Drug intelligence / Profile preview

ABT-279

Development stage
Discontinued
Lead developer
Abbott
Modality
Small Molecules
Administration
Oral
01

Overview

ABT-279 is a potent and highly selective small molecule inhibitor of dipeptidyl peptidase-IV (DPP-IV), originally developed by Abbott Laboratories (now AbbVie) for the treatment of type 2 diabetes. It functions by preventing the degradation of incretin hormones such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), thereby enhancing glucose-dependent insulin secretion and improving glycemic control. ABT-279 is characterized by a 2-cyanopyrrolidide warhead with a C5 ethynyl substitution, which contributes to its high affinity (Ki = 1.0 nM) and significant selectivity over related enzymes such as DPP8 and DPP9 (Ki > 30 μM). Although it demonstrated efficacy and safety in preclinical studies as an orally available clinical candidate, its development appears to have been discontinued.

Other names
2-[4-[[2-[(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]-4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid
02

Targets

DPP8 (Dipeptidyl peptidase 8)DPP-4 (Dipeptidyl Peptidase-IV)KCNH2 (Voltage-gated potassium channel subfamily H member 2)DPP9 (Dipeptidyl Peptidase 9)

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