Centanafadine

Centanafadine
Legal status
Legal status	US: Investigational New Drug;
Identifiers
	IUPAC name (1R,5S)-1-naphthalen-2-yl-3-azabicyclo[3.1.0]hexane;
CAS Number	924012-43-1;
PubChem CID	16095349;
ChemSpider	17253639;
UNII	D2A6T4UH9C;
KEGG	D10697 ;
CompTox Dashboard (EPA)	DTXSID201045788 ;
Chemical and physical data
Formula	C15H15N
Molar mass	209.292 g·mol−1
3D model (JSmol)	Interactive image;
	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]
Site	IC₅₀ (nM)	Action	Ref
SERTTooltip Serotonin transporter	83 nM	Blocker	^[1]
NETTooltip Norepinephrine transporter	6 nM	Blocker	^[1]
DATTooltip Dopamine transporter	38 nM	Blocker	^[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 an IC₅₀ 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]

References

^ ^a ^b ^c ^d ^e "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.
^ "3-Neurotransmitters, 1-Molecule: Optimized Ratios". Neurovance.
^ "EB-1020, a Non-Stimulant Norepinephrine and Dopamine - Preferring Reuptake Inhibitor for the Treatment of Adult ADHD" (PDF). Neurovance. Archived from the original (PDF) on 2015-11-17. Retrieved 2015-11-14.
^ 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.
^ "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 U.S. Research & Development Programs". Otsuka U.S. Otsuka. Retrieved 14 January 2018.^{[permanent dead link‍]}
^ 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)
^ Gunduz-Bruce H (2018-09-26). "SAGE-217 in major depressive disorder: a multicenter, randomized, double-blind, Phase 2 placebo-controlled trial". doi:10.26226/morressier.5b68175eb56e9b005965c44b. S2CID 266120058. Retrieved 2023-06-26.

External links

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[nM-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. Archived from the original (PDF) on 2015-11-17. Retrieved 2015-11-14.

[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.

[euthymics-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.

[Otsuka-8] "Otsuka U.S. Research & Development Programs". Otsuka U.S. Otsuka. Retrieved 14 January 2018.^{[permanent dead link‍]}

[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 H (2018-09-26). "SAGE-217 in major depressive disorder: a multicenter, randomized, double-blind, Phase 2 placebo-controlled trial". doi:10.26226/morressier.5b68175eb56e9b005965c44b. S2CID 266120058. Retrieved 2023-06-26.

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Centanafadine

See also

References

External links

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