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. 2020 Oct 28;16:2499–2509. doi: 10.2147/NDT.S263424

Table 3.

Serotonin 6 and 7 Receptors Antagonist Under Clinical Trial

Compound Indication Clinical Trial Phase Clinical Data and Status Reference
Idalopirdine Schizophrenia Phase II 5-HT6R Antagonist Well tolerated in both dose ranging and a multi-dose cohort [93]
ABT-354 Schizophrenia and Alzheimer’s Phase III 5-HT6R antagonist Tested in phase I and II clinical trials [88]
Lu AE58054 Schizophrenia and Alzheimer’s Phase II 5-HT6R antagonist The primary outcome measure was efficacy effect of treatment based on the Positive and Negative Syndrome Scale total score [88,94]
AVN-211 Schizophrenia Phase II 5-HT6R antagonist Significant improvement of total Positive and Negative Syndrome in female patients [95,96]
SYN-114 Schizophrenia and Alzheimer’s Phase I 5-HT6R antagonist This product has completed phase I single and multiple ascending dose studies [88]
PRX-07034 Schizophrenia Phase II 5-HT6R antagonist No recent reports of development identified for phase I development [97]
SGS-518 Schizophrenia Phase II 5-HT6R antagonist Safe and well tolerated by patients with cognitive improvement. Terminated because of lack of efficacy [32]
LY-483,518 Schizophrenia Phase II 5-HT6R antagonist No recent reports of development identified for phase II development in schizophrenia [89,98]
SUVN-502 Schizophrenia Phase I 5-HT6R antagonist Satisfactory result and passed for phase II [65,99]
RP5063 (RP5000) Schizophrenia Phase III 5-HT 6 and 7 receptor antagonist Effective, well tolerated, and 100 mg oral dose is the maximum tolerated dose [100]
Aripiprazole controlled release Schizophrenia Phase I 5-HT7R antagonist No recent reports of development identified for phase I development in schizophrenia in Europe [101]