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Patent for Sale:

Treatment of Alcoholism and Alcohol Dependence    

A new and comprehensive therapy of alcohol dependence and alcoholism based on a combination of two clinically used components: the amino acid tryptophan and the kynureninase inhibitor benserazide

Overview

Alcoholism and alcohol dependence is a major public health problem in the Western World and beyond. Currently, there are 14.6 million EU citizens with alcohol use disorder. There could be as many as three times this number worldwide. This represents a huge world market. Long-term management of detoxified patients is curreently managed by only 3 types of drugs, 2 of which (acamprosate and naltrexone) have a small effect size, whereas the third, disulfiram, which acts by aversion (deterrence), though superior, exerts side effects. There is thus a need for a more effective and safer alternative. The above 3 drugs address only 1 aspect of the alcohol dependence mechanism. This has led investigators to suggest combination therapy as the most likely way forward. The proposed combination of Trp and BSZ promises to fulfil all the requirements of a comprehensive therapy of alcoholism through its multi-faceted mode of action.

Primary Application of the Technology

(1) An alcohol deterence therapy
(2) Relapse preventative treatment of alcohol-dependent subjects after detoxification

Primary target market:
A huge market of well above 40 million citizens worldwide, comprising detoxified alcohol-dependent patients and risky heavy drinking subjects

Competitive Advantage

Alcohol dependence is a chronic relapsing disorder with high morbidity and mortality, yet despite its seriousness only 3 drugs are used to prevent relapse, 2 of which [acamprosate (Merck-Lipha) and naltrexone (DuPont)] show a weak efficacy, whereas the third, the aldehyde dehydrogenase (ALDH) inhibitor and alcohol-aversive drug disulfiram (generic), is superior, but exerts side effects. An ideal long-term medication for relapse prevention following detoxification of alcohol-dependent patients is one that should address all aspects of the dependence mechanism, namely the desire to drink and the anxiety, depression and agitation (hyperexcitability) experienced upon withdrawal. Each of the above 3 drugs has a single mode of action, e.g. hyperexcitability (acamprosate), opioid-mediated reward (naltrexone); ALDH inhibition (disulfiram).

Of the other drugs tested, (GHB (gamma-hydroxybutyric acid) has potential abuse and dependence properties, and SSRI’s (selective serotonin-reuptake inhibitors) are effective only in a subgroup (late-onset) of alcoholic patients. Current experimental approaches include the selective GABA-b agonist baclofen, the NMDA receptor antagonist and anticonvulsant topiramate and the serotonin 5-HT3 antagonist ondansetrone. The first 2 may be effective in early abstinence (due to their GABA effects), whereas ondansetrone may be effective only in early-onset alcoholism, contrary to expectations. In the presence of alcohol, high-dose baclofen can induce heavy sedation and a case of de novo seizure has recently been reported.

As no single drug can address all aspects of alcohol dependence, experts now favour the concept of “combination therapy as the most likely way forward in drug development in the alcoholism area.

The technology will be superior to existing competition, because it can address all aspects of the alcohol-dependence mechanism, namely: the desire to drink by (1) inducing aversion and (2) diminishing reward, and by undermining (3) anxiety, (4) depression and (5) the hyperexcitability experienced upon alcohol withdrawal. In addition, unlike disulfiram, which has serious side effects and because it and also naltrexone are contra-indicated in alcoholics with liver dysfunction, the proposed Trp-BSZ combination offers a much safer alternative and, in fact, it has already been used in a clinical trial in schizophrenia twith no reported adverse events.

The seller may consider selling these patents individually.

Patent Summary

U.S. Patent Classes & Classifications Covered in this listing:

Class 514: Drug, Bio-Affecting And Body Treating Compositions

This class is an integral part of Class 424. It includes the following subject matter, not provided for elsewhere: 1. Drug and bio-affecting compositions which are capable of: preventing, alleviating, treating, or curing abnormal and pathological conditions of the living body; maintaining, increasing, decreasing, limiting, or destroying a physiologic body function; diagnosing a physiological condition or state by an in vivo test; controlling or protecting an environment or living body by attracting, disabling, inhibiting, killing, modifying, repelling or retarding an animal or micro-organism. 2. Body treating compositions generally intended for deodorizing, protecting, adorning, or grooming a body. 3. Fermentates. Plant and animal extracts, or body fluids or material containing plant or animal cellular structure. 4. Compositions of this class defined in terms of specific structure; e.g., layered tablet, capsule. 5. Processes of using or preparing subject matter of the Class Definition.

Subclass 646: Benzene ring containing
Subclass 724: C-O-group (e.g., alcohol, alcoholate, etc.) DOAI
Subclass 727: Nitrogen containing
Subclass 728: C of C-O- group is nuclear C of a benzene ring (e.g., phenol, phenolate, etc.)
Subclass 730: Benzene ring containing
Subclass 731: C of C-O- group is nuclear C of a benzene ring (e.g., phenol, phenolate, etc.)
Subclass 741: Benzene ring containing

Class 562: Organic Compounds -- Part Of The Class 532 Series

The classes of the 532 series embrace monomeric organic carbon compounds and polymeric organic carbon compounds that are not solid synthetic resins, natural rubbers, or hydrocarbons.

Subclass 405: Aromatic
Subclass 433: Nitrogen bonded directly to carbon of organic radical (e.g., amino acids, etc.)
Subclass 458: Carboxyl, or salt thereof, bonded directly to a ring