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Etripamil (MSP-2017) is a short-acting L-type calcium-channel blocker/antagonist used to treat Paroxysmal Supraventricular Tachycardia (PSVT). It has a rapid onset of action designed for intranasal administration.
On Dec. 12, 2025, Milestone® Pharmaceuticals Inc. (Nasdaq: MIST) announced that the U.S. Food and Drug Administration (FDA) approved its first commercial product, CARDAMYST™ (etripamil) nasal spray, a prescription medication for the conversion of acute symptomatic episodes of paroxysmal supraventricular tachycardia (PSVT) to sinus rhythm in adults.| 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. [1] |
| ADME/Pharmacokinetics |
Absorption
After a single intranasal administration of 70 mg Etripamil, 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 Etripamil 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 Etripamil 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 Etripamil is approximately 2200 to 3500 L. Protein Binding The plasma protein binding rate of Etripamil is approximately 50%. Metabolites/Metabolites The metabolic pathways of Etripamil include hydrolysis, demethylation, N-dealkylation, secondary oxidation, glucuronidation, and taurine conjugation. Etripamil is primarily metabolized by blood esterases and the liver, mainly via the CYP3A4 and CYP3A5 pathways. Etripamil contains a methyl ester group, making it sensitive to esterase metabolism in the blood. Biological Half-Life After administration, the average concentration of Etripamil 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 |
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| Additional Infomation |
Etripamil has been used in research trials for the treatment of paroxysmal supraventricular tachycardia (PSVT).
Drug Indication Treatment of supraventricular arrhythmias Results: A total of 104 patients were enrolled. The conversion rate of SVT to sinus rhythm was 65% to 95% in the Etripamil nasal spray group and 35% in the placebo group; the differences were statistically significant between the three highest-active-component dose groups and the placebo group (Pearson chi-square test). Among patients who converted, the median conversion time of Etripamil was <3 minutes. Adverse events were mainly related to the intranasal administration route or local irritation. Decreased blood pressure mainly occurred in the highest-dose Etripamil group. Conclusion: Etripamil nasal spray can rapidly terminate induced supraventricular tachycardia with a high conversion rate. The safety and efficacy results of this study provide guidance for future research on the self-administration of this novel intranasal calcium channel blocker to terminate supraventricular tachycardia (SVT) in real-world settings, focusing on the selection of Etripamil dosage. (Efficacy and safety of intranasal MSP-2017 [Etripamil] for the treatment of paroxysmal supraventricular tachycardia (PSVT) to sinus rhythm [NODE-1]; NCT02296190). |
| Molecular Formula |
C27H36N2O4
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|---|---|
| Molecular Weight |
452.6
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| Exact Mass |
452.267
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| Elemental Analysis |
C, 71.65; H, 8.02; N, 6.19; O, 14.14
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| CAS # |
1593673-23-4
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| Related CAS # |
2560549-35-9 (HCl); 1593673-23-4
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| PubChem CID |
91824132
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| Appearance |
Brown to wine red solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
593.8±50.0 °C at 760 mmHg
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| Flash Point |
312.9±30.1 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.534
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| LogP |
4.14
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
33
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| Complexity |
645
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O(C([H])([H])[H])C1=C(C([H])=C([H])C(=C1[H])[C@](C#N)(C([H])([H])C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])C([H])([H])C1C([H])=C([H])C([H])=C(C(=O)OC([H])([H])[H])C=1[H])C([H])(C([H])([H])[H])C([H])([H])[H])OC([H])([H])[H]
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| InChi Key |
VAZNEHLGJGSQEL-MHZLTWQESA-N
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| InChi Code |
InChI=1S/C27H36N2O4/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/t27-/m0/s1
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| Chemical Name |
methyl 3-[2-[[(4S)-4-cyano-4-(3,4-dimethoxyphenyl)-5-methylhexyl]-methylamino]ethyl]benzoate
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| Synonyms |
MSP 2017; MSP-2017; Etripamil; 1593673-23-4; Etripamilo; (-)-MSP-2017
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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) |
Ethanol : ~120 mg/mL (~265.14 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (6.63 mM) (saturation unknown) in 10% EtOH + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear EtOH stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 3 mg/mL (6.63 mM) (saturation unknown) in 10% EtOH + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear EtOH stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 3 mg/mL (6.63 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2095 mL | 11.0473 mL | 22.0946 mL | |
| 5 mM | 0.4419 mL | 2.2095 mL | 4.4189 mL | |
| 10 mM | 0.2209 mL | 1.1047 mL | 2.2095 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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