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

非降解型分子胶

别名

BioNIR、Deforolimus、EluNIR

+ [8]

靶点

mTORC1 x mTORC2

作用方式

抑制剂

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+ [7]

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+ [41]

原研机构

ARIAD Pharmaceuticals, Inc.

在研机构-

非在研机构

ARIAD Pharmaceuticals, Inc.

Merck Sharp & Dohme Corp.Merck Sharp & Dohme LLC

+ [1]

权益机构

Merck & Co., Inc.

ARIAD Pharmaceuticals, Inc.

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)

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结构/序列

分子式C53H84NO14P

InChIKeyBUROJSBIWGDYCN-UHFFFAOYSA-N

CAS号572924-54-0

关联

42

项与地磷莫司相关的临床试验

KCT0009812

/ Not yet recruitingN/AIIT

Comparison of Safety and Efficacy of Abbreviated Dual Antiplatelet Therapy in Patients with Acute Myocardial Infarction undergoing Ridaforolimus Eluting Stent EluNIR™ Implantation: A Prospective, Multicenter, Randomized Controlled Study

开始日期2024-11-01

申办/合作机构-

NCT01995500

/ Completed临床2期

BioNIR Ridaforolimus Eluting Coronary Stent System (BioNIR) EUropean Angiography Study

The NIREUS study aims to demonstrate angiographic non-inferiority for the BioNIR Ridaforolimus Eluting Coronary Stent System (hereafter referred to as BioNIR) in comparison to the Resolute zotarolimus-eluting stent (hereafter referred to as Resolute).
The trial hypothesis is that the BioNIR is non-inferior to the Resolute for the primary endpoint of angiographic in-stent late loss at 6 months.

开始日期2014-03-19

申办/合作机构

Medinol Ltd.

NCT01995487

/ CompletedN/A

BioNIR Ridaforolimus Eluting Coronary Stent System (BioNIR) In Coronary Stenosis Trial

The BioNIR study aims to show that the BioNIR ridaforolimus eluting stent is non-inferior to the Resolute zotarolimus-eluting stent for the primary clinical endpoint of target lesion failure (TLF) at 12 months; that it is non-inferior to the Resolute for the secondary endpoint of angiographic in-stent late loss at 13 months; and that it is more cost-effective.

开始日期2014-01-01

申办/合作机构

Medinol Ltd.

100 项与地磷莫司相关的临床结果

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100 项与地磷莫司相关的转化医学

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100 项与地磷莫司相关的专利（医药）

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168

项与地磷莫司相关的文献（医药）

2025-11-01·DRUG DEVELOPMENT RESEARCH

Targeting mTOR Kinase for Cancer Treatment: A Comprehensive Review With Clinical Insights

Review

作者: Hossain, Md. Takdir ; Hossain, Md. Arafat

ABSTRACT:

Cancer remains a significant global health challenge, with increasing incidence and mortality rates worldwide. The mechanistic target of rapamycin (mTOR) pathway, a central regulator of cell growth, proliferation, metabolism, and survival, has emerged as a promising therapeutic target in cancer. Dysregulation of mTOR signaling is implicated in various cancers, including breast, colon, lung, renal cell carcinoma, and multiple myeloma, making it an attractive target for inhibition. This review provides a comprehensive analysis of mTOR‐targeted therapies, focusing on the clinical outcomes, efficacy, safety, and adverse effects of mTOR inhibitors. We explore the mechanisms of mTOR regulation, the impact of mTOR mutations on drug sensitivity, and the development of resistance to mTOR inhibitors. The review also highlights the potential of combination therapies and next‐generation inhibitors to overcome resistance and improve therapeutic outcomes. Key mTOR inhibitors, including rapalogs (e.g., sirolimus, everolimus) and ATP‐competitive inhibitors (e.g., MLN0128, PP242), are discussed in detail, along with their clinical applications and limitations. Additionally, we summarize the findings from major clinical trials, including FDA‐approved mTOR inhibitors like everolimus and temsirolimus, and non‐FDA‐approved inhibitors such as sapanisertib and ridaforolimus. The review underscores the importance of understanding mTOR signaling and its role in cancer progression, offering insights into the future of mTOR‐targeted therapies in oncology.

2025-09-01·Therapeutic Advances in Medical Oncology

Maintenance therapy—a potential strategy to prolong the survival of advanced soft tissue sarcoma patients

Review

作者: Li, Zola Chia-Chen ; Lee, Yeh Chen ; Chen, Tom Wei-Wu ; Bhargava, Prabhat ; Lee, Ming-Jing

Anthracycline-based chemotherapy remains the cornerstone of first-line systemic treatment for most subtypes of advanced soft tissue sarcoma (STS). However, cumulative cardiotoxicity and a decline in quality of life limit the treatment duration of free-form anthracycline, restricting its long-term benefits. Maintenance therapy—defined as the continuation of a less toxic systemic treatment following initial disease control—includes two main strategies: continuation maintenance and switch maintenance. Continuation maintenance involves the extended use of the same agent or one with a similar mechanism of action to preserve the efficacy of the prior treatment while minimizing the toxicities. By contrast, switch maintenance uses a different, potentially less toxic agent to extend disease control after prior treatment. Both approaches are established in other solid tumors and have been explored in STS. The LMS-04 trial demonstrated improved outcomes with doxorubicin plus trabectedin induction followed by trabectedin maintenance in leiomyosarcoma patients. However, this strategy is limited to leiomyosarcoma patients who received first-line doxorubicin plus trabectedin and is associated with high-grade toxicity (grade 3/4 adverse events in 97% of patients). Switch maintenance strategies, such as ridaforolimus and regorafenib, have limitations in efficacy and tolerability, preventing their widespread adoption. Pegylated liposomal doxorubicin (PLD), a liposome-encapsulated formulation of doxorubicin, offers a potential continuation maintenance option. With a similar mechanism of action to free-form anthracycline but reduced cumulative cardiac toxicity, PLD may be both effective and better tolerated in STS patients who have derived benefit from anthracycline-based chemotherapy. A clinical trial investigating continuation maintenance PLD in this patient population is warranted.

2024-11-19·Journal of the American Heart Association

Comparison of Ridaforolimus‐Eluting and Zotarolimus‐Eluting Coronary Stents: 5‐Year Outcomes From the BIONICS and NIREUS Trials

Article

作者: Kandzari, David E. ; Stone, Gregg W. ; Love, Michael P. ; Smits, Pieter C. ; Redfors, Bjorn ; Zornitzki, Lior ; Konigstein, Maayan ; Ozan, Melek O.

Background:

The BIONICS (BioNIR Ridaforolimus‐Eluting Coronary Stent System in Coronary Stenosis) and the NIREUS (BioNIR Ridaforolimus Eluting Coronary Stent System [BioNIR] European Angiography Study) randomized clinical trials showed noninferiority of the ridaforolimus‐eluting stent (RES) compared with the zotarolimus‐eluting stent (ZES) with respect to 1‐year target‐lesion failure and 6‐month angiographic late lumen loss. We aimed to evaluate clinical outcomes between treatment groups over a 5‐year follow‐up.

Methods and Results:

Patient‐level data from the BIONICS (n=1919) and NIREUS (n=302) were pooled, comparing the outcomes of patients implanted with RES and ZES. The primary end point was the 5‐year rate of target‐lesion failure. A total of 2221 patients (63.2±10.3 years, 79.7% men) undergoing percutaneous coronary intervention with RES (n=1159) or ZES (n=1062) were included. Most clinical and angiographic characteristics were similar between groups. At 5 years, the primary end point of target‐lesion failure was similar between treatment groups (12.2% RES versus 11.3% ZES, P =0.52). Rates of TLR (7.6% RES versus 6.8% ZES, P =0.42) target‐vessel–related myocardial infarction (4.8% RES versus 4.9% ZES, P =0.95) and stent thrombosis (0.9% RES versus 0.9% ZES, P =0.87) also did not differ between groups. Target‐vessel revascularization and cardiac death were higher among the RES group (12.3% versus 9.5% P =0.037, and 3.6% versus 2.2% P =0.042, respectively). However, after correction for baseline characteristics, there was no significant difference in cardiac death between groups.

Conclusions:

In a pooled analysis of 2 randomized trials, 5‐year clinical outcomes were similar between patients undergoing percutaneous coronary intervention with RES and ZES. These results support the long‐term safety and efficacy of RES for the treatment of patients with coronary artery disease.

5

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

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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,

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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
转移性骨肉瘤	临床3期	-	ARIAD Pharmaceuticals, Inc.	2007-10-01
转移性软组织肉瘤	临床3期	-	Merck Sharp & Dohme Corp.	2007-10-01
转移性软组织肉瘤	临床3期	-	ARIAD Pharmaceuticals, Inc.	2007-10-01
ER阳性乳腺癌	临床2期	-	Merck Sharp & Dohme Corp.	2010-09-17
KRAS突变非小细胞肺癌	临床2期	-	Merck Sharp & Dohme Corp.	2009-03-01
非小细胞肺癌	临床2期	-	Merck Sharp & Dohme Corp.	2009-03-01
晚期癌症	临床2期	-	ARIAD Pharmaceuticals, Inc.	2009-02-01
晚期癌症	临床2期	-	Merck Sharp & Dohme Corp.	2009-02-01
晚期子宫内膜癌	临床2期	-	Merck Sharp & Dohme Corp.	2008-08-01

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临床结果

适应症

分期

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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


NCT01169532 (CTgov)	临床1期	晚期恶性实体瘤 \| 淋巴瘤	16	biopsy+vorinostat+ridaforolimus	觸壓築壓艱壓鑰膚簾襯 = 壓鑰膚鬱鹽襯構襯糧積顧顧繭網製鬱獵鑰鬱膚 (窪襯齋鹽壓獵鬱夢襯製, 窪簾淵膚壓糧獵積積鬱 ~ 獵簾糧壓積淵顧鏇鑰淵) 更多	-	2021-02-21
NCT00874731 (MK-8669-037 \| 8669-037, CTgov)	临床1期	转移性肿瘤 \| 晚期癌症	23	placebo (Pt 1, Day 1. Placebo)	鬱醖廠齋顧蓋窪窪積構(鏇積觸鏇選製選壓膚窪) = 齋蓋鏇醖選憲餘積糧糧願襯鏇衊網膚蓋憲膚觸 (壓糧衊範夢醖鹽積範憲, 顧艱積觸衊齋夢艱窪膚 ~ 齋鏇餘獵築獵範簾選廠) 更多	-	2019-05-06
				Ridaforolimus (Pt 1, Day 2. Ridaforolimus 100 mg)	鬱醖廠齋顧蓋窪窪積構(鏇積觸鏇選製選壓膚窪) = 壓簾鹽鏇憲壓襯鏇廠糧願襯鏇衊網膚蓋憲膚觸 (壓糧衊範夢醖鹽積範憲, 製蓋遞襯觸築遞糧夢選 ~ 選窪窪糧繭網膚鹽構窪) 更多
NCT01380184 (CTgov)	临床1期	晚期癌症	15	ridaforolimus	鹽淵齋觸齋壓遞願鬱蓋(淵艱壓網壓糧齋艱淵遞) = 鑰鹽鏇醖壓遞鑰構壓齋願醖觸膚築壓顧廠觸壓 (壓遞鑰淵窪顧繭簾艱餘, 願繭觸淵獵鏇餘壓簾衊 ~ 簾餘衊築衊鹽壓壓鑰蓋) 更多	-	2019-04-19
NCT01431534 (CTgov)	临床1期	实体瘤 \| 晚期恶性实体瘤 \| 恶性实体肿瘤 ... 更多	20	Ridaforolimus (Ridaforolimus 22 mg/m^2)	鹽鹹憲鹽廠構願鑰選獵 = 齋齋鏇積艱觸簾範鹽積鹹廠簾築廠壓窪獵願繭 (積鬱選夢鹽選廠製蓋壓, 遞餘窪構衊繭獵鏇積鹹 ~ 鑰製觸遞積蓋網鹽糧窪) 更多	-	2019-03-01
				Ridaforolimus (Ridaforolimus 28 mg/m^2)	鹽鹹憲鹽廠構願鑰選獵 = 餘鹹遞鹹積鬱廠蓋顧鏇鹹廠簾築廠壓窪獵願繭 (積鬱選夢鹽選廠製蓋壓, 簾壓襯繭範膚鬱築壓簾 ~ 壓鑰衊夢糧餘製廠醖蓋) 更多
NCT01243762 (0646-027, CTgov)	临床1期	晚期癌症	47	MK-0752+dalotuzumab (Dalotuzumab 7.5 mg/kg + MK-0752 1800 mg)	獵醖積淵蓋繭繭艱齋鏇 = 糧願積壓遞鹽餘糧選膚蓋醖築鑰膚齋鑰衊膚淵 (糧淵夢製簾壓網壓繭網, 簾網餘顧觸淵鑰繭淵膚 ~ 餘齋蓋鹹製鬱築鏇鬱積) 更多	-	2017-10-30
				MK-0752+dalotuzumab (Dalotuzumab 10 mg/kg + MK-0752 1800 mg)	獵醖積淵蓋繭繭艱齋鏇 = 艱獵艱餘獵顧遞製糧糧蓋醖築鑰膚齋鑰衊膚淵 (糧淵夢製簾壓網壓繭網, 顧醖積窪淵廠鹹醖積鹹 ~ 簾獵淵鏇憲簾襯範壓襯) 更多
NCT01995487 (BIONICS Trial, Pubmed \| Circulation)	N/A	冠心病	1,919	Ridaforolimus-eluting stents (RESs)	鏇繭艱夢觸繭觸鑰製淵(網範鑰獵顧鏇積鏇網淵) = 窪壓範窪築簾獵窪製鬱蓋夢網艱製構憲艱襯顧 (廠齋遞憲蓋築鹹壓憲夢 ) 更多	-	2017-10-03
				Slow-release zotarolimus-eluting stents	鏇繭艱夢觸繭觸鑰製淵(網範鑰獵顧鏇積鏇網淵) = 簾衊艱繭艱繭襯獵襯艱蓋夢網艱製構憲艱襯顧 (廠齋遞憲蓋築鹹壓憲夢 ) 更多
NCT01605396 (8669-064 \| MK-8669-064, Pubmed \| Breast Cancer Res \| Breast Cancer Res Treat) 人工标引	临床2期	晚期乳腺癌	80	dalotuzumab+ridaforolimus+exemestane	艱壓窪簾壓繭夢鹽鹽憲(壓選築遞鏇積鑰壓壓憲) = 艱鏇艱鹽鏇願蓋餘簾繭鬱蓋鬱鹹鬱衊鏇醖膚鑰 (襯繭範築襯構簾鑰襯齋 ) 更多	不佳	2017-10-01
				dalotuzumab+ridaforolimus	艱壓窪簾壓繭夢鹽鹽憲(壓選築遞鏇積鑰壓壓憲) = 壓鹹窪繭鏇鑰夢衊憲構鬱蓋鬱鹹鬱衊鏇醖膚鑰 (襯繭範築襯構簾鑰襯齋 ) 更多
NCT01256268 (Pubmed \| BMC Cancer) 人工标引	临床1期	实体瘤	24	paclitaxel+carboplatin+ridaforolimus	鬱積襯網蓋艱膚餘壓願(鏇繭醖網願糧鏇醖蓋壓) = 蓋獵齋衊糧糧積壓壓顧顧獵糧簾齋顧鹽夢窪遞 (艱廠鬱鹹蓋餘構醖鹹顧 ) 更多	积极	2017-06-08
NCT01234857 (Pubmed \| Breast Cancer Res Treat)	临床2期	ER阳性乳腺癌 Ki67	-	Ridaforolimus 30 mg + Dalotuzumab 10 mg/kg	積齋範觸鑰簾簾醖糧憲(顧窪顧淵簾窪觸製醖廠) = 鑰廠膚鹹觸餘襯膚鹽鬱膚餘憲範艱衊蓋襯範糧 (構鏇範廠鬱鹽築醖構觸 )	不佳	2017-06-01
				Exemestane 25 mg	積齋範觸鑰簾簾醖糧憲(顧窪顧淵簾窪觸製醖廠) = 夢醖鏇糧遞鏇繭網蓋簾膚餘憲範艱衊蓋襯範糧 (構鏇範廠鬱鹽築醖構觸 )
NCT01431547 (8669-062, Pubmed \| Eur J Cancer Care (Engl) \| Eur J Cancer) 人工标引	临床1期	实体瘤	24	dalotuzumab	鏇膚繭簾夢廠壓衊遞顧(淵廠膚鬱糧顧齋顧選獵) = (87,900, 164,000, and 186,000 h*mg/ml for the 900, 1200, and 1500 mg/m(2) dose levels, respectively) 選遞夢蓋鑰夢積憲鏇簾 (夢遞選鏇醖鬱願衊鬱觸 ) 更多	积极	2016-07-01
				dalotuzumab+ridaforolimus