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. 2017 Mar 29;8(19):32101–32116. doi: 10.18632/oncotarget.16646

Table 2. FDA-approved antidepressants inhibit sphere formation by HCC1954 breast tumor cells.

Drug Approved Drug Class Molecular Target(s) IC50
Clomipramine Tricyclic Antidepressant SERT, 5-HT2A, 2C, 3, 6, 7 1.9
Doxepin Tricyclic Antidepressant SERT, 5-HT1A, 2A, 2C, 6 4.1
Latrepirdine Tricyclic Antihistamine 5-HT2C, 5A, 6 4.2
Cyproheptadine Tricyclic Antihistamine 5-HT1A, 2A, 2B, 2C, 3, 6, 7 6.0
Mianserin Tetracyclic Antidepressant 5-HT1F, 2A, 2B, 2C, 6, 7 12.5
Ziprasidone Atypical Antipsychotic SERT, 5-HT1A, 1B, 1D, 2A, 2C, 6, 7 0.8
Asenapine Atypical Antipsychotic 5-HT1A, 1B, 2A, 2B, 2C, 5A, 6, 7 7.5
Vortioxetine Selective Serotonin Reuptake Inhibitor SERT, 5-HT1A, 1B, 1D, 3A, 7 1.1
Vilazodone Selective Serotonin Reuptake Inhibitor SERT, 5-HT1A 1.6
Fluoxetine Selective Serotonin Reuptake Inhibitor SERT, 5-HT2A, 2C 3.4
Paroxetine Selective Serotonin Reuptake Inhibitor SERT 2.7
Sertraline Selective Serotonin Reuptake Inhibitor SERT 1.1

HCC1954 tumorspheres were grown in the presence of different FDA-approved serotonergic antidepressants and their effect on sphere formation monitored. All the antidepressants reduced sphere formation in a dose-dependent fashion. IC50 values (listed in μM) were calculated using Graphpad Prism 6. The IC50 values of the drugs were determined in two biological experiments.