SEP-4199
 Aramisulpride (R)-amisulpride | |
 Esamisulpride (S)-amisulpride | |
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| Formula | C17H27N3O4S |
| Molar mass | 369.48 g·mol−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][2] 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.[3] 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.[2] It is in a phase III trial as of 2023.[4]
References[edit]
- ^ Hopkins, Seth C.; Wilkinson, Scott; Corriveau, Taryn J.; Nishikawa, Hiroyuki; Nakamichi, Keiko; Loebel, Antony; Koblan, Kenneth S. (2021). "Discovery of Nonracemic Amisulpride to Maximize Benefit/Risk of 5-HT7 and D2 Receptor Antagonism for the Treatment of Mood Disorders". Clinical Pharmacology & Therapeutics. 110 (3): 808–815. doi:10.1002/cpt.2282. PMC 8453756. PMID 33961287.
- ^ a b Loebel, Antony; Koblan, Kenneth S.; Tsai, Joyce; Deng, Ling; Fava, Maurizio; Kent, Justine; Hopkins, Seth C. (1 January 2022). "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. 296: 549–558. doi:10.1016/j.jad.2021.09.109. ISSN 0165-0327. PMID 34614447. S2CID 238422271.
- ^ Wu, Jie; Kwan, Angela TH; Rhee, Taeho Greg; Ho, Roger; d’Andrea, Giacomo; Martinotti, Giovanni; Teopiz, Kayla M; Ceban, Felicia; McIntyre, Roger S (21 October 2023). "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. 16 (11): 1085–1092. doi:10.1080/17512433.2023.2274538. ISSN 1751-2433. PMID 37864424. S2CID 264378098.
- ^ "Sumitomo, Otsuka's Schizophrenia Candidate Fails Phase III Trials". BioSpace. Retrieved 9 November 2023.
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