| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
L-type calcium channel
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|---|---|
| ln Vitro |
Etripamil is a novel, short-acting, nondihydropyridine L-type calcium channel blocker formulated for intranasal administration. It exerts its anti-arrhythmic effect by inhibiting voltage-dependent L-type calcium channels (Cav1.2 and Cav1.3), which are critical for mediating calcium entry into cardiac myocytes and regulating excitation-contraction coupling and nodal conduction. Specifically, etripamil targets the L-type calcium channels expressed on atrioventricular (AV) nodal cells, arterial smooth muscles, and contractile myocardial cells. By blocking calcium influx, the drug prolongs the refractory period and slows electrical conduction through the AV node, thereby interrupting the re-entrant circuits responsible for AV-nodal dependent paroxysmal supraventricular tachycardia (PSVT) and facilitating the restoration of sinus rhythm.
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| ln Vivo |
Etripamil is a fast-acting agent with a short duration of action. Etripamil prolonged the baseline PR interval by 8% to 10% approximately five minutes following an intranasal dose of 70 mg. Clinical data shows significant efficacy in terminating arrhythmias within 15 to 60 minutes post-administration, but its effects diminish rapidly, with no significant difference in conversion rates observed by 300 minutes compared to placebo.
Etripamil is a nondihydropyridine, L-type calcium channel blocker. It is a fast-acting drug with a short duration of action. The nasal formulation of etripamil was first approved by the FDA on December 12, 2025 for the conversion of acute symptomatic episodes of paroxysmal supraventricular tachycardia (PSVT) to sinus rhythm in adults. ETRIPAMIL is a small molecule drug with a maximum clinical trial phase of III (across all indications) and has 4 investigational indications. |
| Animal Protocol |
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.
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| ADME/Pharmacokinetics |
Absorption
After a single intranasal administration of 70 mg etrapamide, the mean (%CV) area under the concentration-time curve (AUC) was approximately 5461 (51.6%) ng·min/mL, and the Cmax was approximately 99 (64.6%) ng/mL. After a second intranasal administration of 70 mg etrapamide 10 minutes after the first administration, the mean (%CV) AUC was approximately 7721 (50.3%) ng·min/mL, and the Cmax was approximately 132 (59.1%) ng/mL. After a single intranasal administration of 70 mg, the median (range) Tmax was 7 minutes (3 to 20 minutes). After a second intranasal administration of 70 mg, the median Tmax was 13 minutes (3 to 35 minutes). Excretion Route Following a single intranasal administration of 70 mg of radiolabeled etrapamide to healthy subjects, approximately 29% of the dose is excreted in the urine (<0.05% unchanged), 26% in the feces (<0.05% unchanged), and the remainder is excreted in nasal and facial tissues. Approximately 71% of the total administered dose is excreted within 7–10 days. Volume of Distribution The mean apparent volume of distribution of etrapamide is approximately 2200 to 3500 L. Protein Binding The plasma protein binding rate of etrapamide is approximately 50%. Metabolites/Metabolites The metabolic pathways of etrapamide include hydrolysis, demethylation, N-dealkylation, secondary oxidation, glucuronidation, and taurine conjugation. Etrapamide is primarily metabolized by blood esterases and the liver, mainly via the CYP3A4 and CYP3A5 pathways. Etrapamide contains a methyl ester group, making it sensitive to esterase metabolism in the blood. Biological Half-Life After administration, the average concentration of etrapamide decreases to approximately 60% of its peak concentration (Cmax) at 25 minutes and to approximately 80% of Cmax at 60 minutes. Subsequently, the rate of concentration decline slows, and the half-life is approximately 2.5 hours. |
| References | |
| Additional Infomation |
Results: A total of 104 patients received the medication. The conversion rate of supraventricular tachycardia (SVT) to sinus rhythm was 65%–95% in the etrapamide nasal spray group and 35% in the placebo group; statistically significant differences were observed between the three groups with the highest active compound doses and the placebo group (Pearson chi-square test). The median conversion time for etrapamide to sinus rhythm was <3 minutes in patients who converted. Adverse events were mainly related to the intranasal administration route or local irritation. Decreased blood pressure occurred primarily in the highest-dose etrapamide group. Conclusion: Etrapamide nasal spray rapidly terminates induced SVT with a high conversion rate. The safety and efficacy results of this study can provide guidance for future real-world studies involving patient self-administration of this novel intranasal calcium channel blocker to terminate SVT, specifically regarding etrapamide dosage selection. (Efficacy and safety of intranasal MSP-2017 [etraprami] in the treatment of paroxysmal supraventricular tachycardia converting to sinus rhythm [NODE-1]; NCT02296190).
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| Molecular Formula |
C27H37CLN2O4
|
|---|---|
| Molecular Weight |
489.05
|
| Exact Mass |
488.244185
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| Elemental Analysis |
C, 66.31; H, 7.63; Cl, 7.25; N, 5.73; O, 13.09
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| CAS # |
2560549-35-9
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| Related CAS # |
2560549-35-9 (HCl); 1593673-23-4
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| PubChem CID |
169490895
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| Appearance |
Typically exists as solids at room temperature
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
13
|
| Heavy Atom Count |
34
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| Complexity |
645
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC(C)[C@](CCCN(C)CCC1=CC(=CC=C1)C(=O)OC)(C#N)C2=CC(=C(C=C2)OC)OC.Cl
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| InChi Key |
JHOAIMAMBNLIMD-YCBFMBTMSA-N
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| InChi Code |
InChI=1S/C27H36N2O4.ClH/c1-20(2)27(19-28,23-11-12-24(31-4)25(18-23)32-5)14-8-15-29(3)16-13-21-9-7-10-22(17-21)26(30)33-6;/h7,9-12,17-18,20H,8,13-16H2,1-6H3;1H/t27-;/m0./s1
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| Chemical Name |
methyl 3-[2-[[(4S)-4-cyano-4-(3,4-dimethoxyphenyl)-5-methylhexyl]-methylamino]ethyl]benzoate;hydrochloride
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| Synonyms |
MSP-2017 hydrochloride; 2560549-35-9; Etripamil hydrochloride; Etripamil (hydrochloride); 9TA9AC3H8Z; orb2945709; (-)-MSP-2017 hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0448 mL | 10.2239 mL | 20.4478 mL | |
| 5 mM | 0.4090 mL | 2.0448 mL | 4.0896 mL | |
| 10 mM | 0.2045 mL | 1.0224 mL | 2.0448 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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