Day 2 :
Keynote: Oral peptide delivery: How to address the challenges of peptide stability in the GI tract and oral bioavailability
Time : 09:30 - 09:55
J Richard has got a PhD in Materials Science (University of Paris VI, 1987). He is Senior Vice President for Peptides Development in Ipsen. He has published 67 peer-reviewed scientific papers, 8 book chapters and 2 review editorials in various fields (colloids and interfaces, drug delivery, supercritical fluids, protein formulations, nanoparticles, sustained-release formulations . . .). He is the author of more than 120 international communications and 53 patent families.
Due to their physicochemical characteristics, peptides are usually administered through the parenteral route, often several times daily. Injectable sustained-release peptide formulations based on biodegradable microparticles or implants have been very successful to enhance patient adherence and convenience, and increase safety and efficacy. They are likely to remain a significant and important part of the new peptide products coming to the market. However, the tremendous developments in alternative non-invasive routes of delivery are likely to result in more and more peptides being delivered by the transdermal, nasal, inhalation and oral routes. The main purpose of this talk will be to analyze and compare the various oral peptide delivery technologies progressing in the clinic, discussing the pros and cons of these technologies in regards to stability, bioavailability, safety/efficacy balance, impact on CoGs and manufacturability. Case studies will be presented and discussed, examining clinical results and models for oral peptides in development addressing the key points:- Will the oral bioavailability of peptides be sufficient to fulfill the requirements of health economics and safety?- How the oral pharmacokinetics and efficacy compare versus subcutaneous injection?- Can oral peptide delivery technologies overcome food effects?
SungKyunKwan University, South Korea
Time : 09:55 - 10:20
Dr. Kang Choon Lee is Haengdan Distinguished Professor at College of Pharmacy, SungKyunKwan University, Korea. For over 35 years, Dr. Lee’s Drug Targeting Laboratory has been focused on immuno-targeting and bioconjugation of peptide and protein drugs. Dr. Lee is internationally recognized as one of the leading experts in site-specific peptide/protein PEGylation and firstly demonstrated the therapeutic potential of novel site-specific PEGylated drugs such as GLP-1 and TRAIL. He has published over 150 papers in peer-reviewed journals and served as an invited speaker at many international conferences. Dr. Lee is an inventor on more than 20 patents related to specific bioconjugation and PEGylation of peptide/protein drugs. Dr. Lee is honored as a Fellow of the American Association of Pharmaceutical Scientists (AAPS) in 2003. He currently serves on the editorial advisory board of many international scientific journals. For the clinically translating and commercializing site-specific engineered peptide/protein drugs developed by his laboratory, he founded D&D PharmaTech, Korea and also co-founded and serves as a Board Member of Theraly Pharmaceuticals, USA.
The tremendous potential of biologic drugs is hampered by short half-lives in vivo, resulting in significantly lower potency than activity seen in vitro. These short-acting therapeutic agents require frequent dosing profiles that can reduce applicability to the clinic, particularly for chronic conditions. Therefore, half-life extension technologies are entering the clinic to enable improved or new biologic therapies. PEGylation is a commonly utilized technique to improve drug solubility and stability, prolong blood circulation time, reduce immunogenicity, and decrease dosing frequency. As with any form of molecular modification, the active site is affected and can drastically decrease the bioactivity of the therapeutic agent, especially when the modification is performed on a small molecular weight molecule like peptides and small proteins. Steric hindrance from high molecular weight PEG can lead to a dramatic loss in the biological and pharmacological activity of the molecules. The higher the molecular weight, the lower the bioactivity. Therefore, it is generally accepted that a balance must be struck between the molecular weight of the PEG and the activity of the therapeutic molecule to reach sufficient drug efficacy. The strategic PEGylation technique introduced here offers many benefits over the conventional PEGylated forms of peptides and proteins. Strategic PEGylation signifies that a tradeoff of PEGylation for bioactivity is not necessary. Specifically, this abstract focuses on the strategic PEGylation of potent therapeutic peptides for GLP-1 analogues as a model peptide. Strategic PEGylation can be a platform technology to extend the half-life while preserving the biological activity of peptide and small protein drugs.