Yissum - Research Development Company of the Hebrew University

L-DOPA Amide Derivatives for Treating Parkinson’s Disease

Posted by Yissum - Research Development Company of the Hebrew UniversityResponsive · Innovative Products and Technologies · Israel

Summary of the technology

"Slow release L-DOPA analogs LDA and NALDA, for the treatment of Parkinson’s disease and other related indications. LDA and NALDA are highly lipophyllic and penetrate the brain very efficiently crossing the cell membrane. This property increases the bioavailability of L-DOPA in the brain, and allows smaller amounts to be used compared to that of L-DOPA. The new carriers become substrates for the aromatic amino acid decarboxylase (AADC) only in vivo. This property could eliminate the use of AADC inhibitor (carbidopa) from the treatment of PD patients. The slow conversion of these carriers in the brain to L-DOPA represents a slow release mode of drug administration. A gradual formation of L-DOPA,
would mimic the advantages of a constant and gradual level of dopamine, typical of slow drug medication."

Project ID : 7-2006-138

Description of the technology

Novel treatment for Parkinson’s disease overcomes “on-off” phenomenon

Categories

Parkinson’s disease, L-dopa, L-dopa amide

Development Stage

Concept proven, in vivo human models

Patent Status

Pending patent application in, Europe, US and Israel (PCT publication № WO2004/069146)

Highlights

  • Increases the endogenous level of dopamine to alleviate the motor complications of Parkinson’s disease and to delay the onset of the symptoms from the dramatic decrease in dopamine

  • Formulated for buccal, oral, sub-lingual, parenteral, intranasal, intramuscular, intravenous, subcutaneous, intraduodenal or rectal administration

Our Innovation

  • Provides a pharmaceutical preparation for the treatment of patients suffering from PD comprising a composition of L-Dopamide

  • A water-soluble compound could be applied f for rescue therapy. An advantage over the insoluble L-DOPA

  • Involves an essential structural change to make L-DOPA more soluble and resistant to DOPA Decarboxylase

  • Administrable without Carbidopa due to resistance to DOPA-decarboxylase

  • L-Dopamide is slowly hydrolyzed to L-DOPA because it is resistance to DOPA decarboxylase

  • Slow release addresses the on/off phenomenon of Parkinson’s

  • Degrades to natural products

The Opportunity

Addresses the need for more effective therapy for Parkinson’s disease using a more sustained level of dopamine

Oral results

Oral application in animal model showed longer duration > 40% over L- DOPA.

  • Higher efficiency as a proof of concept in experiments made side by side with L-DOPA

  • PK studies available

Development Milestones

Ready for toxicology studies.

Project manager

Shoshana Keynan
VP, Head of Business Development, Healthcare

Project researchers

Daphne Atlas
HUJI, Faculty of Science
The Alexander Silberman Institute for Life Sciences

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About Yissum - Research Development Company of the Hebrew University

Technology Transfer Office from Israel

Yissum Research Development Company of the Hebrew University of Jerusalem Ltd. Founded in 1964 to protect and commercialize the Hebrew University’s intellectual property. Ranked among the top technology transfer companies, Yissum has registered over 8,900 patents covering 2,500 inventions; has licensed out 800 technologies and has spun-off 90 companies. Products that are based on Hebrew University technologies and were commercialized by Yissum generate today over $2 Billion in annual sales.

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