Centanafadine
Serotonin-norepinephrine-dopamine reuptake inhibitor
From Wikipedia, the free encyclopedia
Centanafadine, sold under the brand name Simtriyo, is a medication used for the treatment of attention deficit hyperactivity disorder (ADHD).[2] It is taken by mouth (orally).[2]
Molecular structure of centanafadine | |
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| Pronunciation | sen-tan-af-a-deen[1] |
| Trade names | Simtriyo |
| Other names | CTN; EB-1020; EB1020; EB-1020-SR; DOV-216,419; DOV-216419; DOV216419 |
| AHFS/Drugs.com | simtriyo |
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| Routes of administration | Oral (extended-release capsules)[2] |
| Drug class | Serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI); Stimulant |
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| Protein binding | >99%[2] |
| Metabolism | Monoamine oxidase A (MAO-A)[2] |
| Elimination half-life | 5.2 hours[2] |
| Excretion | Urine: 88%[2] Feces: 7%[2] |
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| Formula | C15H15N |
| Molar mass | 209.292 g·mol−1 |
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Side effects of centanafadine include headache, appetite loss, insomnia, nausea, dry mouth, abdominal pain, and rash, among others.[2] The drug is a serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI), with preference for norepinephrine and then dopamine over serotonin, and has psychostimulant effects.[3][2]
Centanafadine was approved for medical use in the United States in July 2026.[2] It is pending scheduling as a controlled substance in the United States.[2]
Medical uses
In the United States, centanafadine is indicated for the treatment of attention deficit hyperactivity disorder (ADHD) in adults and children aged six years and older who weight at least 20 kg (44 lb).[2] Use is not recommended in children younger than six years, as a higher incidence of weight loss was observed, or in those weighing less than 20 kg (44 lb), as data is lacking.[2]
Available forms
Centanafadine is available in the form of extended-release oral capsules.[2]
Contraindications
Contraindications of centanafadine include hypersensitivity to centanafadine or its excipients, concomitant use within 14 days of taking or stopping a monoamine oxidase inhibitor (MAOI), and history of pheochromocytoma.[2] The drug also has various warnings and precautions.[2]
Side effects
Side effects of centanafadine include decreased appetite, nausea, rash, abdominal pain, fatigue, insomnia, dry mouth, diarrhea, irritability, elevated mood, and euphoria, among others.[2]
Overdose
There is limited experience with overdose of centanafadine.[2] In clinical trials, centanafadine overdose resulted in symptoms including vomiting, tachypnea, tachycardia, and elevated blood pressure.[2] Stimulant overdose in general may result in posterior reversible encephalopathy syndrome (PRES) symptoms including headache, altered mental status, hypertension, seizures, and visual disturbances.[2] Treatment of centanafadine overdose should be supportive and based on symptoms.[2]
Interactions
Centanafadine is primarily metabolized by monoamine oxidase A (MAO-A) and hence should not be taken in combination with monoamine oxidase inhibitors (MAOIs).[2]
Pharmacology
Pharmacodynamics
Centanafadine is a psychostimulant and acts as a serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI).[2][4] Its IC50 values for monoamine reuptake inhibition have been reported to be 6 nM for norepinephrine, 38 nM for dopamine, and 83 nM for serotonin.[4] Hence, the drug shows 6.3-fold preference for inhibition of norepinephrine reuptake over dopamine reuptake, 13.8-fold preference for inhibition of norepinephrine reuptake over serotonin reuptake, and 2.2-fold preference for inhibition of dopamine reuptake over serotonin reuptake.[4]
Pharmacokinetics
Centanafadine is primarily metabolized by monoamine oxidase A (MAO-A).[2] The elimination half-life of centanafadine is 5.2 hours.[2]
Chemistry
Centanafadine is a substituted naphthylethylamine and cyclized phenethylamine.[5]
Analogues
Some structurally related compounds to centanafadine include various compounds containing a naphthyl aromatic ring joined to an aminoalkyl group such as naphthylaminopropane (PAL-287), naphthylmorpholine (PAL-678), methylnaphthidate (HDMP-28), 1-(2-naphthyl)piperazine (2-NP; 1-deazaquipazine) and WF-23, as well as other substituted 3-azabicyclo[3.1.0]hexanes such as bicifadine, amitifadine and DOV-216,303.
History
Centanafadine's development began with Euthymics Bioscience after it acquired DOV Pharmaceutical.[3] It was developed as a treatment for attention-deficit hyperactivity disorder (ADHD).[3][6] In 2011, Euthymics Bioscience spun off its development of centanafadine to a new company called Neurovance.[7] In March 2017, Otsuka Pharmaceutical acquired Neurovance and the rights to centanafadine.[8] Centanafadine was approved for medical use in the United States in July 2026.[9]
Society and culture
Names
Centanafadine is the generic name of the drug and its International Nonproprietary Name (INN)[10] and United States Adopted Name (USAN).[5] It is also known by its former developmental code names EB-1020 and DOV-216419[3] and is sold under the brand name Simtriyo.[2]
Legal status
Centanafadine was approved for medical use in the United States in July 2026.[2] Centanafadine shows misuse liability similar to that of amphetamine in humans.[2] Its controlled substance scheduling is pending in the United States.[2]
Research
In addition to its approved indication of attention deficit hyperactivity disorder (ADHD), centanafadine is under development for the treatment of anxiety disorders, major depressive disorder, and smoking withdrawal.[3] As of June 2026, it is in phase 3 clinical trials for anxiety disorders and is in phase 2 trials for major depressive disorder and smoking withdrawal.[3] The drug was also under development for the treatment of binge-eating disorder and neuropathic pain, but development for these indications was discontinued.[3]
