Treatment and management of augmentation in restless legs syndrome
Inventors
Clemens, Stefan • Lallemand, Perrine
Assignees
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Publication Number
US-10751327-B2
Publication Date
2020-08-25
Expiration Date
Abstract
The present invention provides methods of treating Restless Legs Syndrome (RLS) including administering to a subject an effective amount of a dopamine D1 receptor antagonist. Compositions and kits useful for treating RLS are also provided.
Core Innovation
The disclosure describes treatment of Restless Legs Syndrome (RLS) by administering the dopamine D1 receptor antagonist ecopipam (SCH 39166). It also describes use of ecopipam with a dopamine D3 receptor agonist and, optionally, an opioid receptor agonist, including for subjects at risk for or suffering from augmentation. The supplied content does not include the background section, so a separate background problem is not explicitly described.
The proposed mechanism is that prolonged D3-receptor agonism increases D1-receptor expression and neural excitability, while D1-receptor blockade may counter this effect. The described findings report that D1 blockade restores responses toward control values and reverses increased spinal reflex amplitudes associated with prolonged D3 agonism. The disclosure also describes applications to non-opioid-dependent chronic pain, formulations, delivery systems, and kits.
Claims Coverage
The supplied relevant claims identify one independent claim. It covers treating RLS with ecopipam and includes dependent refinements concerning combination treatment, augmentation, and an opioid receptor agonist. Three principal inventive features are summarized below.
Treatment of RLS with ecopipam
The independent claim covers a method of treating RLS by administering to a subject an effective amount of the dopamine D1 receptor antagonist ecopipam (SCH 39166).
Combination treatment with a D3 receptor agonist
A dependent claim adds administration of ecopipam in combination with a D3 receptor agonist. The claims identify nafadotride, PD 128907, pramipexole, pergolide, rotigotine, or mixtures thereof as D3 receptor agonist options, and include subjects at risk for or suffering from augmentation.
Additional opioid receptor agonist
A dependent claim further adds administration of an opioid receptor agonist. The claims specify listed opioid receptor agonists or mixtures thereof.
The claims center on ecopipam treatment of RLS, with dependent claims covering combination use with a D3 receptor agonist, treatment involving augmentation, and the addition of an opioid receptor agonist.
Stated Advantages
The disclosure identifies the potential to reduce or reverse augmentation.
Documented Applications
Treatment of Restless Legs Syndrome (RLS), including subjects at risk for or suffering from augmentation.
The disclosure also describes applications to non-opioid-dependent chronic pain, formulations, delivery systems, and kits.
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