Novel lipophilic prodrugs of apomorphine having high affinity to chylomicrons with intestinal lymphatic absorption potential

Novel lipophilic prodrugs of apomorphine having high affinity to chylomicrons  with intestinal lymphatic absorption potential

 

Categories	Drug delivery, Oral bioavailability, Apomorphines
Development Stage	Animal trials were performed
Patent Status	Patent pending
Market Size	The market of drugs dedicated to treating neurological disorders, including Alzheimer's and Parkinson's diseases, is a multi-billion market

Highlights

• Apomorphine is being used to treat a variety of neurological disorders resulting from dopamine imbalances in the brain, including Alzheimer's and Parkinson's diseases.
• Apomorphine's oral bioavailability is extremely low.

The Innovation

• The invention overcomes apomorphine's low oral bioavailability by using novel lipophilic prodrugs of apomorphine having high affinity to chylomicrons (lipoproteins created by the absorptive cells of the small intestine) with intestinal lymphatic absorption potential.
• The invention enables administering the novel lipophilic prodrugs of apomorphine orally with the appropriate lipid based formulation.

Key Features

• Well known and widely used apomorphines have extremely low oral bioavailability.
• The invention enables oral delivery of apomorphine lipophilic prodrugs and derivatives.

Development Milestones

• The lipophilic prodrugs of apomorphine were synthesized.
• The intestinal lymphatic absorption potential and total bioavailability of the lipophilic prodrugs of apomorphine were assessed.
• An animal model revealed improved lymphatic bioavailability correlated highly with the uptake by chylomicrons.

The Opportunity

• The number of Alzheimer's patients is expected to reach 21 millions in 2010. Pakinson's disease, as the second most common neurodegenerative disorder after Alzheimer's disease, affects nearly 2% of people over the age of 65.

Early Stage

Patent pending