Drug development from the bench to the pharmacy: with special reference to dipeptidyl peptidase ‐ 4 inhibitor development

The dipeptidyl peptidase ‐ 4 ( DPP ‐ 4) inhibitor concept is an example of prospective drug design and development based upon a distinct endocrine hypothesis. The design of enzyme inhibitors is a pragmatic approach to drug design; being compatible with the identification and optimization of small molecules that have properties commensurate with oral administration, as well as acceptable drug metabolism, distribution and elimination characteristics. Glucagon‐like peptide 1 ( GLP ‐ 1), a hormone with a spectrum of favourable metabolic actions, including glucose‐dependent stimulation of insulin and inhibition of glucagon secretion, provided the endocrine basis from which the idea of using DPP ‐ 4 inhibitors as anti‐diabetic agents was developed. The origin of the DPP ‐ 4 inhibitor concept was inspired by the angiotensin‐converting enzyme inhibitor approach, which succeeded in establishing a class of extensively used therapeutic agents for the treatment of cardiovascular disorders.