Yissum - Research Development Company of the Hebrew University

Platform Technology for Converting Peptides for Oral Availability

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

Summary of the technology

Synthesis of Cyclic Peptidomimetics and their Prodrugs for oral delivery
Project ID : 6-2017-4503

Yissum - Research Development Company of the Hebrew University

Description of the technology

Keywords

Platform technology, Intestinal permeability, Lipophilic Prodrug Charge Masking, peptides, oral bioavailability

Current development stage

TRL4 - POC & Safety of candidate drug formulation is demonstrated in defined animal model

Application

  • Peptides are key players in a variety of physiological and pathological processes and play very important roles in modulating various cell functions.
  • One of the most important challenges developing peptide drugs is the lack of appropriate physicochemical properties that enables the absorption through biological membranes.
  • Currently, most peptide drugs are administered parentally due to their poor intestinal permeability attributed to their hydrophilicity mainly due to charged groups.

Our Innovation

  • A novel method called Lipophilic Prodrug Charge Masking (LPCM) that enhance the intestinal permeability and the oral bioavailability of charged peptides
  • Significantly increased permeability rate of most peptides compared to the respective unmasked peptides.
  • Brings into the systemic blood circulation the parent drug.
  • Converts active peptides to orally therapeutic treatment

Technology

  • The major challenges in peptide membrane permeability via passive diffusion include the peptide’s high polarity, charge and hydrogen bond potential.
  • In the LPCM method, synthetic methods for the conversion of peptides, peptidomimetic and peptide drugs into their lipophilic prodrug were demonstrated.
  • Charged masked peptide prodrugs were synthesized and masked with urethane/ ester type lipophilic pro-moiety.The prodrug enhanced intestinal permeability allowed its absorption to the blood stream where esterases removed the pro-moiety to regenerate the original peptides.
  • The LPCM method shifts the mechanism of intestinal permeability of the charged peptides from para-cellular to trans-cellular pathway of their lipophilic prodrug

Fig. 1: Principle of the LPCM method

Opportunity

  • New oral peptides/peptidomimetics medications
  • Chronic treatment with good patient compliance
  • Currently being studiedand tested for RGD containing peptide

Project manager

Shani Bullock
VP, Business Development, Healthcare

Project researchers

Chaim Gilon
HUJI, Faculty of Science
The Institute of Chemistry

Amnon Hoffman
HUJI, School of Medicine - IMRIC
School of Pharmacy- Institute for Drug Research

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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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