Oral administration of peptide-based drugs: Beyond Lipinski's rule

Santos, Gabriela B., Ganesan, A. ORCID: https://orcid.org/0000-0003-4862-7999 and Emery, Flavio S. (2016) Oral administration of peptide-based drugs: Beyond Lipinski's rule. ChemMedChem, 11 (20). 2245–2251. ISSN 1860-7179

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The use of peptides in therapy presents several limitations, from physicochemical characteristics to inadequate pharmacokinetic profiles for oral absorption. As peptides are gaining importance in the therapeutic arsenal, there is an increasing need to rationalize the main characteristics of this compound class in the market. Therefore, we performed an extensive analysis of all known peptide drugs and clinical candidates based on their peptide features, physicochemical and structural properties, and correlated these with their administration route and therapeutic classes. Peptide drugs are widely distributed across drug and pharmacological space, covering several therapeutic areas with structural diversity and complexity, distributed between groups of cyclic and linear compounds. Although structural and physicochemical properties are clear within these groups, we counter the consensus that cyclic peptides have better oral availability than linear peptides, as most of the orally administrated peptides have linear structures. This study and review furnishes information that could support peptide drug design, with a new cutoff of known descriptors that go beyond the Rule of Five.

Item Type: Article
Uncontrolled Keywords: drug discovery,drug likeness descriptors,drugs,peptides,physicochemical properties
Faculty \ School: Faculty of Science > School of Pharmacy
UEA Research Groups: Faculty of Science > Research Groups > Medicinal Chemistry (former - to 2017)
Faculty of Science > Research Groups > Chemical Biology and Medicinal Chemistry (former - to 2021)
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Depositing User: Pure Connector
Date Deposited: 24 Sep 2016 00:54
Last Modified: 22 Oct 2022 01:32
URI: https://ueaeprints.uea.ac.uk/id/eprint/60267
DOI: 10.1002/cmdc.201600288

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