Centanafadine

Centanafadine (INN) (former developmental code name EB-1020) is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI) that began its development with Euthymics Bioscience after they acquired DOV Pharmaceutical. It was developed as a treatment for attention-deficit hyperactivity disorder (ADHD) and inhibits the reuptake of norepinephrine, dopamine, and serotonin with a ratio of 1:6:14, respectively.[1][2][3][4] In 2011, Euthymics Bioscience spun off its development of centanafadine to a new company called Neurovance.[5][6] In March 2017, Otsuka Pharmaceutical acquired Neurovance and the rights to centanafadine.[7] As of January 2018, Otsuka's pipeline indicates it is in Phase II and III clinical trials for a number of different applications to medical conditions.[8][9][10]

Centanafadine
Legal status
Legal status
Identifiers
  • (1R,5S)-1-naphthalen-2-yl-3-azabicyclo[3.1.0]hexane
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
Chemical and physical data
FormulaC15H15N
Molar mass209.292 g·mol−1
3D model (JSmol)
  • C1=C(C=CC2=CC=CC=C12)[C@@]34C[C@@H]3CNC4
  • 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 [1]
SiteIC50 (nM)ActionRef
SERTTooltip Serotonin transporter83 nMBlocker[1]
NETTooltip Norepinephrine transporter6 nMBlocker[1]
DATTooltip Dopamine transporter38 nMBlocker[1]

See also

References
  1. "Neurovance's EB-1020 SR for Adult ADHD Shows Stimulant-Like Efficacy and Good Tolerability in Phase 2a Trial" (PDF). Neurovance. Retrieved 14 January 2018.
  2. "3-Neurotransmitters, 1-Molecule: Optimized Ratios". Neurovance.
  3. "EB-1020, a Non-Stimulant Norepinephrine and Dopamine - Preferring Reuptake Inhibitor for the Treatment of Adult ADHD" (PDF). Neurovance.
  4. 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): 522–32. doi:10.1002/syn.21538. PMID 22298359. S2CID 38850652.
  5. "Euthymics". Ethismos Research Inc. Retrieved 14 January 2018.
  6. "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.
  7. "Otsuka Pharmaceutical to Acquire Neurovance, Inc". Otsuka. Retrieved 14 January 2018.
  8. "Otsuka U.S. Research & Development Programs". Otsuka U.S. Otsuka. Retrieved 14 January 2018.
  9. Otsuka Pharmaceutical Development & Commercialization, Inc. (2021-09-17). "A Phase 3, Randomized, Double-blind, Multicenter, Placebo-controlled, Parallel-group Trial Evaluating the Efficacy, Safety, and Tolerability of Centanafadine Sustained-release Tablets in Adults With Attention-deficit/Hyperactivity Disorder". {{cite journal}}: Cite journal requires |journal= (help)
  10. Gunduz-Bruce, Handan (2018-09-26). "SAGE-217 in major depressive disorder: a multicenter, randomized, double-blind, Phase 2 placebo-controlled trial". dx.doi.org. Retrieved 2023-06-26.
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