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Publication Number
US-11478476-B2
Publication Date
2022-10-25
Expiration Date
Abstract
The present invention is directed to a composition comprising a buspirone metabolite, alone or in combination with a second active ingredient, for use in the treatment of movement disorders.
Core Innovation
The disclosed subject matter relates to treating movement disorders, in particular L-DOPA induced dyskinesia (LID) and tardive dyskinesia (TD), using buspirone metabolites. The disclosure emphasizes 6-hydroxybuspirone (6-OH-Busp) and also refers to other buspirone metabolites. The rationale presented is that parent buspirone has limited bioavailability and a risk of serotonergic toxicity at higher doses, while the metabolites can maintain efficacy and potentially improve exposure and reduce serotonergic exposure.
The disclosure further characterizes combination therapy in which buspirone metabolites, including 6-OH-Busp, are used in combination with a second centrally acting active ingredient. The second active ingredient is described as including 5-HT1B/5-HT1D/5-HT1F agonists, including triptans, glutamate neurotransmission modulators, including NMDA/AMPA/kainate receptor antagonists and mGluR modulators, inhibitors of presynaptic glutamate release, and neuronal ion-channel antagonists, including calcium, potassium, and sodium channel antagonists and KCNQ/Kv7.2-7.5 activators.
The disclosure reports pharmacology and in vivo model results related to abnormal involuntary movements using endpoints such as AIMs and VCM. It is reported that 6-OH-Busp and certain combinations attenuate abnormal involuntary movements without obvious behavioral side effects. A PD stepping-test result is also described, suggesting that 6-OH-Busp does not impair L-DOPA efficacy.
Claims Coverage
The provided set contains one independent claim. The independent claim covers treatment of L-DOPA induced dyskinesia or tardive dyskinesia by administering a pharmaceutical composition containing 6-hydroxybuspirone, with stereochemical selection of the 6-OH-Busp form as a key inventive feature.
Treating L-DOPA induced dyskinesia or tardive dyskinesia with 6-hydroxybuspirone composition
A method comprising administering to a subject in need thereof a pharmaceutical composition comprising 6-hydroxybuspirone or a pharmaceutically acceptable salt or ester thereof, for treating L-DOPA induced dyskinesia or tardive dyskinesia.
Stereochemical selection of 6-hydroxybuspirone
The method wherein 6-OH-Busp is selected from the racemate of 6-OH-Busp, the S-form of 6-OH-Busp, or the R-form of 6-OH-Busp.
Overall, the claim coverage focuses on administering 6-hydroxybuspirone, or a pharmaceutically acceptable salt or ester, for treating LID or TD, with explicit selection of the racemate, S-form, or R-form of 6-OH-Busp.
Stated Advantages
Potentially improve exposure and reduce serotonergic exposure.
Attenuate abnormal involuntary movements without obvious behavioral side effects.
Does not impair L-DOPA efficacy.
Documented Applications
Treating L-DOPA induced dyskinesia (LID).
Treating tardive dyskinesia (TD).
Combination therapy for movement disorders using buspirone metabolites with a second centrally acting active ingredient.
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