A patent has been issued to Intranasal Technology for the nasally delivered sedative lorazepam. The patent entails a complete product concept that includes the route of administration, delivery device and formulation.

ITI holds a worldwide exclusive license to market the lorazepam delivery system and intends to sublicense the product to marketing partners. ITI has filed a continuation-in-part to have other benzodiazepines, such as midazolam and diazepam, added to the protected intellectual property.

The approval of the patent is a milestone in ITI's strategy to apply innovative nasal drug delivery technology to off-patent drugs, new chemical entities, maturing and generic products. The Company's objective is to offer safe and viable alternatives to oral, intramuscular and intravenous drug delivery systems.

"Based on a review of the medical literature, it is apparent physicians have desired a rapidly absorbed, noninjectable delivery alternative for benzodiazepines," Dr. Wermeling commented. "The nasal lorazepam formulation is an example of ITI's ability to address an unmet medical need. ITI looks forward to co-development and licensing this technology to interested pharmaceutical marketing partners."

The U.S. Food and Drug Administration (FDA) has approved lorazepam to treat anxiety-related disorders and induce sedation, and it is currently marketed in injectable and tablet forms. ITI believes that companies marketing these preparations have not sought FDA approval to use these medications for intranasal delivery.

The FDA has accepted an Investigational New Drug Application (IND) for the intranasal lorazepam formulation that ITI is developing; it is currently in Phase 1 trials.

In outlining the object of the invention, the U.S. Patent documentation describes the new intranasal administration product as a highly accurate, reproducible and convenient delivery of one or more predetermined unit doses of lorazepam in the form of a nasal spray delivery system. The objective is to produce the relatively rapid onset of a therapeutic effect and the moderate duration of therapeutic activity, with minimal side effects and improved bioavailability, according to the documents.

Furthermore, the system's delivery method is designed to be safe and easy, producing minimal physical discomfort and anxiety to the patient, the patent documents state. The medication is to be delivered through a small, inexpensive, manually operated and disposable device, and will be prepared under aseptic conditions; no significant residue is to be left in the delivery device following administration, thus minimizing abuse potential, according to the documents.

The nasal spray unit dose consists of 1.0 mg of lorazepam using a 10 mg/mL solution. Higher strengths are possible and are being investigated.

In addition to the lorazepam patent, ITI recently acquired the rights to license a water-soluble testosterone prodrug from the same major university. While testosterone in its natural state is water-insoluble and difficult to formulate, the nasal spray testosterone prodrug product could be considered the "therapeutic equivalent" to the currently marketed forms of testosterone since the testosterone-ester is metabolized to testosterone in the bloodstream. The proposed delivery system will replace subphysiologic levels of testosterone, reduce symptoms and offer flexible doses not available in fixed-dose patches.

ITI is seeking a marketing partner for this product and will guide it through the FDA under a 505(b)(2) NDA application.

Lorazepam and the testosterone product are among 11 drug formulations ITI is developing. These include analgesic, sedative, psychotropic, antiemetic, and antipsychotic agents as well as female hormone replacement therapy. Besides lorazepam, the FDA has accepted three other INDs; two compounds are in Phase 2/3 clinical trials, the other is in Phase 1.

ITI has also filed two additional patent requests in the United States for new intranasal formulations and the accompanying technology.

Intranasal Technology is a development-stage pharmaceutical and drug delivery company capitalizing on the advantages of administering prescription drugs through the nasal cavity for systemic delivery.