Drug intelligence / Profile preview

sitagliptin + enalaprilat

Development stage
Unknown
Lead developer
Merck
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This combination therapy involves sitagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, and enalaprilat, the active metabolite of the angiotensin-converting enzyme (ACE) inhibitor enalapril. The interaction between these two classes of drugs was investigated by Vanderbilt University in a mechanistic clinical trial (NCT01202903) to determine if DPP-4 inhibition potentiates vasodilator responses during ACE inhibition. This research is particularly relevant to understanding the pathophysiology of ACE inhibitor-associated angioedema, as both ACE and DPP-4 are involved in the degradation of vasoactive peptides such as substance P and bradykinin. Sitagliptin is primarily indicated for the management of type 2 diabetes mellitus, while enalaprilat is used for the treatment of hypertension and heart failure.

Brand names
JanuviaVasotec
Other names
Sitagliptin and Enalaprilat InteractionDPP-4 inhibitor + ACE inhibitor combination
02

Targets

DPP-4 (Dipeptidyl Peptidase-IV)ACE (Angiotensin Converting Enzyme)

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