oral, ultralong-acting insulin analog
effective in Ph. IIa, hum. t1/2~3 d, 4% F dog
albumin-binding motif + reduced endocytosis
J. Med. Chem., Dec. 28, 2020
Novo Nordisk, Maaloev, DK
Finally, December’s molecule, the Novo Nordisk oral insulin analog OI338, is the first oral insulin to demonstrate similar outcomes to insulin glargine injection in a Ph. II clinical trial. The molecule has an ultralong PK profile (t1/2 = 70 h) due to the inclusion of an albumin-binding long-chain fatty acid. Though the human doses of OI338 are high enough to challenge commercial access, the technical achievement of achieving oral activity in human with such a complex peptide is outstanding.