Vortioxetine (Lu AA21004) HBr
Molecular Weight(MW): 379.36
Vortioxetine (Lu AA21004) is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with IC50 of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.
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|Description||Vortioxetine (Lu AA21004) is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with IC50 of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.|
|Features||A multimodal antidepressant.|
Lu-AA21004 inhibits recombinant human CYP1A2, CYP2C9, CYP2D6 and CYP3A4 with IC50 of 40 μM, 39 μM, 9.8 μM and 10 μM, respectively.  Lu AA21004 is a partial h5-HT1B receptor agonist with EC50 of 460 nM and intrinsic activity of 22% using a whole-cell cAMP-based assay. Lu AA21004 binds to the r5-HT7 receptor with a Ki value of 200 nM and is a functional antagonist at the r5-HT7 receptor with an IC50 of 2 μM in an in vitro whole-cell cAMP assay. 
|In vivo||For Lu-AA21004 the hepatic clearances and oral bioavailabilities in rats are found to be 7.1 (L/h)/kg and 16%. Lu-AA21004 (2.5 mg/kg, 5 mg/kg, or 10 mg/kg sc) increases the extracellular levels of 5-HT in the ventral hippocampus in conscious rats. Lu-AA21004 (5 mg/kg, or 10 mg/kg sc) also results in significantly higher basal levels of 5-HT in the medial prefrontal cortex (mPFC) after 3 days of treatment. Lu-AA21004 occupies SERT by 43% and 57% after 3 days of treatment with 5 mg/kg or 10 mg/kg in the rat medial prefrontal cortex.  Lu AA21004 dose-dependent occupies 5-HT1B receptor and the SERT with ED50 of 3.2 mg/kg and 0.4 mg/kg in rats one hour after subcutaneous administration. Lu AA21004 affects the Bezold-Jarisch reflex in the rat dose dependently, inhibiting transient bradycardia with ED50 of 0.11 mg/kg. Lu AA21004 (2.5-10.0 mg/kg s.c.) increases extracellular levels of 5-HT, DA, and NA in the medial prefrontal cortex and in the ventral hippocampus in rats. Lu AA21004 (5 mg/kg s.c.) increases in the extracellular levels of 5-HT (200%) in the ventral hippocampus of rats with 41% occupancy at the SERT. Lu AA21004 (7.8 mg/kg s.c.) significantly decreases the immobility time in the FSL rats but not in the FRL rats. Lu AA21004 (8.0 mg/kg p.o.) produces an increase in social interaction as well as a small, but significant, increase in locomotor activity in rats. Lu AA21004 (7.9 mg/kg s.c.) shows a dose-dependent anxiolytic-like effect in the conditioned fear assay in rats.  Vortioxetine (10 mg/kg) significantly increases freezing 60 min before acquisition in male Sprague-Dawley rats, suggesting enhanced contextual memory formation during acquisition and/or consolidation. Vortioxetine (5 mg/kg) also causes increased freezing rates during retention, an effect that reached statistical significance by post hoc tests. Vortioxetine (2.5 mg/kg or 5 mg/kg) prior to acquisition shows average exploration times of 29s and 33s for the novel object, respectively. Vortioxetine (10 mg/kg) significantly reduces nociception in rats, assessed as increased paw withdrawal latency. Vortioxetine at 5 and 10 mg/kg increases the levels of ACh to 224% and 204% of baseline 20 min after injection. |
|In vitro||DMSO||76 mg/mL (200.33 mM)|
|Ethanol||17 mg/mL (44.81 mM)|
|In vivo||Add solvents individually and in order:
15% Captisol, pH 9
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03053362||Not yet recruiting||Major Depressive Disorder|Cognitive Change||Brain and Cognition Discovery Foundation||March 2017||Phase 2|Phase 3|
|NCT02972632||Recruiting||Major Depressive Disorder||Takeda||December 2016||Phase 4|
|NCT02637895||Recruiting||Post-Traumatic Stress Disorder||University of Miami|Takeda|Emory University||December 2016||Phase 4|
|NCT02749721||Recruiting||Major Depressive Disorder||Rush University Medical Center|Takeda Pharmaceuticals North America, Inc.|ElMindA Ltd||December 2016||Phase 4|
|NCT02969876||Recruiting||Depressive Disorder|Major Depression|Depression|Depression, Unipolar||Massachusetts General Hospital|Takeda||November 2016||Phase 4|
|NCT02932904||Recruiting||Healthy Volunteers||Takeda||November 2016||Phase 4|
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