Treating extrapyramidal syndrome using trapidil

Inventors

BORDBAR, Aarash

Assignees

Sinopia Biosciences Inc

Interested in licensing this patent?

MTEC can help explore whether this patent might be available for licensing for your application.

Publication Number

US-12268691-B2

Patent

Publication Date

2025-04-08

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 a method for treating or preventing levodopa-induced dyskinesia in a subject by administering to the subject a Trapidil compound or a pharmaceutically acceptable salt thereof. The subject matter is specifically directed to levodopa-induced dyskinesia as the therapeutic target.

The disclosure includes Trapidil derivatives, metabolites, prodrugs, analogs, and pharmaceutically acceptable salts, with specific named forms such as AR12455, AR12456, AR12460, AR12463, AR12464, AR12465, and AR12565, and metabolites including desethyl-trapidil and TP1/TP2. It also includes a transcriptomic marker panel associated with ERK and related pathway modulation, including AP-1/ERK and cholesterol synthesis and cell-cycle markers such as FOSL2, JUN/JUND, ATF3, SREBF2, INSIG1, ERK, MYC, and BCL2.

The partial document further states a dosing and administration framework for Trapidil, including oral daily dose ranges, single versus multiple daily dosing, and intravenous or subcutaneous administration. It also describes combination therapy in which Trapidil is administered with additional therapeutic agents, including levodopa, with timing described as simultaneous or sequential and with fixed versus separate dosage forms.

Claims Coverage

The consolidated claim coverage centers on one independent claim directed to treating or preventing levodopa-induced dyskinesia by administering a Trapidil compound or a pharmaceutically acceptable salt, with several dependent refinements adding inventive features such as specific Trapidil derivatives, timing relative to levodopa, symptom characterization, daily dose range, and dosing frequency.

Trapidil administration for levodopa-induced dyskinesia

A method for treating or preventing levodopa-induced dyskinesia in a subject by administering to the subject a Trapidil compound or a pharmaceutically acceptable salt thereof.

Trapidil derivative selection from AR12455/AR12456/AR12460/AR12463/AR12464/AR12465/AR12565

The method uses a Trapidil derivative selected from AR12455, AR12456, AR12460, AR12463, AR12464, AR12465, or AR12565.

Timing prior to levodopa dosing

Administering a Trapidil compound or a pharmaceutically acceptable salt prior to administering levodopa.

Dyskinesia characterized by specified symptom set

Levodopa-induced dyskinesia is characterized by one or more specified symptoms including hyperkinetic movements, chorea, dystonia, involuntary muscle movements, or athetosis.

Daily dose range constraint

A daily dose of the Trapidil compound or a pharmaceutically acceptable salt ranging from about 50 mg/day to about 1,000 mg/day.

Administration frequency constraint

Administering a dose of the Trapidil compound or a pharmaceutically acceptable salt 1 to 5 times per day.

Coverage is centered on administering Trapidil or a pharmaceutically acceptable salt to treat or prevent levodopa-induced dyskinesia, with further constraints on selected Trapidil derivatives, timing relative to levodopa, symptom characterization, daily dose range, and dosing frequency.

Stated Advantages

Treating or preventing levodopa-induced dyskinesia in a subject.

Documented Applications

Use of Trapidil administration in a method for treating or preventing levodopa-induced dyskinesia in a subject.

Transcriptomic marker panel use for monitoring and selection in relation to Trapidil-associated modulation of the ERK pathway, including AP-1/ERK, cholesterol synthesis, and cell-cycle markers.

Treating or preventing extrapyramidal syndromes including dyskinesia, dystonia, akathisia, and drug-induced Parkinsonism.

JOIN OUR MAILING LIST

Stay Connected with MTEC

Keep up with active and upcoming solicitations, MTEC news and other valuable information.