Centanafadine Explained

Centanafadine [1]
Site IC50 (nM) Action Ref
83 nM Blocker
6 nM Blocker
38 nM Blocker

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.[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]

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Notes and References

  1. News: Neurovance's EB-1020 SR for Adult ADHD Shows Stimulant-Like Efficacy and Good Tolerability in Phase 2a Trial. 14 January 2018. Neurovance.
  2. Web site: 3-Neurotransmitters, 1-Molecule: Optimized Ratios . Neurovance.
  3. Web site: EB-1020, a Non-Stimulant Norepinephrine and Dopamine - Preferring Reuptake Inhibitor for the Treatment of Adult ADHD . Neurovance . 2015-11-14 . 2015-11-17 . https://web.archive.org/web/20151117023856/http://euthymics.com/wp-content/uploads/2012/10/White-Paper-EB1020-092612.pdf . dead .
  4. Bymaster FP, Golembiowska K, Kowalska M, Choi YK, Tarazi FI . Pharmacological characterization of the norepinephrine and dopamine reuptake inhibitor EB-1020: implications for treatment of attention-deficit hyperactivity disorder . Synapse . 66 . 6 . 522–32 . June 2012 . 22298359 . 10.1002/syn.21538 . 38850652 .
  5. Web site: Euthymics. Ethismos Research Inc.. 14 January 2018. euthymics.
  6. News: EUTHYMICS BIOSCIENCE, INC. PRESENTS DATA THAT SUPPORT ADVANCING EB-1020 INTO CLINICAL TRIALS FOR ADULT ADHD. 14 January 2018. Neurovance. December 7, 2011.
  7. Web site: Otsuka Pharmaceutical to Acquire Neurovance, Inc.. Otsuka. 14 January 2018.
  8. Web site: Otsuka U.S. Research & Development Programs. Otsuka U.S.. Otsuka. 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 .
  10. Web site: Gunduz-Bruce . Handan . 2018-09-26 . SAGE-217 in major depressive disorder: a multicenter, randomized, double-blind, Phase 2 placebo-controlled trial . 2023-06-26 . 10.26226/morressier.5b68175eb56e9b005965c44b . 266120058 .

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