PE0139 is a novel, super-long-acting basal insulin for the treatment of hyperglycemia associated with diabetes dosed as a once-weekly injection. PE0139 is a fully mature, native insulin molecule (B and A chains) genetically fused to our ELP polymer. The compound is manufactured using PhaseBio’s ELP-based E. coli expression system, where refolding of the drug occurs naturally in the cytosol. PE0139 is in a simple formulation that facilitates co-formulation with GLP-1 receptor agonists, including PhaseBio’s proprietary GLP-1, PB1023, and other GLP-1 receptor agonists.
A phase 1 single ascending dose study of PE0139 in adults with type 2 diabetes demonstrated prolonged exposure to the drug that would enable once-weekly administration and a low peak-to-trough ratio, which is particularly important for basal insulin. This profile was confirmed in a phase 2a multiple ascending dose study.