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Further Insights for Oral Uptake of Cyclic Peptides
Novartis Pharma AG
Translating Macro cyclic and Constrained Peptide Therapeutics into the Clinic
Bicycle Therapeutics Ltd
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.
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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.
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.
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. 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.
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.
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.