Centanafadine

Centanafadine
Legal status
Legal status
Identifiers
IUPAC name
  • (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)
SMILES
  • C1=C(C=CC2=CC=CC=C12)[C@@]34C[C@@H]3CNC4
InChI
  • 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
SERT83 nMBlocker[1]
NET6 nMBlocker[1]
DAT38 nMBlocker[1]

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 III clinical trials.[8]

See also

References

  1. 1 2 3 4 5 "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.
  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.
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