molecules of the year


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

1 min read

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.

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