrolled in a prospective, double blind, placebo-controlled study and randomized to either NCX 4016 800mg bid or its placebo for 6 months. The primary study outcome was the absolute claudication distance (ACD) on a constant treadmill test (10% incline, 3km/hr); main secondary end-point was the change of the mean far-wall right common carotid artery IMT.

开始日期2003-09-01

申办/合作机构

Nicox Research Institute Srl

NCT00157508 / Terminated临床2期IIT

A Pilot, Randomised, Double-blind, Cross-over Study to Assess the Renal and Systemic Effects of NCX4016 in Patients With Type 2 Diabetes and Early Nephropathy

Aspirin is commonly used for treatment of painful and inflammatory diseases and in the prevention of the cardiovascular disease. A major drawback of aspirin treatment is the well recognized gastrointestinal toxicity. Recent research indicate that coupling a nitric oxide (NO)derivate to the aspirin moiety retains its therapeutic effects while avoiding its undesirable gastrointestinal side effects. NO has cytoprotective effects, such as blood flow modulation, mucus release and repair of mucosal injury. NCX4016, a NO-releasing derivative of acetylsalicilic acid, has been shown to retain the analgesic, anti-inflammatory and antithrombotic activity of aspirin, but with less gastrointestinal toxicity. In addition, preliminary data suggested that NCX4016 may restore insulin sensitivity in eNOS deficient mice.
This study was aimed to evaluate the activity of NCX4016, compared to aspirin, on albuminuria, insulin sensitivity and cardiac and renal hemodynamic in patients with type 2 diabetes mellitus. The patients after one month of placebo treatment, entered two 1-month treatments periods, with equivalent doses (800 mg of NCX4016, 325 mg of aspirin) of NCX4016 or aspirin.

开始日期2003-03-01

申办/合作机构-

100 项与 Nitroaspirin 相关的临床结果

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100 项与 Nitroaspirin 相关的转化医学

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100 项与 Nitroaspirin 相关的专利（医药）

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223

项与 Nitroaspirin 相关的文献（医药）

2024-08-14·European Heart Journal - Cardiovascular Pharmacotherapy

Aspirin-free strategy for percutaneous coronary intervention in acute coronary syndrome based on the subtypes of acute coronary syndrome and high bleeding risk: the STOPDAPT-3 trial

Article

作者: Tamura, Toshihiro ; Tsujita, Kenichi ; Obayashi, Yuki ; Ogata, Nobuhiko ; Hata, Yoshiki ; Abe, Koji ; Tanigawa, Takashi ; Ando, Kenji ; Yamamoto, Ko ; Akashi, Yoshihiro J ; Kusuyama, Takanori ; Kawahatsu, Kando ; Suwa, Satoru ; Takenaka, Hiroyuki ; Morimoto, Takeshi ; Nakano, Masatsugu ; Tanaka, Hiroyuki ; Nakagami, Takuo ; Sugimoto, Atsuhiko ; Tanabe, Kengo ; Miura, Shin-Ichiro ; Tokuyama, Hideo ; Wakatsuki, Tetsuzo ; Makiguchi, Noriko ; Fujita, Takanari ; Nishida, Koji ; Nakazawa, Gaku ; Wakeyama, Takatoshi ; Onishi, Yuko ; Takaya, Tomofumi ; Tomita, Hirofumi ; Kaitani, Kazuaki ; Kumagai, Koji ; Akao, Masaharu ; Yamaguchi, Junichi ; Nishida, Yasunori ; Hayashi, Fujio ; Serikawa, Takeshi ; Watanabe, Hirotoshi ; Ishihara, Shozo ; Matsuoka, Shunzo ; Kozuma, Ken ; Morishima, Itsuro ; Wakabayashi, Kohei ; Hibi, Kiyoshi ; Nozaki, Yoichi ; Uehara, Hiroki ; Okayama, Hideki ; Kawai, Kazuya ; Yamada, Minoru ; Morino, Yoshihiro ; Kimura, Takeshi ; Ikari, Yuji ; Nishikawa, Ryusuke ; Tsubakimoto, Yoshinori ; Doijiri, Tatsuki ; Abe, Shichiro ; Kinoshita, Makoto ; Suzuki, Hiroshi ; Shiode, Nobuo ; Kobayashi, Yoshio ; Kato, Ryuichi ; Noda, Toshiyuki ; Inoko, Moriaki ; Doi, Masayuki ; Yoshida, Ruka ; Isawa, Tsuyoshi ; Natsuaki, Masahiro ; Nishikura, Tenjin ; Kaneko, Takeo ; Higuchi, Motoaki ; Ono, Koh ; Kurita, Tairo ; Nakano, Yukiko ; Yokomatsu, Takafumi ; Kadota, Kazushige ; Yumoto, Kazuhiko ; Tabuchi, Isao ; Ishikawa, Tetsuya ; Sakamoto, Hiroki ; Nanasato, Mamoru ; Kirigaya, Hidekuni

AbstractBackground and aimsHigh bleeding risk (HBR) and acute coronary syndrome (ACS) subtypes are critical in determining bleeding and cardiovascular event risk after percutaneous coronary intervention (PCI).Methods and resultsIn 4476 ACS patients enrolled in the STOPDAPT-3, where the no-aspirin and dual antiplatelet therapy (DAPT) strategies after PCI were randomly compared, the pre-specified subgroup analyses were conducted based on HBR/non-HBR and ST-segment elevation myocardial infarction (STEMI)/non-ST-segment elevation ACS (NSTE-ACS). The co-primary bleeding endpoint was Bleeding Academic Research Consortium (BARC) type 3 or 5, and the co-primary cardiovascular endpoint was a composite of cardiovascular death, myocardial infarction, definite stent thrombosis, or ischaemic stroke at 1 month. Irrespective of the subgroups, the effect of no-aspirin compared with DAPT was not significant for the bleeding endpoint (HBR [N = 1803]: 7.27 and 7.91%, hazard ratio (HR) 0.91, 95% confidence interval (CI) 0.65–1.28; non-HBR [N = 2673]: 3.40 and 3.65%, HR 0.93, 95% CI 0.62–1.39; Pinteraction = 0.94; STEMI [N = 2553]: 6.58 and 6.56%, HR 1.00, 95% CI 0.74–1.35; NSTE-ACS [N = 1923]: 2.94 and 3.64%, HR 0.80, 95% CI 0.49–1.32; Pinteraction = 0.45), and for the cardiovascular endpoint (HBR: 7.87 and 5.75%, HR 1.39, 95% CI 0.97–1.99; non-HBR: 2.56 and 2.67%, HR 0.96, 95% CI 0.60–1.53; Pinteraction = 0.22; STEMI: 6.07 and 5.46%, HR 1.11, 95% CI 0.81–1.54; NSTE-ACS: 3.03 and 1.71%, HR 1.78, 95% CI 0.97–3.27; Pinteraction = 0.18).ConclusionIn patients with ACS undergoing PCI, the no-aspirin strategy compared with the DAPT strategy failed to reduce major bleeding events irrespective of HBR and ACS subtypes. The numerical excess risk of the no-aspirin strategy relative to the DAPT strategy for cardiovascular events was observed in patients with HBR and in patients with NSTE-ACS.

2024-07-31·The FASEB Journal

RETRACTION: NCX‐4016, a nitric oxide‐releasing aspirin, protects endothelial cells against apoptosis by modulating mitochondrial function

RETRACTION: S. Fiorucci, A. Mencarelli, R. Mannucci, E. Distrutti, A. Morelli, P. del Soldato, S. Moncada, “NCX‐4016, a nitric oxide‐releasing aspirin, protects endothelial cells against apoptosis by modulating mitochondrial function,” The FASEB Journal 16, no. 12 (2002): 1645–1647. https://doi.org/10.1096/fj.02‐0297fje.The above article, published online on 07 August 2002 in Wiley Online Library (wileyonlinelibrary.com), has been retracted by agreement between the journal Editor‐in‐Chief, Dr. Loren E. Wold; the Federation of American Societies for Experimental Biology; and Wiley Periodicals LLC. The retraction has been agreed due to concerns raised by a third party regarding the similarity of blots in Figure 7. The authors did not respond to inquiries by either the society or the publisher. In addition, the authors' institution did not respond to our request to begin an investigation. An investigation by the society and the publisher determined that there is overwhelming evidence that images in Figure 7 were manipulated. Because the images in question were imperative to the conclusions presented in the article, all parties agreed the article must be retracted.

2024-01-01·Discovery Medicine

Inhibition Effects of Acetylsalicylic Acid with Nitric Oxide (NO-ASA) on Neoplastic Changes in the Exocrine Pancreas Acinar Cells of the Azaserine Injected Rats

Article

作者: Yıldız, Hasan ; Doğan, Serhat

BACKGROUNDAtypical acinar cell foci (AACF) seen in pancreatic cancer are fatal and have been studied with some causative agents. However, for the first time, the effect of acetylsalicylic acid with nitric oxide (NO-ASA) on AACF was examined in this study. Although NO-ASA has very successful inhibitory effects against some types of cancer, it has not been investigated whether they can exert their inhibition effects on AACFs.METHODSFor experimental purposes, 21 14-day-old male Wistar albino rats were used. Azaserine (30 mg/kg) was dissolved in 0.9% NaCl solution and injected intraperitoneally (i.p.) into 14 rats, except for the Control group (Cont) rats, for three weeks. Rats that were injected with azaserine once a week for three weeks and those that did not receive treatment were divided into experimental groups. 15 days after the end of the azaserine injection protocol, NO-ASA was applied to azaserine with NO-ASA (Az+NO-ASA) group rats three consecutive times with an interval of 15 days by gavage. At the end of the 5-month period, pancreatic tissue was dissected and weighed. Pancreas preparations prepared from histological sections were examined for AACF burden and analyzed via a video image analyzer. One-way analysis of variance (ANOVA) non-parametric statistical analyses were performed to test whether there was a difference between the averages of the experimental and Control groups.RESULTSAACF burden in both groups injected with azaserine was found to be statistically significant in all categories compared to that of the Control group (p < 0.05). The average Calculated Estimated average AACF volume (mm³) values, the Calculated estimated average AACF diameter (μm), the Estimated average number of AACF per unit volume, AACF rate as a % of Calculated Organ Volume were higher in the AzCont group rats than in the Az+NO-ASA group, when compared, and there was an important level statistical difference between the groups (p < 0.05). It was determined that for all parameters AACFs load in Az+NO-ASA group rats were significantly reduced compared to that of AzCont group rats (p < 0.05).CONCLUSIONSWe observed that, as a result of the NO-ASA application, the experimental AACF focus ratio created by azaserine injection was significantly inhibited. The inhibitory effect of AACFs in Az+NO-ASA group rats may have resulted from the significant and independent chemopreventive and/or chemotherapeutic activity of NO-ASA against exocrine pancreatic AACF foci.

100 项与 Nitroaspirin 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB12445

研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
间歇性跛行	临床2期	意大利	Nicox Research Institute Srl	2003-09-01
外周动脉闭塞性疾病	临床2期	意大利	Nicox Research Institute Srl	2003-09-01
2型糖尿病	临床2期	瑞士	Nicox SA	-
2型糖尿病	临床2期	意大利	Nicox SA	-
疼痛	临床2期	美国	Nicox SA	-

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


ASCO2023	N/A	肝细胞癌	-	Long-term aspirin use	壓蓋構衊糧廠觸願壓鬱(獵積鹽選夢夢選遞醖夢) = 遞鑰憲艱艱餘醖鏇獵廠鬱夢鑰夢獵膚醖獵鏇餘 (鹹遞夢鹹齋鬱鏇鹹鑰蓋 ) 更多	积极	2023-05-31
				No long-term aspirin use	壓蓋構衊糧廠觸願壓鬱(獵積鹽選夢夢選遞醖夢) = 遞蓋遞繭襯築觸遞憲鏇鬱夢鑰夢獵膚醖獵鏇餘 (鹹遞夢鹹齋鬱鏇鹹鑰蓋 ) 更多
WCLC2019	N/A	ALK阳性非小细胞肺癌 \| EGFR突变的非小细胞肺癌 \| ROS1阳性非小细胞肺癌一线	74	Vitamin D supplementation	(襯壓憲鑰鏇夢廠鹹膚觸) = 襯糧範壓齋鬱顧構範餘獵構餘窪衊繭衊築齋餘 (鏇餘壓鑰夢鹹壓觸鹽窪 ) 更多	-	2019-09-08
				No Vitamin D supplementation	(襯壓憲鑰鏇夢廠鹹膚觸) = 糧糧餘廠襯鬱糧蓋衊願獵構餘窪衊繭衊築齋餘 (鏇餘壓鑰夢鹹壓觸鹽窪 ) 更多
ASCO_GU2017	N/A	辅助	1,481	Aspirin intake	衊獵襯構獵廠鏇淵鏇衊(範襯簾鏇蓋顧艱觸鑰網) = 壓遞選網糧夢壓觸糧齋築選壓鏇餘範壓製鹽獵 (獵壓醖艱顧壓壓鏇鹹構 )	积极	2017-03-29
				No aspirin intake	糧襯齋淵鬱範簾窪願獵(鏇醖憲簾醖願蓋醖窪觸) = 鹹蓋蓋壓憲艱憲廠鬱繭願齋齋襯醖積願鬱窪網 (壓餘淵積糧網衊鏇範遞 ) 更多
AHNS2016	N/A	-	570	Continued ASA therapy	壓窪範簾構網窪鹽淵憲(鹽網積窪蓋夢網網鏇鏇) = A total of 6 patients developed hematoma between both groups, and 1 (16.7%) required operative exploration 獵願積醖獵廠餘築積夢 (餘鹹觸艱廠窪鏇廠糧糧 )	-	2016-07-16
				Naïve (no ASA therapy)
Prostate, Lung, Colorectal, and Ovarian (PLCO) Cancer Screening Trial (AACR2013)	N/A	前列腺癌	3,857	Daily or more than daily aspirin use	鑰遞糧願膚窪製遞選醖(遞襯網窪築遞願糧顧糧): HR = 0.77 (95% CI, 0.48 ~ 1.25)	-	2013-04-15
				No aspirin use
1113 (AUA2011)	N/A	颅内高压	-	Daily administration of sildenafil 0.13 mg	範醖繭觸醖齋獵鏇膚壓(網壓獵顧淵窪簾餘淵製) = 窪觸鬱鬱鏇顧艱襯網廠製築淵積構夢獵廠憲醖 (醖築觸構繭構鑰夢憲網 )	-	2011-04-01
				Weekly administration of sildenafil 0.5 mg	範醖繭觸醖齋獵鏇膚壓(網壓獵顧淵窪簾餘淵製) = 網壓衊夢範壓獵夢繭壓製築淵積構夢獵廠憲醖 (醖築觸構繭構鑰夢憲網 )