An adenosine A2A receptor antagonist
Tozadenant (SYN115) is an orally active, selective adenosine A2A receptor antagonist.
In animal models of Parkinson’s disease, tozadenant improves motor neuron function.
Tozadenant (60 mg twice daily) was not associated with a signi cant reduction in o -time, and tozadenant (240 mg twice daily) was associated with an increased rate of discontinuation because of adverse events (17 of 84 patients [20%]). Tozadenant at dose of 120 or 180 mg twice daily was e ective at reducing o -time and was generally well tolerated. Further investigation of tozadenant treatment in phase 3 trials is guaranteed. Perfusion MRI showed that tozadenant induced highly signi cant suppressed in regional cerebral blood ow, with the most important decreases occurring in bilateral thalami.
Reference:
[1].Hauser RA, Olanow CW, Kieburtz KD et al.? Tozadenant (SYN115) in patients with Parkinson's disease who have motor fluctuations on levodopa: a phase 2b, double-blind, randomised trial. Lancet Neurol. 2014 Aug;13(8):767-76
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| Human experiment [1]: | |
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Patients |
Patients with Parkinson’s disease. |
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Dosage form |
60, 120, 180, or 240 mg twice daily for 12 weeks. |
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Applications |
Tozadenant increases mean daily total on-time and improved total UPDRS scores for parts I-III in the combined tozadenant 120 mg twice-daily and 180 mg twice-daily group and in the 120 mg twice-daily group. Also, tozadenant significantly improved CGI-S and CGI-I scores. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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参考文献: [1]. Hauser RA, Olanow CW, Kieburtz KD, et al. Tozadenant (SYN115) in patients with Parkinson's disease who have motor fluctuations on levodopa: a phase 2b, double-blind, randomised trial. Lancet Neurol,2014, 13(8): 767-776. |
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