Related Experiment Video
Updated: Jan 24, 2026

Facile Preparation and Photoactivation of Prodrug-Dye Nanoassemblies
Published on: February 17, 2023
Orally Active Aminopeptidase A Inhibitor Prodrugs: Current State and Future Directions
Mathilde Keck1,2, Reda Hmazzou1, Catherine Llorens-Cortes3
1Laboratory of Central Neuropeptides in the Regulation of Body Fluid Homeostasis and Cardiovascular Functions, Collège de France, Center for Interdisciplinary Research in Biology (CIRB), INSERM U1050/CNRS UMR 7241, 11 Place Marcelin Berthelot, 75005, Paris, France.
Purpose Of Review:
To review the data supporting the use of aminopeptidase A (APA) inhibitor prodrugs as centrally acting antihypertensive agents.
Recent Findings:
Brain renin-angiotensin system (RAS) hyperactivity has been implicated in the development and maintenance of hypertension. Angiotensin III, generated by APA, one of the main effector peptides of the brain RAS, exerts a tonic stimulatory control over blood pressure in hypertensive rats. This identified brain APA as a potential therapeutic target for the treatment of hypertension, leading to the development of RB150/firibastat, an orally active prodrug of the specific and selective APA inhibitor, EC33. When given orally, RB150/firibastat crosses the gastrointestinal and blood-brain barriers, enters the brain, and generates two active molecules of EC33 which inhibit brain APA activity, blocking brain angiotensin III formation, and decrease blood pressure for several hours in hypertensive rats. Orally active APA inhibitor prodrugs, by blocking brain RAS activity, represent promising novel strategy for treating hypertension.
More Related Videos
Related Concept Videos
Prodrugs
Prodrugs help overcome...
Oral Hypoglycemic Agents: α-Glucosidase Inhibitors
Acarbose and miglitol are...
Antihypertensive Drugs: Direct Renin Inhibitors
Anticoagulant Drugs: Vitamin K Antagonists and Direct Oral Anticoagulants
Warfarin, a prominent vitamin K antagonist family member, exerts its effect by inhibiting the enzyme VKORC1 (vitamin K epoxide reductase complex 1). By hindering this enzyme, warfarin...
Eukaryotic Transcription Inhibitors
Eukaryotic transcription inhibitors usually contain two distinct domains, a...
Oral Cavity
Teeth: The teeth are the hardest structures in our bodies. Humans have two sets of teeth throughout their lifetime: deciduous (baby) teeth and permanent teeth. Each tooth consists of several parts: the crown (visible part), the root (embedded in the jaw), enamel (hard outer...

