Current status of selected oral peptide technologies in advanced preclinical development and in clinical trials

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Title: Current status of selected oral peptide technologies in advanced preclinical development and in clinical trials
Authors: Aguirre, Tanira A. S.
Teijeiro-Osorio, D.
Rosa, Mónica
Brayden, David James
et al.
Permanent link: http://hdl.handle.net/10197/7801
Date: 15-Nov-2016
Abstract: The development of oral dosage forms that allows absorption of therapeutic peptides to the systemic circulation is one of the greatest challenges for the pharmaceutical industry. Currently, a number of technologies including either mixtures of penetration enhancers or protease inhibitors and/or nanotechnology-based products are under clinical development. Typically, these formulations are presented in the form of enteric-coated tablets or capsules. Systems undergoing preclinical investigation include further advances in nanotechnology, including intestinal microneedle patches, as well as their combination with regional delivery to the colon. This review critically examines four selected promising oral peptide technologies at preclinical stage and the twelve that have progressed to clinical trials, as indicated in www.clinicaltrials.gov. We examined these technologies under the criteria of peptide selection, formulation design, system components and excipients, intestinal mechanism of action, efficacy in man, and safety issues. The conclusion is that most of the technologies in clinical trials are incremental rather than paradigm-shifting and that even the more clinically-advanced oral peptide drugs examples of oral bioavailability appear to yield oral bioavailability values of only 1-2% and are, therefore, only currently suitable for a limited range of peptides.
Funding Details: European Commission - Seventh Framework Programme (FP7)
Type of material: Journal Article
Publisher: Elsevier
Copyright (published version): 2016 Elsevier
Keywords: Oral peptides;Intestinal permeation enhancers;Therapeutic peptides;Peptide clinical trials;Oral nanotechnology
DOI: 10.1016/j.addr.2016.02.004
Language: en
Status of Item: Peer reviewed
Appears in Collections:Conway Institute Research Collection
Veterinary Medicine Research Collection

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