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Methods and compositions for treatment of disorders ameliorated by muscarinic receptor activation

a technology of muscarinic receptor and composition, which is applied in the direction of drug composition, contraceptive device, biocide, etc., can solve the problems of severe side effects, limited efficacy of both typical and atypical antipsychotics, and increased risk of mortality for patients with schizophrenia. , to achieve the effect of reducing side effects and achieving a higher maximum tolerated dos

Inactive Publication Date: 2014-04-10
PURETECH VENTURES +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The invention relates to the use of an Inhibitor to alleviate the side effects of an Activator. In a first embodiment, the Inhibitor is used to reduce the side effects of the Activator. In a second embodiment, the Inhibitor allows for a higher maximum tolerated dose of the Activator.

Problems solved by technology

Patients who suffer from schizophrenia both experience a major decline in quality of life and are at increased risk for mortality due to a number of factors, such as an increased suicide rate.
The cost of schizophrenia to society is also significant as sufferers of schizophrenia are much more likely to be incarcerated, homeless or unemployed.
The first generation of antipsychotics are generally known as “typical antipsychotics” while newer antipsychotics are generally called “atypical antipsychotics.” Both typical and atypical antipsychotics have limited efficacy and severe side effects.
The side effect profile of current antipsychotics further decreases compliance in a patient population that is already frequently non-compliant.
However, Syed et al. reported in a 2008 review that there is inadequate data to guide clinical practice.
However, because xanomeline also bound to subtypes of receptors other than M1, a number of various serious side effects were observed including GI side effects, cardiac side effects and problems with hyper-salivation.
To date, nobody has been able to harness the approach of employing muscarinic agonists because of the side effects associated with the agents' binding certain muscarinic receptor subtypes.

Method used

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  • Methods and compositions for treatment of disorders ameliorated by muscarinic receptor activation

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0127]In one example, the invention is a single capsule formulation containing 75 milligrams of xanomeline and 20 milligrams of trospium chloride. The capsule consists of a gelatin shell surrounding a fill material composed of the active compounds, a vehicle, a surfactant and a modifier. The vehicle is polyethylene glycol with a molecular weight in the range of from 500 to 10,000 Daltons and is 10% of the fill material by weight. The surfactant is polysorbate 80 and represents 0.1% by weight of the fill material. The modifier is fumed silica present at 0.25% by weight of the fill material. The total fill material represents 50% of the total capsule weight and the gelatin shell is 50% of the total capsule weight.

example 2

[0128]A second formulation is the capsule in Example 1 with an additional outer controlled release layer comprising an enteric material (material that is relatively insoluble in the acidic environment of the stomach). There are a variety of enteric materials known to one skilled in the art. For this specific formulation we use hydroxyethylcellulose which would compose 20% of total capsule weight.

example 3

[0129]A third example is a formulation prepared as in Example 2, with the capsule containing 225 mg of xanomeline and 60 milligrams of trospium chloride.

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Abstract

Methods for the treatment of CNS disorders using combinations of muscarinic activators and inhibitors, and medicaments comprising muscarinic activators and inhibitors.

Description

FIELD OF INVENTION[0001]The present invention relates to: 1) A method of using a combination of one or more muscarinic agonists and one or more muscarinic antagonists for treatment of diseases that are ameliorated by activation of muscarinic receptors (e.g., schizophrenia and related disorders); 2) A medicament comprising one or more muscarinic agonists and one or more muscarinic antagonists.BACKGROUND OF THE INVENTION[0002]The acetylcholine neurotransmitter system plays a significant role in a variety of central nervous system (CNS) and peripheral functions. Acetylcholine signaling occurs through two different families of receptors: nicotinic receptors and muscarinic receptors. Muscarinic cholinergic receptors are G-protein coupled receptors with five different receptor subtypes (M1-M5) (Raedler et al. American Journal of Psychiatry. 160: 118. 2003), each of which are found in the CNS but have different tissue distributions. Activation of the muscarinic system through use of muscar...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/4439A61K31/46A61K31/4725
CPCA61K31/4439A61K31/46A61K31/4725A61K9/4858A61K9/4891A61K47/38A61K47/26A61K9/20A61P25/00A61P25/14A61P25/28A61P25/18A61P25/26A61P25/24A61P25/30A61K31/138A61K2300/00A61K31/222A61K31/4025A61K31/4178A61K31/438A61K31/44A61K45/06A61K9/48A61K9/4825A61K9/485A61K9/4866
Inventor ELENKO, ERICMILLER, ANDREW C.MURRAY, III, PHILIP E.
Owner PURETECH VENTURES
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