全氟戊烷/全氟异戊烷(Dodecafluoropentane) - 药物靶点：Potassium channel_专利_临床

概要

基本信息

药物类型

小分子化药

别名

dodecafluoropentane、EchoGen、Perflenapent/Perflisopent

+ [4]

靶点

Potassium channel

作用机制

钾离子通道调节剂

治疗领域

心血管疾病

在研适应症-

非在研适应症

心血管疾病

原研机构

Sonus Pharmaceuticals, Inc.

在研机构-

非在研机构

Sonus Pharmaceuticals, Inc.

最高研发阶段撤市

首次获批日期

欧盟 (1998-07-17),

心血管疾病

最高研发阶段(中国)-

特殊审评-

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结构

分子式C5F12

InChIKeyNJCBUSHGCBERSK-UHFFFAOYSA-N

CAS号678-26-2

关联

100 项与全氟戊烷/全氟异戊烷相关的临床结果

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100 项与全氟戊烷/全氟异戊烷相关的转化医学

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100 项与全氟戊烷/全氟异戊烷相关的专利（医药）

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44

项与全氟戊烷/全氟异戊烷相关的文献（医药）

2023-09-01·Journal of ultrasound in medicine : official journal of the American Institute of Ultrasound in Medicine

An Experimental Study: Treatment of Subcutaneous C6 Glioma in Rats Using Acoustic Droplet Vaporization.

Article

作者: Yao, Lei ; Liu, Zheng ; Li, Hui ; Yin, Jiabei ; Luo, Tingting ; Yang, Guoliang

OBJECTIVE:

The objective of this study was to investigate the treatment effects of acoustic droplet vaporization (ADV) on tumors.

METHODS:

Experiments were conducted on subcutaneous C6 glioma implanted in 37 rats. Twenty-five rats were divided into five groups treated by ultrasound (US) + dodecafluoropentane (DDFP), US + microbubble (MB), US, DDFP, or saline, respectively. ADV was performed using DDFP droplets (2-5 μm) triggered by non-focused pulsed ultrasound. Macroscopic and histological changes of the tumor were compared with investigation of the tumor ablation effect of ADV. Tumor temperature was measured before and immediately after treatment to explore temperature changes. Furthermore, another 12 rats with bilateral tumors were divided into two groups. Six animals received ADV treatment on unilateral tumor, while another six received saline injection on unilateral tumor. The tumor blood perfusion, tumor volume and related immune response were measured.

RESULTS:

The tumors treated by ADV were partially damaged without significant temperature rise. For the animals with bilateral tumors, the tumor blood perfusion around the damaged area on the side receiving ADV still existed. Additionally, the bilateral tumors of animals treated with ADV were smaller than those of animals treated with saline, along with stronger immune response and more tumor cell apoptosis in tumors on both sides.

CONCLUSION:

The study demonstrated that ADV treatment could damage subcutaneous glioma in rats by mechanical effect and enhance systemic immune response to furtherly inhibit the tumor growth.

2023-08-01·Cancer research communications

Dodecafluoropentane Emulsion as a Radiosensitizer in Glioblastoma Multiforme.

Article

作者: Lickliter, Jason D ; Ruben, Jeremy ; Jennens, Ross ; Gzell, Cecelia ; Kichenadasse, Ganessan ; Zhou, Heling ; Stea, Baldassarre ; Mason, Ralph P ; Becker, Jennifer ; Unger, Evan

Purpose:

Glioblastoma multiforme (GBM) is a hypoxic tumor resistant to radiotherapy. The purpose of this study was to assess the safety and efficacy of a novel oxygen therapeutic, dodecafluoropentane emulsion (DDFPe), in chemoradiation treatment of GBM.

Experimental Design:

In this multicenter phase Ib/II dose-escalation study, patients were administered DDFPe via intravenous infusion (0.05, 0.10, or 0.17 mL/kg) while breathing supplemental oxygen prior to each 2 Gy fraction of radiotherapy (30 fractions over 6 weeks). Patients also received standard-of-care chemotherapy [temozolomide (TMZ)]. Serial MRI scans were taken to monitor disease response. Adverse events were recorded and graded. TOLD (tissue oxygenation level-dependent) contrast MRI was obtained to validate modulation of tumor hypoxia.

Results:

Eleven patients were enrolled. DDFPe combined with radiotherapy and TMZ was well tolerated in most patients. Two patients developed delayed grade 3 radiation necrosis during dose escalation, one each at 0.1 and 0.17 mL/kg of DDFPe. Subsequent patients were treated at the 0.1 mL/kg dose level. Kaplan-Meier analysis showed a median overall survival of 19.4 months and a median progression-free survival of 9.6 months, which compares favorably to historical controls. Among 6 patients evaluable for TOLD MRI, a statistically significant reduction in tumor T₁ was observed after DDFPe treatment.

Conclusions:

This trial, although small, showed that the use of DDFPe as a radiosensitizer in patients with GBM was generally safe and may provide a survival benefit. This is also the first time than TOLD MRI has shown reversal of tumor hypoxia in a clinical trial in patients. The recommended dose for phase II evaluation is 0.1 mL/kg DDFPe.Trial Registration: NCT02189109.

Significance:

This study shows that DDFPe can be safely administered to patients, and it is the first-in-human study to show reversal of hypoxia in GBM as measured by TOLD MRI. This strategy is being used in a larger phase II/III trial which will hopefully show a survival benefit by adding DDFPe during the course of fractionated radiation and concurrent chemotherapy.

2023-06-16·Intensive care medicine experimental

The impact of intravenous dodecafluoropentane on a murine model of acute lung injury.

Article

作者: Kempf, Carrie ; Mosier, Jarrod M ; Unger, Evan ; Garcia, Joe G N ; Sammani, Saad

INTRODUCTION:

Intravenous oxygen therapeutics present an appealing option for improving arterial oxygenation in patients with acute hypoxemic respiratory failure, while limiting iatrogenic injury from conventional respiratory management.

METHODS:

We used an established two-hit murine model of acute lung injury (ARDS/VILI) to evaluate the effect of intravenous dodecafluoropentane (DDFPe) on oxygen saturation and bronchoalveolar lavage cell counts and protein levels. Twenty hours after challenge with intratracheal lipopolysaccharide, mice were intubated and ventilated with high tidal volumes (4 h) to produce acute lung injury. DDFPe (0.6 mL/kg) or saline was administered by IV bolus injection at the initiation of mechanical ventilation and again at 2 h. Oxygen saturation was measured every 15 min. Bronchoalveolar lavage was performed at the conclusion of the experiment.

RESULTS:

The two-hit ARDS/VILI model produced substantial inflammatory acute lung injury reflected by markedly increased bronchoalveolar lavage (BAL) cell counts compared to BAL cell counts in spontaneous breathing controls (5.29 ± 1.50 × 10^-6 vs 0.74 ± 0.014 × 10^-6 cells/mL) Similarly, BAL protein levels were markedly elevated in ARDS/VILI-challenged mice compared with spontaneous breathing controls (1109.27 ± 223.80 vs 129.6 ± 9.75 ng/mL). We fit a linear mixed effects model that showed a significant difference in oxygen saturation over time between DDFPe-treated mice and saline-treated mice, with separation starting after the 2-h injection. DDFPe-treated ARDS/VILI-challenged mice also exhibited significant reductions in BAL cell counts but not in BAL protein.

CONCLUSION:

DDFPe improves oxygen saturation in a murine model of ARDS/VILI injury with the potential for serving as an intravenous oxygen therapeutic.

100 项与全氟戊烷/全氟异戊烷相关的药物交易

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研发状态

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
心血管疾病	欧盟	Sonus Pharmaceuticals, Inc.	1998-07-17
心血管疾病	冰岛	Sonus Pharmaceuticals, Inc.	1998-07-17
心血管疾病	列支敦士登	Sonus Pharmaceuticals, Inc.	1998-07-17
心血管疾病	挪威	Sonus Pharmaceuticals, Inc.	1998-07-17

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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


NCT02963376 (Pubmed \| J Vasc Interv Radiol) 人工标引	临床1/2期	急性缺血性卒中	24	Dodecafluoropentane	壓鑰淵獵襯壓範衊襯鏇(鹹壓觸繭鏇鏇醖簾繭遞) = Early initiation of DDFPe treatment resulted in better NIHSS score response than late initiation (P = 0.03). 襯醖蓋夢壓蓋鏇築膚醖 (鏇壓鏇憲簾繭憲遞齋餘 ) 更多	积极	2019-08-01
NCT02963376 (Pubmed \| J Vasc Interv Radiol) 人工标引	临床1/2期	急性缺血性卒中	24	Placebo		积极	2019-08-01
ISC2015	N/A	-	6	Dodecafluoropentane emulsion	壓選膚積醖窪齋艱積繭(積淵蓋鑰簾網觸遞獵鏇) = 鹽顧夢選夢鑰鹹夢繭壓壓顧願蓋鹽鬱鑰衊鹹鬱 (繭築窪築窪憲繭築醖膚 ) 更多	-	2015-02-01
ISC2013	N/A	-	8	Dodecafluoropentane Emulsion (Single bolus (0.6 mL/kg))	餘繭憲窪網窪艱膚觸蓋(襯築蓋遞膚鏇壓鏇醖餘) = 構膚糧鹽鬱襯選顧壓衊壓鹽築壓顧糧淵蓋壓窪 (廠衊艱製構積願鏇衊夢 ) 更多	-	2013-02-01