• Japanese
  • Korean
  • Chinese
Cover Image

Innovations in the Delivery of Peptides

Peptides are an important class of drugs, but their potential for treating chronic diseases will be fully realized only if more acceptable delivery methods than daily injections can be developed. Recognition of this has led to advances in oral, intranasal, inhaled, transdermal, and buccal formulations. This report analyses the products and companies at the forefront of such research.

FEATURES AND BENEFITS

  • Assess the breadth of innovations that have been applied to the delivery of peptide drugs.
  • Compare the various technologies developed for use within particular indications.
  • Evaluate the merits and limitations of each company's peptide delivery solutions.
  • Gain insight from analysis of the patents filed to protect specific delivery technologies.
  • Understand the technical principles on which the delivery technologies are based.

HIGHLIGHTS

The demise of Exubera, an inhaled insulin product, has had a knock-on effect on the inhaled insulin technologies and there are now few still in development, despite products offering strong advantages such as fast absorption, fast onset of action, and a non-invasive mode of administration.

New oral nanotechnology peptide formulations are showing promise, particularly in the area of insulin and GLP-1 analog delivery. New long-acting peptides and controlled release injectable formulations are extending peptide half-lives significantly, leading to weekly and even monthly subcutaneous injectable formulations.

First- and second-generation transdermal patch technologies were not suitable for peptide drug delivery due to the need for low molecular weight and low dose loading, but third-generation patch technologies (such as thermal ablation, microneedles, vesicular carriers, and iontophoresis) are offering promise in the delivery of several peptides.

YOUR KEY QUESTIONS ANSWERED

  • What type of delivery technologies are available to those developing peptide therapeutics?
  • What peptide delivery challenges are the innovations intended to overcome?
  • Which indications offer the greatest advances by investment in delivery technologies?
  • Which companies have already formed partnerships with the inventors of cutting-edge delivery techniques?
  • What hurdles remain for specific technologies and how far are they from being employed in a commercialized drug?

Table of Contents

About the author

  • Disclaimer

EXECUTIVE SUMMARY

  • Peptide delivery technologies overview
  • Innovations in peptide delivery for diabetes and obesity
  • Innovations in peptide delivery for osteoporosis and other bone diseases
  • Innovations in peptide delivery for cardiovascular diseases
  • Innovations in peptide delivery for CNS and inflammatory diseases
  • Innovations in peptide delivery for GI diseases, cancer, and hormonal conditions

Peptide delivery technology overview

  • Summary
  • Introduction
  • Issues in the development of therapeutic peptides
  • Benefits of less-invasive modes of administration
  • Key parameters
  • Developments in injectable peptide delivery
  • Challenges of oral peptide delivery
    • Degradation of peptides in the digestive tract
    • Peptides may have a narrow window of absorption from the GI tract
  • Mechanisms of transport across the gastrointestinal mucosa
  • Technologies used in oral delivery of therapeutic peptides
    • Enzyme inhibitors
    • Permeation enhancers
    • Mucoadhesives
    • Encapsulation technologies
    • M-cell targeting
  • Companies involved in oral delivery of peptides
    • Unigene's Enteripep technology
    • Aegis Therapeutics' Intravail technology
    • Oramed's oral peptide delivery technology
    • Merrion's GIPET technology
    • Biodel's VIAtab technology
    • Emisphere's Eligen technology
    • Bone Medical and Diabetology's Axcess technology
  • Nanotechnology used in the oral delivery of peptides
    • NOD Pharmaceuticals' nanoparticle oral delivery (NOD) technology
    • MonoSol Rx and Midatech PharmFilm transbuccal insulin
    • NanoMega Medical Corporation's Imulin (chitosan nanoparticles)
    • Access Pharmaceuticals' CobOral nanoparticle technology
  • Inhaled peptide delivery
    • MannKind's Technosphere inhalable technology
  • Transdermal peptide delivery
    • Combination of chemical enhancers
    • Biochemical enhancers
  • Third-generation transdermal delivery technologies
    • Vyteris's Smart Patch technology
    • TransPharma Medical's ViaDor technology
    • Altea Therapeutics' PassPort transdermal patch
    • Phosphagenics' Targeted Penetration Matrix (TPM)
    • Zosano ZP Transdermal Microprojection Delivery technology

Innovations in peptide delivery for diabetes and obesity

  • Summary
  • Introduction
  • Insulins
    • Background
    • Types of new injectable insulins and delivery systems
    • Innovative transdermal delivery of insulin
    • Inhalable insulin
    • Oral insulin
    • Novel insulin approaches to treating type 1 diabetes
  • Glucagon-like peptide analogs
    • Byetta (exenatide)
    • New injectable delivery technologies for GLP-1 analogs
    • Early-stage GLP-1 analogs
    • Long-acting injectable GLP-1 dual agonists
    • Inhalable GLP-1 analog - MKC253 (GLP-1/Technosphere inhaler)
    • Transdermal GLP-1 analog - VIaDor-GLP-1 agonist
    • Oral delivery of GLP-1 analogs
  • Insulin and GLP-1 combination products
    • IDegLira (NN9068)
    • Insulin, amylin, and/or GLP-1 formulation
    • ACP004 (GLP-1 + insulin fixed dose combination)
  • Other new peptides for treating diabetes, obesity, and other metabolic diseases
    • NN9161
    • Oxymera (oxyntomodulin ELP fusion protein)
    • MOD-600 (REV-PEG-Oxyntomodulin)
    • UGP281 (oral calcitonin analog)
    • Oral/intranasal Intravail - leptin hormone fragment obesity treatment
    • Oral PYY3 - 36
    • ZP2435
    • AC165198 (Phybrid fusion protein)
    • RM-493 (BIM-22493)
    • ARX618

Innovations in peptide delivery for osteoporosis and other bone diseases

  • Summary
  • Introduction
  • Calcitonin
    • Current therapies and market landscape
    • Oral calcitonin products in development
    • Transdermal calcitonin - ViaDor-calcitonin
  • Parathyroid hormone
    • Current therapies and market landscape
    • Oral and intranasal delivery of PTH analogs
    • Transdermal delivery of PTH and analogs
    • Innovative injection and depot delivery of PTH analogs

Innovations in peptide delivery for cardiovascular diseases

  • Summary
  • Introduction
  • New long-acting treatments for heart failure
    • Sustained-release VSXP325
    • Long-acting atrial natriuretic peptides
    • COR-1 (cyclic peptide)
    • Once-weekly recombinant relaxin ReCODE
    • Neucardin (Recombinant human neuregulin-1; rhNRG-1)
    • RLX030 (recombinant human relaxin-2)
    • Cardeva (B-type natriuretic peptide)
  • Peptide delivery approaches for other cardiovascular and related diseases
    • Nanofiber gel PAD therapy
    • Vasomera (VIP-ELP-120; PB-1046; PB-1120)
    • Oral L-4F peptide
    • AP214 (ZP1480) - SIP
    • Peginesatide acetate (Hematide, AF37702)

Innovations in peptide delivery for CNS and inflammatory diseases

  • Summary
  • Introduction
  • New beta interferon and glatiramer acetate formulations for MS
    • NU100 (liquid recombinant human interferon beta-1b)
    • NU400 (PEGylated interferon beta-1b)
    • ARX424 (PEGylated interferon beta)
    • Glatiramer acetate depot system
    • Glatiramer acetate and cannabidiol combination nasal delivery
  • New peptide treatments for multiple sclerosis
    • ATX-MS-1467
    • PI-2301
    • GM607
  • Parkinson's and Alzheimer's diseases
    • MANF RapidMist
    • Pepticlere nasal spray
    • Insulin nasal spray
  • Acute ischemic stroke
  • Pain
    • PDC-41
    • THA902 XL (Medusa-enabled long acting THA902)
    • CEL-021
  • Fibrosis
    • Medusa-enabled disitertide (P144)
    • Medusa-enabled P17
    • PRM-151 (rhPTX-2)
    • PRM-167 (intravitreal injection of rhPTX-2)

Innovations in peptide delivery for GI diseases, cancer, and hormonal conditions

  • Summary
  • Introduction
  • Irritable bowel syndrome constipation-predominant
    • Plecanatide (SP-304)
  • Inflammatory bowel disease - ulcerative colitis
    • SP-333
  • Chemotherapy-induced diarrhea
    • Elsiglutide (ZP1846)
  • Short bowel syndrome
    • Gattex (teduglutide; ALX0600; GLP-2 analogue NPS)
  • Diabetic gastroparesis
    • RM131 (BIM-28131)
  • Mucositis
    • NX002
  • Cancer
    • Acyline GIPET enhanced
    • Q-leuprolide
    • Somatuline Autogel
    • OP499
    • Stapled peptides cancer research program
    • Lutathera ((177Lutetium)-DOTA-Tyr3-octreotate; LU177; Lutate)
    • HM10660A (LAPS-IFNa)
  • Growth hormone deficiency
    • HM10560A (LAPS-rhGH)
    • CR024 (once-daily nasal spray somatropin - CriticalSorb)
    • CR016 (long-acting depot somatropin - CriticalMix)
    • MOD-4023 (hGH-CTP)
    • ARX201
  • Acromegaly - Q-leuprolide

Conclusions and future developments

  • Conclusions

Appendix

  • Scope
  • Methodology
  • Abbreviations
  • References

TABLES

  • Table: Oral peptide delivery drivers and resistors
  • Table: Companies developing innovative oral peptide delivery technologies (part 1)
  • Table: Companies developing innovative oral peptide delivery technologies (part 2)
  • Table: Unigene's Enteripep oral peptide delivery technology
  • Table: Aegis Therapeutics' technology for oral/nasal peptide delivery
  • Table: Oramed Pharmaceuticals' oral delivery technology
  • Table: Merrion's GIPET oral peptide delivery technology
  • Table: Biodel's VIAtab sublingual peptide delivery technology
  • Table: Emisphere's Eligen oral peptide delivery technology
  • Table: Bone Medical and Diabetology's Axcess technology PCT applications
  • Table: Companies developing nanotechnology for oral peptide delivery
  • Table: Advantages and disadvantages of inhaled peptide delivery
  • Table: Advantages and disadvantages of transdermal peptide delivery
  • Table: Third-generation transdermal delivery technologies for peptide delivery
  • Table: Innovative injectable insulin formulations (part 1)
  • Table: Innovative injectable insulin formulations (part 2)
  • Table: Oral insulin formulations in development for the treatment of diabetes
  • Table: Recently marketed and late-stage injectable GLP-1 technologies
  • Table: Early-stage GLP-1 analogs - technologies and products
  • Table: Novel injectable GLP-1 dual agonists for treating diabetes and obesity
  • Table: Oral technologies for delivering GLP-1 analogs for type 2 diabetes
  • Table: Fixed-dose combination insulin + GLP-1 analog products in development
  • Table: New delivery technologies and peptides for treating obesity
  • Table: Oral formulations of salcatonin
  • Table: Oral and intranasal formulations of PTH analogs
  • Table: Transdermal delivery of PTH and analogs
  • Table: Injection and depot delivery of PTH analogs
  • Table: New peptide delivery approaches for treating heart failure
  • Table: Peptide delivery technologies for cardiovascular and related diseases
  • Table: Drivers and resistors for new peptide delivery products for multiple sclerosis
  • Table: New potential biobetter formulations of interferon beta and glatiramer
  • Table: Novel peptide treatments for multiple sclerosis
  • Table: Peptide delivery formulations for Parkinson's and Alzheimer's diseases
  • Table: Novel peptides for treating pain
  • Table: Novel peptide treatments for fibrotic conditions
  • Table: Peptides and delivery technologies for treating GI diseases
  • Table: Novel peptide and delivery technologies for cancer
  • Table: Novel growth hormone delivery technologies

FIGURES

  • Figure: Advantages and disadvantages of peptides versus small-molecule drugs
  • Figure: Mechanisms of transport of compounds across the intestinal epithelium
  • Figure: Access Pharmaceuticals' Nanoparticle CobOral drug delivery technology
  • Figure: TransPharma Medical's ViaDor RF-MicroChannel transdermal delivery
  • Figure: Long-acting GLP-1 receptor agonists for subcutaneous injection
Show More
Pricing