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Centanafadine

From Wikipedia, the free encyclopedia
(Redirected from EB-1020)

Centanafadine
Molecular structure of centanafadine
3D representation of a centanafadine molecule
Clinical data
Trade namesSimtriyo
Other namesCTN; EB-1020; EB1020; EB-1020-SR; DOV-216,419; DOV-216419; DOV216419
AHFS/Drugs.comsimtriyo
License data
Routes of
administration		Oral (extended-release capsules)[1]
Drug classNorepinephrine-dopamine-serotonin reuptake inhibitor
ATC code
  • None
Legal status
Legal status
Pharmacokinetic data
Protein binding>99%[1]
MetabolismMonoamine oxidase A (MAO-A)[1]
Elimination half-life5.2 hours[1]
ExcretionUrine: 88%[1]
Feces: 7%[1]
Identifiers
  • (1R,5S)-1-naphthalen-2-yl-3-azabicyclo[3.1.0]hexane
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC15H15N
Molar mass209.292 g·mol−1
3D model (JSmol)
  • C1[C@H]2[C@@]1(CNC2)C3=CC4=CC=CC=C4C=C3
  • InChI=1S/C15H15N/c1-2-4-12-7-13(6-5-11(12)3-1)15-8-14(15)9-16-10-15/h1-7,14,16H,8-10H2/t14-,15+/m1/s1
  • Key:HKHCSWPSUSWGLI-CABCVRRESA-N

Centanafadine, sold under the brand name Simtriyo, is a medication used for the treatment of attention deficit hyperactivity disorder (ADHD).[1] It is a serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI).[2] It is taken by mouth (orally).[1]

Centanafadine was approved for medical use in the United States in July 2026.[1]

Medical uses

[edit]

Centanfadine is indicated for the treatment of attention deficit hyperactivity disorder (ADHD) in people aged six years of age and older weighing at least 20 kg (44 lb).[1]

Available forms

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Centanafadine is available in the form of extended-release oral capsules.[1]

Side effects

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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

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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

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Centanafadine acts as a serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI).[1][3] Its IC50Tooltip half-maximal inhibitory concentration 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]

Pharmacology[3]
SiteIC50 (nM)ActionRef
SERTTooltip Serotonin transporter83 nMInhibitor[3]
NETTooltip Norepinephrine transporter6 nMInhibitor[3]
DATTooltip Dopamine transporter38 nMInhibitor[3]

Pharmacokinetics

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Centanafadine is primarily metabolized by monoamine oxidase A (MAO-A).[1] The elimination half-life of centanafadine is 5.2 hours.[1]

Chemistry

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Centanafadine is a substituted naphthylethylamine and cyclized phenethylamine.[4]

History

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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.[5] In March 2017, Otsuka Pharmaceutical acquired Neurovance and the rights to centanafadine.[6] Centanafadine was approved for medical use in the United States in July 2026.[7]

Society and culture

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[edit]

Centanafadine was approved for medical use in the United States in July 2026.[1] Centanafadine shows misuse liability similar to that of amphetamine in humans.[1] Its controlled substance scheduling is pending in the United States.[1]

Names

[edit]

Centanafadine is the generic name of the drug and its International Nonproprietary Name (INN)[8] and United States Adopted Name (USAN).[4] It is also known by its former developmental code names EB-1020 and DOV-216419[2] and is sold under the brand name Simtriyo.[1]

Research

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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.[2] 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.[2] The drug was also under development for the treatment of binge-eating disorder and neuropathic pain, but development for these indications was discontinued.[2]

References

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  1. 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 https://www.accessdata.fda.gov/drugsatfda_docs/label/2026/218145s000lbl.pdf
  2. 1 2 3 4 5 6 7 "Centanafadine - Otsuka Pharmaceutical". AdisInsight. 30 June 2026. Retrieved 28 July 2026.
  3. 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.
  4. 1 2 "Centanafadine". PubChem. Retrieved 28 July 2026.
  5. ↑ "Euthymics Bioscience, Inc. Presents Data That Support Advancing EB-1020 into Clinical Trials for Adult ADHD". Fierce Pharma. 7 December 2011. Retrieved 31 July 2026.
  6. ↑ "Otsuka Pharmaceutical to Acquire Neurovance, Inc" (Press release). Otsuka. 1 March 2017. Retrieved 14 January 2018.
  7. ↑ "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" (Press release). Otsuka. 24 July 2026. Retrieved 25 July 2026.
  8. ↑ World Health Organization (2015). "International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 74". WHO Drug Information. 29 (3). hdl:10665/331070.
[edit]
  • Clinical trial number NCT05428033 for "A Trial of Centanafadine Efficacy and Safety in Children With Attention-deficit/Hyperactivity Disorder (ADHD)" at ClinicalTrials.gov
  • Clinical trial number NCT05257265 for "A Trial of Centanafadine Efficacy and Safety in Adolescents With Attention- Deficit/Hyperactivity Disorder" at ClinicalTrials.gov
  • Clinical trial number NCT03605680 for "A Trial Evaluating the Efficacy, Safety, & Tolerability of Centanafadine Sustained-release Tablets in Adults With Attention-deficit/Hyperactivity Disorder" at ClinicalTrials.gov
  • Clinical trial number NCT03605836 for "A Trial to Evaluate the Efficacy, Safety, and Tolerability of Centanafadine Sustained-release Tablets in Adults With Attention-deficit/Hyperactivity Disorder" at ClinicalTrials.gov
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