Treating extrapyramtdal syndrome using trapidil
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Publication Number
US-11628170-B2
Publication Date
2023-04-18
Expiration Date
Abstract
Disclosed herein are methods, pharmaceutical combinations, or kits for the prevention or treatment of extrapyramidal syndromes, for example, dyskinesia, dystonia, akathisia, or drug-induced Parkinsonism, with the administration of a therapeutic effective amount of Trapidil, a derivative, a metabolite, a prodrug, an analog, or a pharmaceutically acceptable salt thereof.
Core Innovation
The invention relates to Trapidil, and Trapidil derivatives, metabolites, prodrugs, analogs, or pharmaceutically acceptable salts, for prevention and treatment of extrapyramidal syndromes. The disclosed syndrome scope includes dyskinesia, dystonia, akathisia, tardive dyskinesia, and drug-induced Parkinsonism, and the chemical identification for Trapidil is given as N,N-diethyl-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine.
The document further discloses combination therapy using Trapidil together with levodopa and additional therapeutic agents. Representative Trapidil derivatives and metabolites include AR12455/12456/12460/12463-12465/12560/12565, desethyl-trapidil, TP-1, and TP-2, together with pharmaceutically acceptable salt forms.
In addition to the therapeutic use, the document discloses a transcriptomic marker panel associated with extrapyramidal syndromes, including markers tied to ERK/MAPK pathway-associated gene expression. The disclosed marker set includes FOSL2, JUN, JUND, ATF3, SREBF2, INSIG1, MVK, MVD, LDLR, HMGCR, DUSP14, SQSTM1, IER3, and cell-cycle/apoptosis markers including CDKN1A, MYC, and BCL2.
Claims Coverage
The provided content includes one independent claim. The claim covers a combination therapy method for treating Parkinson’s disease using Trapidil, including a specified derivative or metabolite or a pharmaceutically acceptable salt, together with levodopa, with a stated Trapidil dose range and specific derivative/metabolite selections.
Trapidil and levodopa combination therapy for Parkinson’s disease
A combination therapy method for treating Parkinson’s disease in a subject in need thereof by administering Trapidil, a derivative, a metabolite, or a pharmaceutically acceptable salt thereof, and levodopa.
Specific Trapidil derivative and Trapidil metabolite selection
The derivative of Trapidil is 5-piperidino-7-(N-(n-amyl)-N-(beta-hydroxyethyl)-amino)-s-triazolo(1,5-a)pyrimidine and the metabolite of Trapidil is TP-1.
Trapidil dose range in the combination
Trapidil is administered in a dose of about 50 mg to about 300 mg.
The core coverage is a Parkinson’s-disease combination therapy method comprising Trapidil, with a specified derivative form and TP-1 as the metabolite option or a pharmaceutically acceptable salt, administered together with levodopa, with Trapidil dosed in about 50 mg to about 300 mg.
Stated Advantages
Treating Parkinson’s disease in the subject by administering Trapidil or a derivative, metabolite, or pharmaceutically acceptable salt thereof together with levodopa.
Documented Applications
Prevention and treatment of extrapyramidal syndromes, including dyskinesia, dystonia, akathisia, tardive dyskinesia, and drug-induced Parkinsonism.
Treatment of Parkinson’s disease in a subject in need thereof using Trapidil in combination with levodopa.
Clinical study design for tardive dyskinesia described as randomized and double blind.
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