// Workers AI · dad joke modeWhat did Centanafadine say to its friend? "You're a central figure
 Molecular structure of centanafadine | |
 3D representation of a centanafadine molecule | |
| Clinical data | |
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| Trade names | Simtriyo |
| Other names | CTN; EB-1020; EB1020; EB-1020-SR; DOV-216,419; DOV-216419; DOV216419 |
| Routes of administration | Oral[1] |
| Drug class | Serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI); Psychostimulant |
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| Pharmacokinetic data | |
| Protein binding | >99%[1] |
| Metabolism | Monoamine oxidase A (MAO-A)[1] |
| Elimination half-life | 5.2 hours[1] |
| Excretion | Urine: 88%[1] Feces: 7%[1] |
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| Chemical and physical data | |
| Formula | C15H15N |
| Molar mass | 209.292 g·mol−1 |
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Centanafadine, sold under the brand name Simtriyo, is a serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI) and psychostimulant which is used in the treatment of attention deficit hyperactivity disorder (ADHD).[1][2] It is taken orally in a controlled-release formulation.[1][2]
Medical uses
[edit]Centanfadine is used in the treatment of attention deficit hyperactivity disorder (ADHD) in children, adolescents, and adults.[1]
Available forms
[edit]Centanafadine is available in the form of 140 mg, 210 mg, and 280 mg extended-release oral capsules.[1]
Side effects
[edit]Side effects of centanafadine include decreased appetite, nausea, rash, abdominal pain, fatigue, insomnia, dry mouth, diarrhea, irritability, elevated mood, and euphoria, among others.[1]
Interactions
[edit]Centanafadine is primarily metabolized by monoamine oxidase A (MAO-A) and hence should not be taken in combination with monoamine oxidase inhibitors (MAOIs).[1]
Pharmacology
[edit]Pharmacodynamics
[edit]Centanafadine acts as a serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI).[1][2][3] 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.[3] 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.[3]
| Site | IC50 (nM) | Action | Ref |
|---|---|---|---|
| SERT | 83 nM | Inhibitor | [3] |
| NET | 6 nM | Inhibitor | [3] |
| DAT | 38 nM | Inhibitor | [3] |
Pharmacokinetics
[edit]Centanafadine is primarily metabolized by monoamine oxidase A (MAO-A).[1] The elimination half-life of centanafadine is 5.2 hours.[1]
Chemistry
[edit]Centanafadine is a substituted naphthylethylamine and cyclized phenethylamine.
History
[edit]Centanafadine's development began with Euthymics Bioscience after it acquired DOV Pharmaceutical.[2] It was developed as a treatment for attention-deficit hyperactivity disorder (ADHD).[2] In 2011, Euthymics Bioscience spun off its development of centanafadine to a new company called Neurovance.[4][5] In March 2017, Otsuka Pharmaceutical acquired Neurovance and the rights to centanafadine.[6] As of July 24th 2026 Centanafadine has received First in Class FDA approval for the treatment of ADHD in Adults and Pediatric Patients aged 6 and older. [7]
Society and culture
[edit]Names
[edit]Centanafadine is the generic name of the drug and its INN and USAN.[8]
Legal status
[edit]Centanafadine shows misuse liability similar to that of amphetamine in humans.[1] Its controlled substance scheduling is pending in the United States.[1]
Research
[edit]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, smoking withdrawal.[1] 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.[1] The drug was also under development for the treatment of binge-eating disorder and neuropathic pain, but development for these indications was discontinued.[1]
See also
[edit]References
[edit]- 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 https://otsuka-us.com/media/static/Simtriyo-PI.pdf
- 1 2 3 4 5 "Otsuka Pharmaceutical". AdisInsight. 30 June 2026. Retrieved 28 July 2026.
- 1 2 3 4 5 6 7 Bymaster FP, Golembiowska K, Kowalska M, Choi YK, Tarazi FI (June 2012). "Pharmacological characterization of the norepinephrine and dopamine reuptake inhibitor EB-1020: implications for treatment of attention-deficit hyperactivity disorder". Synapse. 66 (6): 522–532. doi:10.1002/syn.21538. PMID 22298359. S2CID 38850652.
- ↑ "Euthymics". Ethismos Research Inc. Retrieved 14 January 2018.
- ↑ "EUTHYMICS BIOSCIENCE, INC. PRESENTS DATA THAT SUPPORT ADVANCING EB-1020 INTO CLINICAL TRIALS FOR ADULT ADHD" (PDF). Neurovance. December 7, 2011. Retrieved 14 January 2018.
- ↑ "Otsuka Pharmaceutical to Acquire Neurovance, Inc". Otsuka. Retrieved 14 January 2018.
- ↑ "Otsuka Receives FDA Approval for First-in-Class SIMTRIYO® (centanafadine) for the Treatment of Attention-Deficit Hyperactivity Disorder (ADHD) in Adults and Pediatric Patients Aged 6 Years and Older | Otsuka US". www.otsuka-us.com. Retrieved 2026-07-25.
- ↑ "Centanafadine". PubChem. Retrieved 28 July 2026.