PL8177 for Inflammatory Bowel Disease

PL8177 for Inflammatory Bowel Disease

PL8177, a selective MC1r agonist peptide, is our lead clinical development
candidate for inflammatory bowel diseases, including ulcerative colitis. PL8177 is a
cyclic peptide comprised of seven amino acids. We filed an Investigational New
Drug (“IND”) application on PL8177 in late 2017 and in 2018 successfully completed
subcutaneous dosing of human subjects in a Phase 1 single and multiple ascending
dose clinical safety study.

For ulcerative colitis and other inflammatory bowel diseases we will administer
PL8177 in an oral formulation designed to deliver PL8177 to the interior wall of the
diseased bowel. PL8177 activates MC1r present on the interior wall of the bowel in
ulcerative colitis and other inflammatory bowel diseases. We believe that delivering
PL8177 directly to MC1r in the bowel wall will maximize treatment effect while
minimizing any systemic or off-target effects.

In 2019 we completed a micro-dose clinical study of radiolabeled PL8177 in healthy
subjects using an oral, delayed-release, polymer formulation. The micro-dose study
demonstrated release of polymer bound PL8177 in the lower gastrointestinal tract
after oral administration with a favorable pharmacokinetic profile. The study also
demonstrated that with the oral formulation PL8177 was not systemically
absorbed.

A Phase 2 study in ulcerative colitis using the oral, delayed-release, polymer
formulation of PL8177 is scheduled to start in the second half of calendar 2020.