地磷莫司(Ridaforolimus) - 药物靶点：mTORC1 x mTORC2_专利_临床

概要

基本信息

药物类型

小分子化药

别名

BioNIR、Deforolimus、EluNIR

+ [8]

靶点

mTORC1 x mTORC2

作用机制

mTORC1抑制剂(哺乳动物雷帕霉素靶蛋白(mTORC1)复合体抑制剂)、mTORC2抑制剂(mTOR复合物-2抑制剂)

治疗领域

肿瘤皮肤和肌肉骨骼疾病其他疾病+ [5]

在研适应症-

非在研适应症

晚期癌症晚期子宫内膜癌晚期恶性实体瘤+ [21]

原研机构

ARIAD Pharmaceuticals, Inc.

在研机构-

非在研机构

Merck Sharp & Dohme Corp.Merck GmbH

ARIAD Pharmaceuticals, Inc.

+ [2]

最高研发阶段终止临床3期

首次获批日期-

最高研发阶段(中国)终止

特殊审评孤儿药 (美国)

结构

分子式C53H84NO14P

InChIKeyBUROJSBIWGDYCN-UHFFFAOYSA-N

CAS号572924-54-0

关联

45

项与地磷莫司相关的临床试验

NCT04761939 / CompletedN/A

BIONICS Small Vessels Trial EluNIR Ridaforolimus Eluting Coronary Stent System (EluNIR) In Coronary Stenosis Trial

Device:
EluNIR Ridaforolimus Eluting Coronary Stent System - (hereafter referred to as EluNIR) 2.25 mm diameter (8 mm, 12 mm, 15 mm, 17 mm, 20 mm, 24 mm, 28 mm and 33 mm length)
Objectives:
To further assess the safety and efficacy of the small diameter (2.25 mm) Ridaforolimus Eluting Stent - EluNIR.
Subject Population:
Subjects who underwent PCI for angina (stable or unstable), silent ischemia (in absence of symptoms a visually estimated target lesion diameter stenosis of ≥70%, a positive non-invasive stress test, or FFR ≤0.80 must be present), NSTEMI, and recent STEMI (>24 hours from initial presentation and stable) with attempted implantation of a 2.25 mm diameter EluNIR stent.
Trial Design and Methods:
This is a prospective, multi-center, single-arm, open-label clinical trial. Clinical follow-up for all patients will be performed at 30 days 6 months, and 1 year after the procedure.

开始日期2020-12-31

申办/合作机构

Medinol Ltd.

NCT03702608 / CompletedN/A

Prospective, Multi-center, Single-arm, Open-label Clinical Trial, to Further Assess the Safety and Efficacy of Long (38 mm) Ridaforolimus Eluting Stent - EluNIR

This is a prospective, multi-center, single-arm, open-label clinical trial. Clinical follow-up will be performed at 30 days. Follow-up by phone will be performed at 6 months, and 1 year after the procedure. Study Objective is to further assess the safety and efficacy of long (38 mm) Ridaforolimus Eluting Stent - EluNIR.

开始日期2018-11-14

申办/合作机构

Medinol Ltd.

NCT01605396 / Completed临床2期

A Phase II Randomized Trial of the Combination of Ridaforolimus and Exemestane, Compared to Ridaforolimus, Dalotuzumab and Exemestane in High Proliferation, Estrogen Receptor Positive Breast Cancer Patients

The purpose of the study is to evaluate the efficacy of the triplet of ridaforolimus, dalotuzumab and exemestane compared to the combination of ridaforolimus and exemestane in post-menopausal participants with breast cancer. The primary hypothesis of the study is that the triplet of ridaforolimus, dalotuzumab and exemestane will improve progression free survival (PFS) compared to ridaforolimus and exemestane.

开始日期2012-07-04

申办/合作机构

Merck Sharp & Dohme LLC

100 项与地磷莫司相关的临床结果

登录后查看更多信息

100 项与地磷莫司相关的转化医学

登录后查看更多信息

100 项与地磷莫司相关的专利（医药）

登录后查看更多信息

160

项与地磷莫司相关的文献（医药）

2024-04-01·Current Molecular Medicine

The mTOR Signaling Pathway and mTOR Inhibitors in Cancer: Next-generation Inhibitors and Approaches

Article

作者: Akgul, Busra ; Kelleci, Kübra ; Korkut, Şenay Vural ; Ihlamur, Murat ; Abamor, Emrah Şefik ; Zengin, Yağmur

Abstract:mTOR is a serine/threonine kinase that plays various roles in cell growth, proliferation, and metabolism. mTOR signaling in cancer becomes irregular. Therefore, drugs targeting mTOR have been developed. Although mTOR inhibitors rapamycin and rapamycin rapalogs (everolimus, rapamycin, temsirolimus, deforolimus, etc.) and new generation mTOR inhibitors (Rapalink, Dual PI3K/mTOR inhibitors, etc.) are used in cancer treatments, mTOR resistance mechanisms may inhibit the efficacy of these drugs. Therefore, new inhibition approaches are developed. Although these new inhibition approaches have not been widely investigated in cancer treatment, the use of nanoparticles has been evaluated as a new treatment option in a few types of cancer.:This review outlines the functions of mTOR in the cancer process, its resistance mechanisms, and the efficiency of mTOR inhibitors in cancer treatment. Furthermore, it discusses the next-generation mTOR inhibitors and inhibition strategies created using nanoparticles.:Since mTOR resistance mechanisms prevent the effects of mTOR inhibitors used in cancer treatments, new inhibition strategies should be developed. Inhibition approaches are created using nanoparticles, and one of them offers a promising treatment option with evidence supporting its effectiveness.

2024-01-16·Journal of the American Heart Association

Percutaneous Coronary Interventions Using a Ridaforolimus‐Eluting Stent in Patients at High Bleeding Risk

Article

作者: Jadhav, Sachin ; Segev, Amit ; Konigstein, Maayan ; Kerner, Arthur ; Kornowski, Ran ; Halabi, Majdi ; Vaknin-Assa, Hana ; Baumbach, Andreas ; Roguin, Ariel ; Blaxill, Jonathan ; Hoole, Stephen ; Danenberg, Haim ; Karamasis, Grigoris V ; Ben-Yehuda, Ori ; Lev, Eli ; Jonas, Michael ; Johnson, Thomas W ; Assali, Abid ; Issever, Melek Ozgu ; Witberg, Guy ; Anderson, Richard

BackgroundPatients treated with percutaneous coronary intervention are often considered to be at a high bleeding risk (HBR). Drug‐eluting stents have been shown to be superior to bare‐metal stents in patients with HBR, even when patients were given abbreviated periods of dual antiplatelet therapy (DAPT). Short DAPT has not been evaluated with the EluNIR ridaforolimus‐eluting stent. The aim of this study was to evaluate the safety and efficacy of a shortened period of DAPT following implantation of the ridaforolimus‐eluting stent in patients with HBR.Methods and Results This was a prospective, multicenter, binational, single‐arm, open‐label trial. Patients were defined as HBR according to the LEADERS‐FREE (Prospective Randomized Comparison of the BioFreedom Biolimus A9 Drug‐Coated Stent versus the Gazelle Bare‐Metal Stent in Patients at High Bleeding Risk) trial criteria. After percutaneous coronary intervention, DAPT was given for 1 month to patients presenting with stable angina. In patients presenting with an acute coronary syndrome, DAPT was given for 1 to 3 months, at the investigator's discretion. The primary end point was a composite of cardiac death, myocardial infarction, or stent thrombosis up to 1 year (Academic Research Consortium definite and probable). Three hundred fifteen patients undergoing percutaneous coronary intervention were enrolled, and 56.4% presented with acute coronary syndrome; 33.7% were receiving oral anticoagulation. At 1 year, the primary end point occurred in 15 patients (4.9%), meeting the prespecified performance goal of 14.1% ( P <0.0001). Stent thrombosis (Academic Research Consortium definite and probable) occurred in 2 patients (0.6%). Bleeding Academic Research Consortium type 3 and 5 bleeding occurred in 6 patients (1.9%). ConclusionsWe observed favorable results in patients with HBR who underwent percutaneous coronary intervention with a ridaforolimus‐eluting stent and received shortened DAPT, including a low rate of ischemic events and low rate of stent thrombosis.Registration URL: https://www.clinicaltrials.gov ; Unique identifier: NCT03877848.

2024-01-01·Catheterization and Cardiovascular Interventions

Percutaneous coronary intervention with ridaforolimus eluting‐stents in small vessel coronary artery disease

Article

作者: Rubinshtein, Ronen ; Konigstein, Maayan ; Pereg, David ; Cafri, Carlos ; Kerner, Arthur ; Gabarin, Mustafa ; Arow, Ziad ; Koifman, Edward ; Jonas, Michael ; Segev, Amit ; Witberg, Guy ; Vaknin-Assa, Hana ; Issever, Melek Ozgu ; Assali, Abid ; Roguin, Ariel

AbstractIntroductionThe ridaforolimus‐eluting stent (RES) system uses a novel cobalt alloy‐based coronary stent with a durable elastomeric polymer eluting ridaforolimus.Aim of studyTo assess the safety and efficacy of small diameter (2.25 mm) RES (EluNIR) in small coronary artery disease.MethodsA prospective, multicenter, single‐arm, open‐label clinical trial. Clinical follow‐up was performed at 30 days, 6 months, and 1 year after the procedure. Target lesions were located in native coronary arteries or bypass graft conduits, with visually estimated diameter of ≥2.25 mm to ≤2.5 mm. The primary endpoint was combined device success, defined as final in‐stent residual diameter stenosis <30%, without 30‐day major adverse cardiovascular events (MACE).ResultsA total of 81 patients were enrolled in the study. Twenty‐three patients (28%) had acute coronary syndrome (ACS) at presentation and 37 (46%) had prior myocardial infarction (MI). Most of the target lesions were located in the circumflex coronary artery (44%) and were classified as B2/C grade according to the American Heart Association/American College of Cardiology classification. The final mean minimal lumen diameter, mean reference vessel diameter, and mean residual percent diameter stenosis were 2.0 ± 0.2 mm, 2.3 ± 0.1 mm, and 14 + 6.6%, respectively. The primary endpoint of device success without 30‐day MACE was achieved in 98.8% of the patients. Target lesion failure (TLF) at 6 months was 1.2%. Thirty‐day and 1‐year MACE rates were 1.2% and 2.5%, respectively.ConclusionThe EluNIR 2.25 mm stent shows excellent results in small coronary artery disease and adds another tool in the treatment of this complex lesion type.

6

项与地磷莫司相关的新闻（医药）

2023-10-25

·NS Medical Devices

Medinol secures FDA approval for EluNIR-PERL coronary stent system

EluNIR-PERL, the latest addition to Medinol’s EluNIR family of DES products, has four radiopaque markers, two at each end of the stent, and a radiopaque catheter tip made of hybrid polymer-metal, to facilitate superior visualisation during PCI procedures EluNIR-PERL drug-eluting coronary stent closeup. (Credit: PRNewswire/ CoSo Health) Israeli medical device maker Medinol has received the US Food and Drug Administration (FDA) approval for its EluNIR-PERL drug-eluting stent (DES) system to treat coronary artery disease. EluNIR-PERL is the latest coronary stent in its EluNIR family of DES products and builds on the company’s existing EluNIR DES system. The system comes with four radiopaque markers, two at each end of the stent, and a radiopaque catheter tip made of hybrid polymer-metal. Its unique features facilitate superior visualisation during PCI procedures including navigation through complex anatomies and placement of the stent, said the medical device maker. Medinol CEO Yoram Richter said: “We are pleased to bring technologies to the US that focus both on the benefit to patients as well as unique and meaningful advantages to surgeons, allowing for precise stent placement, shorter procedure times and reduced radiation exposure.” EluNIR-PERL is the company’s seventh-generation stent and features a unique stent design that leverages its unique CoCr framework. The CoCr framework comprises struts with varying widths and integrates radiopaque markers into the structure of the stent system. In addition, the stent also features a specialised radiopaque-enhanced metal spring tip intended for navigating through complex anatomies. The advanced design features would enable physicians with accurate positional information and precise stent placement during PCI procedures, said the medical device company. Medinol intends to commercialise the EluNIR-PERL in the US, exclusively through CoSo Health, a healthcare supply and logistics company that distributes and sells medical devices. Building on its sales rep-light model, advanced cloud-based logistics platform and customised delivery model, CoSo Health is said to reduce waste from the supply chain. CoSo Health CEO Jae Lee said: “We are proud to distribute one of the world’s best drug-eluting stents via our intuitive and easy-to-use SaaS+ platform, which reduces layers in the supply chain.”

放射疗法

2023-10-24

·PRNewswire

Medinol Receives FDA Approval for Next Generation EluNIR-PERL™ Drug-Eluting Coronary Stent System

CoSo Health to exclusively distribute Medinol's most advanced coronary DES in the U.S. DENVER and TEL AVIV, Israel, Oct. 24, 2023 /PRNewswire/ -- Medinol today announced United States Food and Drug Administration (FDA) approval for the EluNIR-PERL™ drug-eluting stent (DES) for the treatment of coronary artery disease. Continue Reading EluNIR-PERL™ Drug-Eluting Coronary Stent Closeup EluNIR-PERL builds upon the proven performance and clinical data of the EluNIR™ DES system. As the latest evolution in the EluNIR DES family, EluNIR-PERL features four radiopaque markers, two at each end of the stent, and a hybrid polymer-metal radiopaque catheter tip. These unique features allow outstanding visualization during PCI procedures whether navigating through complex anatomies or precise placement of the stent. "We are pleased to bring technologies to the U.S. that focus both on benefit to patients as well as unique and meaningful advantages to surgeons, allowing for precise stent placement, shorter procedure times and reduced radiation exposure," said Yoram Richter, CEO of Medinol. "We are proud to distribute one of the world's best drug-eluting stents via our intuitive and easy-to-use SaaS+ platform, which reduces layers in the supply chain," said Jae Lee, CEO of CoSo Health. EluNIR-PERL™ is exclusively available in the United States through CoSo Health, an innovative healthcare supply and logistics company changing the way medical devices are distributed and sold. About CoSo Health CoSo Health is redefining the healthcare supply chain with an innovative SaaS+ platform that more efficiently sources, warehouses, and distributes medical supplies and devices, bringing best-in-class products and devices to the market at great value. Visit or contact CoSo Health Chief Executive Officer Jae Lee at [email protected]. About Medinol At Medinol, we are aggressively changing paradigms in how disease states are diagnosed and treated. Whether designing cutting edge devices for stenting multiple areas of the body, dramatically reducing complications in Structural Heart procedures or providing real time insights into the physiological metrics of the human body through implantable sensors, we boldly reassess current technology and procedures and look years into the future to pioneer new devices to broaden the reach of physicians both physically and geographically. For more information, see . SOURCE CoSo Health

放射疗法

2023-05-31

·NS Medical Devices

Medinol Partners with CoSo Health to Launch the EluNIR Drug-Eluting Stent in the U.S.

CoSo Health to work with U.S. Endovascular and others to reach the U.S. market The announcement comes at a time when hospitals, payers and outpatient facilities are seeking ways to reduce surgical costs. (Credit: Medinol) CoSo Health today announced signing a U.S. distribution agreement with Medinol for EluNIR, a new generation, thin-strut drug-eluting stent (DES). Medinol is a global leader in the development of innovative implantable medical devices. U.S. Endovascular sells peripheral and coronary devices nationwide. CoSo Health is changing the way medical devices are distributed and sold. Through its sales rep-light model, innovative cloud-based logistics platform and customized delivery model, CoSo Health cuts waste from the supply chain. The announcement comes at a time when hospitals, payers and outpatient facilities are seeking ways to reduce surgical costs. “We are extremely excited to partner with CoSo Health to expand our reach within the U.S.,” said Jeff Roach, Chief Commercial Officer at Medinol. “We are both innovators – Medinol with world-class implantable device technology and CoSo Health with logistics and distribution. Together, we are disrupting the distribution of drug-eluting stents through a direct-to-end user model that brings tremendous economic value to purchasers.” The EluNIR DES offers excellent clinical outcomes and an outstanding safety profile. Its best-in-class metal-to-artery ratio and ultra-durable polymer coating, along with a unique delivery system, combine to provide a new standard in treatment capabilities. Successive generations of EluNIR are coming to the global market soon. Source: Company Press Release

100 项与地磷莫司相关的药物交易

登录后查看更多信息

外链

KEGG	Wiki	ATC	Drug Bank
D08900	地磷莫司	L01XE19	DB06233

研发状态

10 条进展最快的记录,

登录

后查看更多信息

适应症	最高研发状态	国家/地区	公司	日期
转移性骨肉瘤	临床3期	-	Merck Sharp & Dohme Corp.	2007-10-01
转移性软组织肉瘤	临床3期	-	Merck Sharp & Dohme Corp.	2007-10-01
晚期肉瘤	临床3期	-	Merck Sharp & Dohme Corp.	2004-10-01
平滑肌肉瘤	临床3期	-	Merck Sharp & Dohme Corp.	2004-10-01
淋巴瘤	临床3期	美国	Merck Sharp & Dohme Corp.	2004-06-01
前列腺癌	临床3期	美国	ARIAD Pharmaceuticals, Inc.	-
白血病	临床1期	美国	Merck Sharp & Dohme Corp.	2004-06-01
骨髓增生异常综合征	临床1期	美国	Merck Sharp & Dohme Corp.	2004-06-01
原发性骨髓纤维化	临床1期	美国	Merck Sharp & Dohme Corp.	2004-06-01
前列腺癌	临床1期	美国	ARIAD Pharmaceuticals, Inc.	-

登录后查看更多信息

临床结果

适应症

分期

评价

查看全部结果

研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT01169532 (ASCO2014)	临床1期	-	15	Ridaforolimus 20mg QD + Vorinostat 100mg BID	(鑰膚築鹹鹹襯壓鬱艱鹹) = 餘鏇淵廠願齋齋鏇糧窪觸鑰鏇簾鏇繭醖齋選餘 (觸網糧遞淵壓範憲獵鹽 )	-	2014-05-20
NCT01169532 (ASCO2014)	临床1期	-	15	Ridaforolimus 20mg QD + Vorinostat 200mg BID	(鑰膚築鹹鹹襯壓鬱艱鹹) = 鹽繭繭選鑰鑰觸鹽鹹顧觸鑰鏇簾鏇繭醖齋選餘 (觸網糧遞淵壓範憲獵鹽 )	-	2014-05-20
NCT00770185 (Pubmed \| Obstet Gynecol Surv)	临床2期	转移性子宫内膜恶性肿瘤	34	Oral ridaforolimus 40mg	膚鬱夢鑰糧簾鑰繭蓋膚(餘鹽鏇鬱艱蓋襯膚餘鹽) = 積範衊憲觸憲糧壓壓獵鏇鹽觸餘觸壓艱獵夢衊 (網壓壓膚鬱醖襯鏇網襯 ) 更多	积极	2014-11-01
NCT01295632 (Pubmed \| Eur J Cancer Care (Engl)) 人工标引	临床1期	晚期恶性实体瘤	28	ridaforolimus+MK-0752	(艱鹹繭觸壓遞鑰醖選衊) = 蓋顧憲糧鑰餘顧觸構艱廠淵願鑰鹹齋遞網範鏇 (範選夢網糧夢夢糧繭觸 ) 更多	积极	2015-09-01
NCT01256268 (Pubmed \| BMC Cancer) 人工标引	临床1期	实体瘤	24	paclitaxel+carboplatin+ridaforolimus	(糧蓋醖齋網築選艱蓋願) = 廠醖網繭積構簾觸廠壓衊鏇觸遞範齋鹽憲廠積 (窪醖簾鏇膚齋鹽遞鏇膚 ) 更多	积极	2017-06-08
NCT00736970 (Pubmed \| Clin Breast Cancer)	临床2期	乳腺癌 \| HER2阳性转移性乳腺癌	34	Ridaforolimus	(鏇淵選構膚憲齋顧鏇膚) = 襯願夢糧構壓衊蓋簾膚鏇窪廠壓網膚蓋製蓋鬱 (範繭壓簾窪醖窪壓製窪 ) 更多	积极	2015-02-01
NCT01256268 (ASCO2016)	临床1期	实体瘤	24	Ridaforolimus + Paclitaxel + Carboplatin	(糧鏇衊淵艱蓋壓窪繭構) = 廠願顧築範積選願積鹹窪積糧糧艱餘夢獵願網 (餘願窪膚鏇夢壓鑰淵築 ) 更多	积极	2016-05-20
NCT01605396 (Pubmed \| Breast Cancer Res) 人工标引	临床2期	晚期乳腺癌	80	dalotuzumab+ridaforolimus+exemestane	(醖築蓋鹽糧窪醖範餘夢) = 範範夢願網範衊鏇艱觸蓋構夢餘顧襯願憲顧鑰 (糧繭網積醖糧積憲繭衊 ) 更多	不佳	2017-10-01
NCT01605396 (Pubmed \| Breast Cancer Res) 人工标引	临床2期	晚期乳腺癌	80	dalotuzumab+ridaforolimus	(醖築蓋鹽糧窪醖範餘夢) = 獵壓衊淵艱夢夢窪襯鬱蓋構夢餘顧襯願憲顧鑰 (糧繭網積醖糧積憲繭衊 ) 更多	不佳	2017-10-01
NCT01295632 (Pubmed \| Clin Cancer Res) 人工标引	临床1期	肿瘤	35	Ridaforolimus+MK 2206	(積願網憲窪願淵艱壓壓) = 鏇齋壓觸膚窪淵齋廠鏇簾憲構鬱鏇範製鑰繭積 (觸衊鏇襯鬱膚築鏇憲餘 ) 更多	积极	2015-12-01
NCT00739830 (Pubmed \| J Urol) 人工标引	临床2期	晚期子宫内膜癌	130	Ridaforolimus	(襯遞醖範範獵壓鬱鹹膚) = 築鏇壓築膚窪選繭網衊憲壓膚衊獵膚鹹鏇夢餘 (觸糧夢獵醖簾夢獵選壓, 2.7 ~ 7.3) 更多	积极	2015-11-01
NCT00739830 (Pubmed \| J Urol) 人工标引	临床2期	晚期子宫内膜癌	130	Chemotherapy	(襯遞醖範範獵壓鬱鹹膚) = 遞鑰壓獵顧顧遞壓鹽醖憲壓膚衊獵膚鹹鏇夢餘 (觸糧夢獵醖簾夢獵選壓, 1.9 ~ 2.3) 更多	积极	2015-11-01
NCT01234857 (Pubmed \| Breast Cancer Res)	临床2期	ER阳性乳腺癌	115	Ridaforolimus 30 mg + Dalotuzumab 10 mg/kg	(窪鏇夢齋選糧鬱廠鹽鏇) = 窪選壓觸糧製憲鏇鬱觸蓋淵製壓觸夢餘艱蓋顧 (範鹽簾網構餘製構選醖 )	不佳	2017-06-01
NCT01234857 (Pubmed \| Breast Cancer Res)	临床2期	ER阳性乳腺癌	115	Exemestane 25 mg	(窪鏇夢齋選糧鬱廠鹽鏇) = 齋製膚繭鑰糧範顧構構蓋淵製壓觸夢餘艱蓋顧 (範鹽簾網構餘製構選醖 )	不佳	2017-06-01