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Key Sessions

Thomas Vorherr

Further Insights for Oral Uptake of Cyclic Peptides

Novartis Pharma AG

Gavin Bennett

Translating Macro cyclic and Constrained Peptide Therapeutics into the Clinic

Bicycle Therapeutics Ltd

08:00 - 09:00 60 mins
Registration
09:00 - 09:10 10 mins
Chairperson’s Opening Remarks
  • Lukas Leder - Investigator, Novartis Institutes for Biomedical Research (NIBR), Switzerland
09:10 - 09:50 40 mins
Info
PRECLINICAL, NON-CLINICAL & CLINICAL DEVELOPMENTS, DELIVERY & FORMULATION
Further Insights for Oral Uptake of Cyclic Peptides
  • Thomas Vorherr - Director Peptide Discovery , Novartis Pharma AG

In the context of permeability, latest insights on oral bioavailability of peptides are shared. In particular, strategies aiming at modifying peptides to maintain or to enhance solubility while enabling permeability constitute a significant challenge, but are of high interest to ensure a smooth drug discovery process. In this context, the role of metabolism is also discussed by comparing closely related peptides.

09:50 - 10:30 40 mins
PRECLINICAL, NON-CLINICAL & CLINICAL DEVELOPMENTS, DELIVERY & FORMULATION
Cost Efficient Purification of Peptides via ZEOsphere DRP Mixed-Mode Chromatography
  • Alessandro Butte - CEO, DataHow AG
10:30 - 11:15 45 mins
Morning Coffee Break and Networking
11:15 - 11:55 40 mins
Info
PRECLINICAL, NON-CLINICAL & CLINICAL DEVELOPMENTS, DELIVERY & FORMULATION
Oral insulin: an impending reality?
  • Dr Miriam Kidron - Chief Scientific Officer and Director, Oramed Pharmaceuticals Ltd.

Oramed’s oral insulin formulation has been associated with blunted postmeal glucose excursions, stabilized glucose swings and reduced bolus insulin requirements in type 1 diabetes patients. When delivered at bedtime, it has led to lowered nighttime, morning fasting and daytime blood glucose levels in type 2 diabetes patients. The delivery platform is projected to revolutionize drug bioavailability and patient care.

11:55 - 12:35 40 mins
Info
PRECLINICAL, NON-CLINICAL & CLINICAL DEVELOPMENTS, DELIVERY & FORMULATION
Compliance-Ready LC-MS Workflows for Synthetic Peptide Analysis
  • Asish Chakraborty - Ph.D, Waters Corporation

With greater efficacy, safety, and tolerability in humans as compared to small molecules, peptides are drawing more attention as potential drug candidates targeting a wide variety of diseases. As investment into these peptide-based therapeutics grows, there is an increasing need for more efficient workflows that can bring these drugs to market in a timely manner while preserving product quality and safety.

Waters provides leading solutions for lab-scale purification, characterization, and monitoring of synthetic peptides and their impurities. Flexible, robust and compliance-ready LC-UV and LC-UV-MS workflows have been developed to meet the analytical needs of our customers, enabling them to speed development while ensuring peptide drug quality and safety.

Being in compliance has never been more important for ensuring product quality and improving productivity through less downtime due to data integrity questions. Indeed, compliance solution is becoming a must for making sure that results are reliable, accurate and trustworthy, and Waters is the only provider able to deliver and support this.

In this presentation, we will lead you through the journey of purification, method development, characterization, and impurity profiling of synthetic peptides and discuss the benefits of LC-MS in each step of the analysis.

12:35 - 13:45 70 mins
Lunch and Networking
13:45 - 14:25 40 mins
Info
PRECLINICAL, NON-CLINICAL & CLINICAL DEVELOPMENTS, DELIVERY & FORMULATION
Design and Development of a Self-Assemble Drug Delivery System
  • Sheauyu Teddy Hsu, PhD - Managing Director, Adepthera

Therapeutic proteins and peptides are generally administered parenterally. Due to sensitivity to proteolysis and renal clearance, many peptide therapeutics need continuous administration or frequent doses of injections to achieve efficacy. Conjugation or fusion to polyethylene glycol (PEG), fatty acids, albumin, antibodies and unstructured proteins such as XTEN and PAS have been developed to extend the half-life of polypeptide drugs. These approaches extend the circulating half-life mainly by increasing the molecular mass of peptide moieties. Techniques employing slow-release carriers, including oil suspension, crystal particle suspension, liposomes, microspheres, and hydrogels have also been used to improve the pharmacokinetics, bioavailability, patient compliance, and efficacy of peptide therapeutics. However, most of these sustained-release techniques are associated with select disadvantages, including immunogenicity and complex fabrication processes. Therefore, alternative techniques that can further improve the delivery of peptide therapeutics are much needed. To improve the development of polypeptide therapeutics, we have developed a novel technology that generate self-assemble peptide therapeutic candidates with a minimum immunogenic footprint. In this presentation, we will discuss the discovery and design of this novel technology and its applications in peptide drug development.

14:25 - 15:05 40 mins
Info
PRECLINICAL, NON-CLINICAL & CLINICAL DEVELOPMENTS, DELIVERY & FORMULATION
Lessons Learnt from Peptide Therapeutics in Preclinical and Clinical Development
  • Les Miranda, PhD - Executive Director Research, Therapeutic Discovery, Amgen, Inc.

Drug discovery research on new pain targets with human genetic validation, including the voltage-gated sodium channel NaV1.7, is being pursued to address the unmet medical need for treatment of chronic pain and the rising opioid epidemic.  Although there has been considerable effort directed at the identification of a Nav1.7 inhibitory monoclonal antibody, the only reported NaV1.7 targeting monoclonal antibody could not be reproduced[1].  As part of efforts to better understand the general potential of utilizing large molecule scaffolds, we pursued an alternate approach to generate a large molecule inhibitor of Nav1.7 function.  In this presentation we describe the combined engineering of antibodies and peptides to facilitate the identification of peptide-antibody hybrids with improved NaV1.7 inhibitory activity and pharmacokinetics.  A bespoke data visualization system to support large molecule engineering campaigns will also be presented.

15:05 - 15:45 40 mins
Info
PRECLINICAL, NON-CLINICAL & CLINICAL DEVELOPMENTS, DELIVERY & FORMULATION
Development of complex peptides – insights from a CDMO perspective
  • Dr. Daniel Bourgin - Business Development CPS Europe, Dr. Reddy's Laboratories SA, Switzerland

Unlike drug discovery organizations where invention of new molecules as first in class drugs or superior drugs to existing molecules on safety and efficacy is of priority, CDMO’s focus will be on Chemical development & scale up by applying QbD principles and associated challenges with an eye on the commercialization. Peptides, as medicines for several indications, have become a class of compounds which the pharma industry has placed a big bet. This provides an unique opportunity to CDMO’s offering for peptides as a service to work on variety of peptides  - linear, cyclic by both solid and solution phase by partnering with multiple innovators. The presentation illustrates our experiences and knowledge gained over the last few years including a case study on challenges in the development and process validation for Linaclotide.

15:45 - 16:30 45 mins
Afternoon Coffee Break
16:30 - 17:10 40 mins
PRECLINICAL, NON-CLINICAL & CLINICAL DEVELOPMENTS, DELIVERY & FORMULATION
Translating Macro cyclic and Constrained Peptide Therapeutics into the Clinic
  • Gavin Bennett - Head of Pre-Clinical Development, Bicycle Therapeutics Ltd
17:10 - 17:50 40 mins
Info
PRECLINICAL, NON-CLINICAL & CLINICAL DEVELOPMENTS, DELIVERY & FORMULATION
Identification, Characterization, and Management of Rare Genetic Disorders of Obesity: From Bench to Bedside
  • Dr. Lex Van der Ploeg - Chief Scientific Officer, Rhythm Pharmaceuticals

Severe, early-onset obesity and excessive hunger have been reported in individuals with ultra-rare variants in several genes, including genes encoding components upstream of the melanocortin-4 receptor (MC4R) (e.g., leptin receptor, pro-opiomelanocortin and genes involved in the Bardet-Beidl syndrome). Efforts for an enhanced MC4R pathway understanding, patient identification, clinical characterization, and interventional studies with the MC4R agonist setmelanotide in individuals affected by rare genetic disorders of obesity are ongoing.


17:50 - 19:20 90 mins
End of Day 2 and Networking Evening Reception in the Exhibition Hall