title: Lessons learned from the clinical development of oral peptides.
abstract: The oral delivery of peptides and proteins has been hampered by an array of obstacles. However, several promising novel oral delivery systems have been developed. This paper reviews the most advanced oral formulation technologies, and highlights key lessons and implications from studies undertaken to date with these oral formulations. Special interest is given to oral salmon calcitonin (CT), glucagon-like peptide-1 (GLP-1), insulin, PYY-(3-36), recombinant human parathyroid hormone (rhPTH(1-31)-NH2) and PTH(1-34), by different technologies. The issues addressed include (i) interaction with water, (ii) interaction with food, (iii) diurnal variation, (iv) inter- and intra-subject variability, (v) correlation between efficacy and exposure and (vi) key deliverables of different technologies. These key lessons may aid research in the development of other oral formulations.
authors.affiliation: Nordic Bioscience A/S, Herlev, Denmark.
authors.forename: Morten Asser
authors.initials: MA
authors.lastname: Karsdal
authors.forename: Bente Juul
authors.initials: BJ
authors.lastname: Riis
authors.forename: Nozer
authors.initials: N
authors.lastname: Mehta
authors.forename: William
authors.initials: W
authors.lastname: Stern
authors.forename: Ehud
authors.initials: E
authors.lastname: Arbit
authors.forename: Claus
authors.initials: C
authors.lastname: Christiansen
authors.forename: Kim
authors.initials: K
authors.lastname: Henriksen
mesh_terms: D000284:Administration, Oral; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods*; D065569:Gastrointestinal Absorption; D006801:Humans; D010446:Peptide Fragments / Q000008:administration & dosage* / Q000493:pharmacokinetics; D011994:Recombinant Proteins / Q000008:administration & dosage* / Q000493:pharmacokinetics; D013678:Technology, Pharmaceutical / Q000379:methods*
chemical_list: D004337:Drug Carriers; D010446:Peptide Fragments; D011994:Recombinant Proteins
keywords: bone; calcitonin; cartilage; clinical trial; diabetes; oral formulation