Treating extrapyramidal syndrome using trapidil
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Publication Number
US-10350212-B2
Publication Date
2019-07-16
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 provides a combination therapy method for treating or preventing a movement disorder in a subject in need thereof. The method comprises administering to the subject a therapeutically effective combination of Trapidil, a derivative, a metabolite, or a pharmaceutically acceptable salt thereof, together with levodopa. In this way, the movement disorder is treated or prevented in the subject.
The disclosure identifies Trapidil as N,N-diethyl-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine, and describes Trapidil derivatives, Trapidil metabolites, Trapidil prodrug, Trapidil analogs, and pharmaceutically acceptable salts. It also states that Trapidil modulates extrapyramidal-syndrome related transcriptomic marker signatures and links disease biology to an extrapyramidal-syndrome transcriptomic marker panel and ERK/MAPK-pathway-associated inflammatory and upregulation signatures.
The document further describes formulations and pharmaceutical coating and formulation materials suitable for oral delivery of Trapidil, including cellulose derivatives and related coating systems with pH-dependent dissolution behavior, together with coating excipients and plasticizers, and options for controlled-release and pulsatile delivery. Oral suspension or dispersion excipients are also discussed, together with injectable, topical, rectal, and mucoadhesive compositions. It further describes therapeutic regimen timing and frequency concepts, computational identification, RNA-seq analyses, PK/PD study designs, in vivo efficacy models, and an outlined clinical trial for tardive dyskinesia.
Claims Coverage
The independent claim coverage centers on a combination-therapy method using Trapidil, a derivative, a metabolite, or a pharmaceutically acceptable salt thereof, with levodopa to treat or prevent a movement disorder, with refinements directed to delayed onset, dyskinesia-specific prevention, levodopa dose reduction, potentiation of levodopa effect, and administration as a combined dosage form.
Trapidil plus levodopa combination therapy for movement disorders
Administering a therapeutically effective combination of Trapidil, a derivative, a metabolite, or a pharmaceutically acceptable salt thereof, together with levodopa, to treat or prevent a movement disorder in a subject in need thereof.
Combination therapy delays onset of a movement disorder
The combination therapy delays the onset of a movement disorder in a subject.
Trapidil decreases the levodopa dose
Trapidil, a pharmaceutically acceptable salt thereof, decreases the levodopa dose administered to the subject compared with levodopa dosing without Trapidil or its salt.
Trapidil potentiates the effect of levodopa
Trapidil, a pharmaceutically acceptable salt thereof, potentiates the effect of levodopa.
Dyskinesia defined movement disorder with delayed onset or slowed progression
The movement disorder is dyskinesia, and the preventing effect is a delay in onset of dyskinesia or a slowing down of the progression of dyskinesia.
Combined dosage form administration
Trapidil or a pharmaceutically acceptable salt of Trapidil and levodopa are administered as a combined dosage form.
Across the inventive claim coverage, Trapidil and levodopa are used in combination to treat or prevent movement disorders, with refinements directed to delaying onset, including dyskinesia onset, slowing dyskinesia progression, potentiating levodopa effect, decreasing levodopa dose, and administration as a combined dosage form.
Stated Advantages
Delays the onset of a movement disorder.
Prevents dyskinesia by delaying onset of dyskinesia or slowing down progression of dyskinesia.
Potentiates the effect of levodopa.
Decreases the dose of levodopa administered compared with levodopa dosing without Trapidil.
Documented Applications
Treating or preventing a movement disorder in a subject in need thereof using a therapeutically effective combination of Trapidil or a derivative, metabolite, or salt and levodopa.
Preventing dyskinesia by delaying onset of dyskinesia or slowing down progression of dyskinesia.
Combination therapy that delays onset of a movement disorder.
Computational identification of Trapidil reversing an extrapyramidal syndrome transcriptomic signature and related RNA-seq analyses.
PK/PD study designs and in vivo efficacy models for tardive dyskinesia and levodopa-induced dyskinesia.
An outlined clinical trial for tardive dyskinesia.
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