The number of people diagnosed with inflammatory bowel disease (IBD) is increasing. An estimated 3 million US adults were diagnosed with IBD in 2015, whereas the number of IBD patients was only 1.8 million in 1999. Most importantly, no medications have yet reported complete remission for IBD patients. Current therapeutics, both small molecules and biologics, are focused on reducing the immune response by targeting pro-inflammatory cytokines (e.g. TNFs, IL12/23s) and immune activating cells (e.g. lymphocytes, neutrophils). Limitations on current therapeutics based on anti-inflammatory mechanism of action include: 1) side effects of corticosteroids in prolonged exposure; 2) lack of efficacy of aminosalicylates; and 3) reduced remission and loss of response in TNF inhibitors. Also, Janus kinase (JAK) inhibitors used for moderate-to-severe IBD patients also raised concerns for venous thromboembolism, along with serious heart-related side effects stated from FDA.

NIPEP-IBD, 19 amino acid sequenced peptide, was designed to bind to selectively to integrin beta 1 expressed on the wound epithelium. This way, the peptide primarily travels to the target wound epithelium rather to distribute off-target site. The mode of action of the NIPEP-IBD after binding with integrin beta 1 is described.

The NIPEP-IBD has been found to be highly effective in epithelial restitution via FAK-Rho signaling pathway, as confirmed from the in vitro cell study using Caco-2 and HT-29 epithelial cells. The regenerative biomarker of epithelium including ZO-1, Occludin, Claudin-5 was significantly increased by the treatment of NIPEP-IBD in the experimentally created IBD in vitro model. The animal study with both acute and chronic IBD model further confirmed that the NIPEP-IBD, when subcutaneously injected, demonstrated significant improvement of the recovery as compared with the positive control, i.e., TNF-a antibody, with marked mucosal regeneration as reflected by histologic observation. 

19 amino acid, purity 99%