PRODUCTS

SUBLINGUAL APOMORPHINE

INTRODUCTION

In May 2006, Amarin acquired the global rights to a novel sublingual (under the tongue) formulation of apomorphine for the treatment of “off” episodes in patients with advanced Parkinson’s disease.

“Off” episodes develop in the later stages of Parkinson’s disease where many patients, despite continuing to take their medication, experience periods when they lose the ability to move. This is termed bradykinesia (slowed movement) or akinesia (inability to move). These “off” episodes, which typically occur 3 to 4 times per day, can also be associated with other symptoms such as muscle pain, anxiety and panic.

Apomorphine is one of the most potent medications for treating Parkinson’s disease, in particular “off” episodes in patients with advanced symptoms. Apomorphine is classified as a dopamine agonist. Dopamine agonists imitate the action of dopamine rather than replace it in the way other trademarks do. Dopamine is known as a neurotransmitter (chemical messenger). It enables the brain to transmit signals from one area to another, which allows the brain to control and co-ordinate body movements.

“Off” episodes are estimated to affect approximately 100,000 late stage Parkinson’s disease patients in the US, with a similar number in Europe, and as such represents an orphan indication.

Intellectual Property

Current IP for this product comprises a patent filing which covers the novel formulation of apomorphine. If granted, 20 years of protection will follow providing protection until 2025.

Opportunity – unmet Need

Apomorphine has been available in subcutaneous injection form in Europe for a number of years and more recently in the US. It is believed that the use of subcutaneous apomorphine is limited by site pain and local swelling caused by the needle and level of acidity, which is exacerbated by the need for many patients to inject multiple times per day which in many cases must be administered by a caregiver or family member.

Apomorphine is currently not available in oral form for a rescue treatment in Parkinson’s disease as it is extensively broken down during its passage from the gut through the liver resulting in very low blood concentrations.

Amarin's novel formulation aims to provide rapid absorption of apomorphine directly into the bloodstream after sublingual administration, thereby avoiding the problem of breakdown in the liver. Also, this novel formulation would offer patients a more user friendly and pain free alternative to the currently available formulation of apomorphine and could result in higher rates of utilization.

DEVELOPMENT TO DATE

Amarin has successfully progressed its sublingual apomorphine candidate through a series of Phase I pharmacokinetic studies to prove the concept and to optimize the formulation. The results to date show that Amarin’s sublingual formulation has the same speed of absorption as the injection formulation and a profile that supports its further development for the intended indication.

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