INDICATED FOR SCHIZOPHRENIA

Loxapine is for the treatment of anxiety and aggression in patients suffering from schizophrenia or bipolar 1 disorder.

Loxapine oral film will utilize the company's proprietary VersaFilm™ technology, allowing for an improved product to offer patients significant therapeutic benefits compared to existing medications. A fast acting loxapine oral film dosage form that can be used to effectively treat acute agitation associated with schizophrenia or bipolar 1 disorder in non-institutionalized patients while reducing the risk of pulmonary problems is needed as it could substantially reduce the potential risks of violence and injury to patients and others by preventing or reducing the duration and severity of an episode of acute agitation.

IntelGenx has demonstrated in a successful pilot study that buccal absorption of the drug from the loxapine oral film results in a significantly higher bioavailability of the drug compared to oral tablets. IntelGenx is currently optimizing the film to further improve time to reach peak plasma concentrations. According to Datamonitor, sales of schizophrenia drugs across the seven major markets (the US, Japan, France, Germany, Italy, Spain, and the UK) were estimated at $5.2 billion in 2012 and by 2021, the market is forecast to grow to $6.9 billion at a compound annual growth rate (CAGR) of 3.3%.

Agitation associated with schizophrenia or bipolar mania is not uncommon, and if left untreated can rapidly escalate into physically aggressive behavior that can be potentially dangerous to the agitated individual and others. In a clinical setting agitation associated with schizophrenia and bipolar mania are often effectively managed with behavioral and psychological techniques, with unexpected acute agitation typically being treated with parenterally administered sedatives such as benzodiazepines and/or antipsychotic drugs such as olanzapine and ziprasidone.

On December 21, 2012, the U.S. Food and Drug Administration approved a loxapine product formulated into an inhaled powder for direct administration to the lungs and is indicated for the treatment of acute agitation associated with schizophrenia or bipolar 1 disorder in adults. A statistically significant reduction in agitation occurs at 2 hours, and an improvement is achieved at 10 minutes after administration. The onset of a statistically significant reduction in agitation occurs at 5 minutes. However, to mitigate the risk of bronchospasm, inhaled loxapine powder must be administered only in an enrolled healthcare facility, and only to patients that have been pre-screened to ensure they are not susceptible to pulmonary issues.

Loxapine oral capsules have been available for the treatment of schizophrenia since about 1988, with the typical dosage being 30-50 mg twice daily. The loxapine capsules are unsuitable for treating acute agitation associated with schizophrenia or bipolar 1 disorder because onset of therapeutic relief occurs approximately 20-30 minutes after administration. Such delayed onset of relief would significantly increase the risk of injury to a person being treated and those administering treatment.

INT0036 is indicated for the treatment of schizophrenia and utilizes the company's proprietary VersaFilm™ technology, allowing for an improved product to offer patients significant therapeutic benefits compared to existing medications. IntelGenx has demonstrated in a successful pilot study that buccal absorption of the drug from the INT0036 film product results in a significantly higher bioavailability of the drug compared to oral tablets. According to Datamonitor, sales of schizophrenia drugs across the seven major markets (the US, Japan, France, Germany, Italy, Spain, and the UK) were estimated at $5.2 billion in 2012 and by 2021, the market is forecast to grow to $6.9 billion at a compound annual growth rate (CAGR) of 3.3%. IntelGenx is currently looking for a partnership or alliance opportunity to complete development and commercialize INT0036.