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

Diabetic Medicine : a Journal of the British Diabetic Association
R D Carr

Abstract

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.

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Citations

May 20, 2016·Diabetic Medicine : a Journal of the British Diabetic Association·R I G Holt
May 20, 2020·Diabetic Medicine : a Journal of the British Diabetic Association·R D Carr, A Solomon
Sep 16, 2020·Nature Reviews. Endocrinology·Carolyn F Deacon

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