Which pipeline products are available for protein and peptide-based therapeutics?
Protein and peptide-based therapeutics have been in use for more than three decades since the approval of recombinant human insulin, the first protein therapy, in 1982. Earlier, most biologic drugs were delivered through the subcutaneous route. However, over time, advances in delivery formulations have enabled the development of orally administrable versions of therapeutic proteins / peptides. Owing to numerous compelling reasons, the concept of oral delivery has gained significant traction. The first oral protein / peptide-based product candidate, Linzess®, was launched in 2012 in the US and EU. Recently, Trulance®, another orally administrable product was approved in the US (January 2017) for the treatment of chronic idiopathic constipation (CIC). In fact, in January 2018, Trulance® was approved for another indication, namely irritable bowel syndrome with constipation (IBS-C).
Around 100 oral protein / peptide therapeutics are currently being developed across various preclinical / clinical stages for a diverse range of indications. Two products, namely Linzess® (Ironwood Pharmaceuticals) and Trulance® (Synergy Pharmaceuticals), are commercially available; of these, Trulance® was approved in January 2017. Nearly 41% of the pipeline molecules are under clinical development; of these, 8 molecules are being investigated in phase III and phase II/III, 18 molecules in phase II, 5 molecules in phase II (planned), 1 in phase I/II, and 9 molecules in phase I and phase I (planned) clinical trials. However, majority (57%) of the product candidates in the pipeline are still in the preclinical and discovery stages.
To overcome the challenges related to the effective administration of oral biologics, several innovative technologies to formulate and deliver oral biologics are being developed. Notable examples of advanced drug delivery technologies include (in decreasing order of number of pipeline products) Robotic Pill Maker technology (Rani Therapeutics), Peptelligence® (Enteris BioPharma), Axcess
TM oral drug delivery technology (Proxima Concepts), Oral Peptide Utility System (OPUS) technology (Biolingus), Sublingual Immunotherapy (SLIT) technology (Biolingus), and Oramed Protein Oral Delivery (POD) technology (Oramed Pharmaceuticals).
According to a recent report published by Roots Analysis on, 42% of the products in the development pipeline are designed to treat various metabolic disorders, including (in decreasing order of number of pipeline products) diabetes, obesity and non-alcoholic steatohepatitis (NASH). Nearly 15% of therapy candidates are being developed for the treatment of digestive and gastrointestinal disorders, including (in decreasing order of number of pipeline products) chronic idiopathic constipation (CIC), irritable bowel syndrome with constipation (IBS-C), inflammatory bowel disease (IBD) (Crohn's disease and ulcerative colitis), opioid-induced constipation (OIC) and short bowel syndrome (SBS). Products are also being developed for other therapeutic areas, such as autoimmune disorders (9), infectious diseases (9), hormonal disorders (5), bone disorders (4), blood disorders (3), various oncological indications (2), respiratory disorders (2), urogenital disorders (2), genetic disorders (1) and neurodegenerative disorders (1).