Etripamil
(Synonyms: MSP-2017; (-)-MSP-2017) 目录号 : GC65248
Etripamil (MSP-2017) 是一种短效的、L-型 钙通道 拮抗剂，能用于阵发性室上性心动过速 (PSVT) 的研究。Etripamil (MSP-2017) 通过钙离子慢通道抑制钙离子内流，从而减缓房室结传导，延长房室结不应期。
Cas No.:1593673-23-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Etripamil (MSP-2017) is a short-acting L-type calcium-channel antagonist, can be used for the research of Paroxysmal Supraventricular Tachycardia (PSVT). Etripamil (MSP-2017) slows atrioventricular nodal conduction and prolongs atrioventricular nodal refractory periods by inhibiting calcium ion influx through the calcium slow channels in the atrioventricular node cells[1][2].
[1]. Stambler BS, et al. Etripamil Nasal Spray for Rapid Conversion of Supraventricular Tachycardia to Sinus Rhythm. J Am Coll Cardiol. 2018 Jul 31;72(5):489-497.
[2]. Milestone Pharmaceuticals Announces USAN Approval of Generic Name "Etripamil" for its Phase 2 Clinical Development Product for the Treatment of Paroxysmal Supraventricular Tachycardia.
| Cas No. | 1593673-23-4 | SDF | Download SDF |
| 别名 | MSP-2017; (-)-MSP-2017 | ||
| 分子式 | C27H36N2O4 | 分子量 | 452.59 |
| 溶解度 | Ethanol : 120 mg/mL (265.14 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2095 mL | 11.0475 mL | 22.0951 mL |
| 5 mM | 0.4419 mL | 2.2095 mL | 4.419 mL |
| 10 mM | 0.221 mL | 1.1048 mL | 2.2095 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Etripamil nasal spray: an investigational agent for the rapid termination of paroxysmal supraventricular tachycardia (SVT)
Expert Opin Investig Drugs 2020 Jan;29(1):1-4.PMID:31825681DOI:10.1080/13543784.2020.1703180.
Introduction: Paroxysmal supraventricular tachycardia (SVT) can be very bothersome and may potentially lead to considerable health-care utilization. Non-parenteral medication is currently unavailable for the rapid termination of paroxysmal SVT. However, an intranasal spray formulation of Etripamil, a short-acting calcium-channel blocker, is under investigation as a convenient, safe, and rapidly efficacious means to terminate paroxysmal SVT.Areas covered: This review summarizes the clinical rationale, potential benefit, and clinical trials safety and efficacy data for the use of Etripamil nasal spray to terminate paroxysmal SVT.Expert opinion: Based on the efficacy and tolerability demonstrated in phase 1 and 2 clinical trials, Etripamil nasal spray is a potential convenient, safe, and effective means for patients to terminate paroxysmal SVT. It has the potential to improve quality of life, reduce health-care burden, and alter the current management paradigm for many patients with SVT. Further ongoing evaluation in ambulatory patients will help to determine its real-life practicality, safety, and effectiveness.
Update on Etripamil Nasal Spray for the At-home Treatment of Acute Paroxysmal Supraventricular Tachycardia
Heart Int 2021 Jul 15;15(1):2-6.PMID:36277324DOI:10.17925/HI.2021.15.1.2.
The current treatment of sustained paroxysmal supraventricular tachycardia (PSVT) often requires attendance at a medical facility. This burden is driven by the lack of an effective self-administered treatment for PSVT. Etripamil (Milestone Pharmaceuticals, Saint-Laurent, QC, Canada) is a novel intra-nasal preparation of a rapidly effective but short-acting calcium-channel blocker, which shows promise in offering out-of-hospital treatment for patients with PSVT. Studies, to date, have demonstrated good tolerability and potential efficacy, with a safety profile that is acceptable for unsupervised self-administration. This article reviews the current epidemiology and international guidelines for the treatment of acute PSVT, the pharmacology and clinical trial evidence behind the novel agent Etripamil, and considers its potential role in the management of patients with PSVT.
A Novel Calcium Channel Blocker: Etripamil: What is the Future of Intranasal Drug Delivery in the Treatment of Cardiac Arrhythmias?
Cardiol Rev 2021 Sep-Oct;29(5):253-258.PMID:33060411DOI:10.1097/CRD.0000000000000362.
Symptomatic paroxysmal cardiac arrhythmias are common cardiac conditions that lead to a decreased quality of life, increased healthcare costs, and significant morbidity. Many cardiac arrhythmias increase in frequency with age, and as the elderly population continues to increase, so will the incidence and prevalence of cardiac arrhythmias. The long-term treatment options for patients with paroxysmal arrhythmias include ablation procedures and daily oral antiarrhythmics. Acute management entails vagal maneuvers, intravenous antiarrhythmics, and synchronized cardioversion. However, there are limited treatment options for patients with less frequent and less severe arrhythmias, ablation refractory disease, or who are poor candidates for ablative procedures, For abortive therapy, oral anti-arrhythmic medications are ineffective due to their slow onset of action and intravenous medications require treatment at an acute care facility, which is both costly and stressful to the patient. Etripamil is a novel intranasal non-dihydropyridine calcium channel blocker that has begun phase III clinical trials for the treatment of paroxysmal supraventricular tachycardias. Due to its intranasal mode of delivery, Etripamil has a rapid onset of action, and could feasibly be administered by the patient themselves. Clinical phase II trials of Etripamil in moderate to high doses demonstrated efficacy comparable to the standard of care, and took an average of 3 minutes from drug administration to conversion to sinus rhythm. In this article, we have conducted an extensive literature review of intranasal drug delivery, calcium channel blockers, and Etripamil, to discuss the future possibilities of using this new medication.
Etripamil Nasal Spray for Rapid Conversion of Supraventricular Tachycardia to Sinus Rhythm
J Am Coll Cardiol 2018 Jul 31;72(5):489-497.PMID:30049309DOI:10.1016/j.jacc.2018.04.082.
Background: There is no nonparenteral medication for the rapid termination of paroxysmal supraventricular tachycardia. Objectives: The purpose of this study was to assess the efficacy and safety of Etripamil nasal spray, a short-acting calcium-channel blocker, for the rapid termination of paroxysmal supraventricular tachycardia (SVT). Methods: This phase 2 study was performed during electrophysiological testing in patients with previously documented SVT who were induced into SVT prior to undergoing a catheter ablation. Patients in sustained SVT for 5 min received either placebo or 1 of 4 doses of active compound. The primary endpoint was the SVT conversion rate within 15 min of study drug administration. Secondary endpoints included time to conversion and adverse events. Results: One hundred four patients were dosed. Conversion rates from SVT to sinus rhythm were between 65% and 95% in the Etripamil nasal spray groups and 35% in the placebo group; the differences were statistically significant (Pearson chi-square test) in the 3 highest active compound dose groups versus placebo. In patients who converted, the median time to conversion with Etripamil was <3 min. Adverse events were mostly related to the intranasal route of administration or local irritation. Reductions in blood pressure occurred predominantly in the highest Etripamil dose. Conclusions: Etripamil nasal spray rapidly terminated induced SVT with a high conversion rate. The safety and efficacy results of this study provide guidance for Etripamil dose selection for future studies involving self-administration of this new intranasal calcium-channel blocker in a real-world setting for the termination of SVT. (Efficacy and Safety of Intranasal MSP-2017 [Etripamil] for the Conversion of PSVT to Sinus Rhythm [NODE-1]; NCT02296190).
First Randomized, Multicenter, Placebo-Controlled Study of Self-Administered Intranasal Etripamil for Acute Conversion of Spontaneous Paroxysmal Supraventricular Tachycardia (NODE-301)
Circ Arrhythm Electrophysiol 2022 Dec;15(12):e010915.PMID:36441560DOI:10.1161/CIRCEP.122.010915.
Background: Pharmacologic termination of paroxysmal supraventricular tachycardia (PSVT) often requires medically supervised intervention. Intranasal Etripamil, is an investigational fast-acting, nondihydropyridine, L-type calcium channel blocker, designed for unsupervised self-administration to terminate atrioventricular nodal-dependent PSVT. Phase 2 results showed potential safety and efficacy of Etripamil in 104 patients with PSVT. Methods: NODE-301, a phase 3, multicenter, double-blind, placebo-controlled study evaluated the efficacy and safety of Etripamil nasal spray administered, unsupervised in patients with symptomatic sustained PSVT. After a medically supervised Etripamil test dose while in sinus rhythm, patients were randomized 2:1 to receive Etripamil 70 mg or placebo. When PSVT symptoms developed, patients applied a cardiac monitor and attempted a vagal maneuver; if symptoms persisted, they self-administered blinded treatment. An independent Adjudication Committee reviewed continuous electrocardiogram recordings. The primary efficacy endpoint was termination of adjudicated PSVT within 5 hours after study drug administration. Results: NODE-301 accrued 156 positively adjudicated PSVT events treated with Etripamil (n=107) or placebo (n=49). The hazard ratio for the primary endpoint, time-to-conversion to sinus rhythm during the 5-hour observation period, was 1.086 (95% CI, 0.726-1.623; P=0.12). In predefined sensitivity analyses, Etripamil effects (compared with placebo) occurred at 3, 5, 10, 20, and 30 minutes (P<0.05). For example, at 30 minutes, there was a 53.7% of SVT conversion in the treatment arm compared to 34.7% in the placebo arm (hazard ratio, 1.87 [95% CI, 1.09-3.22]; P=0.02). Etripamil was well tolerated; adverse events were mainly related to transient nasal discomfort and congestion (19.6% and 8.0%, respectively, of randomized treatment-emergent adverse events. Conclusions: Although the primary 5-hour efficacy endpoint was not met, analyses at earlier time points indicated an Etripamil treatment effect in terminating PSVT. Etripamil self-administration during PSVT was safe and well tolerated. These results support continued clinical development of Etripamil nasal spray for self-administration during PSVT in a medically unsupervised setting. Registration: URL: https://www. Clinicaltrials: gov; Unique identifier: NCT03464019.