SEP-4199 explained
| Legal Status: | Investigational |
| Cas Number: | 71675-90-6 |
| Cas Supplemental: | (R)
71675-92-8 (S) |
| Unii: | B4J10KD2KI |
| Unii2: | ES3TWM82E8 |
| Pubchem: | 5746246 |
| Pubchem2: | 3055076 |
| C: | 17 |
| H: | 27 |
| N: | 3 |
| O: | 4 |
| S: | 1 |
SEP-4199 is a non-racemic amisulpride engineered to have higher binding affinity for the 5-HT7 receptor and lower affinity for the D2 receptor compared to conventional racemic amisulpride.[1] It contains the R- and S-enantiomers of amisulpride in an 85:15 ratio rather than a 50:50 ratio. The modification is hoped to give the compound improved efficacy and fewer side effects.[2] It is under development for the treatment of depression in people with bipolar disorder. If approved, it would be the first amisulpride approved in the US for psychiatric indications.[3] It is in a phase III trial as of 2023.[4]
Notes and References
- Hopkins . Seth C. . Wilkinson . Scott . Corriveau . Taryn J. . Nishikawa . Hiroyuki . Nakamichi . Keiko . Loebel . Antony . Koblan . Kenneth S. . Discovery of Nonracemic Amisulpride to Maximize Benefit/Risk of 5-HT7 and D2 Receptor Antagonism for the Treatment of Mood Disorders . Clinical Pharmacology & Therapeutics . 2021 . 110 . 3 . 808–815 . 10.1002/cpt.2282. 33961287 . 8453756 .
- Wu . Jie . Kwan . Angela TH . Rhee . Taeho Greg . Ho . Roger . d’Andrea . Giacomo . Martinotti . Giovanni . Teopiz . Kayla M . Ceban . Felicia . McIntyre . Roger S . A narrative review of non-racemic amisulpride (SEP-4199) for treatment of depressive symptoms in bipolar disorder and LB-102 for treatment of schizophrenia . Expert Review of Clinical Pharmacology . 21 October 2023 . 16 . 11 . 1085–1092 . 10.1080/17512433.2023.2274538 . 37864424 . 264378098 . en . 1751-2433.
- Loebel . Antony . Koblan . Kenneth S. . Tsai . Joyce . Deng . Ling . Fava . Maurizio . Kent . Justine . Hopkins . Seth C. . A Randomized, Double-blind, Placebo-controlled Proof-of-Concept Trial to Evaluate the Efficacy and Safety of Non-racemic Amisulpride (SEP-4199) for the Treatment of Bipolar I Depression . Journal of Affective Disorders . 1 January 2022 . 296 . 549–558 . 10.1016/j.jad.2021.09.109 . 34614447 . 238422271 . 0165-0327. free .
- Web site: Sumitomo, Otsuka's Schizophrenia Candidate Fails Phase III Trials . BioSpace . 9 November 2023.
