Drug intelligence / Profile preview

pentaerythrityl tetranitrate

Development stage
Phase 3
Lead developer
Aristo Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

Pentaerythrityl tetranitrate (PETN) is a long-acting organic nitrate vasodilator primarily utilized for the management of coronary artery disease, angina pectoris, and congestive heart failure. Unlike other organic nitrates such as nitroglycerin, PETN is uniquely associated with a lack of nitrate tolerance and endothelial dysfunction during long-term therapy. It functions as a nitric oxide (NO) donor that requires bioactivation by the enzyme mitochondrial aldehyde dehydrogenase (ALDH2). The released NO stimulates soluble guanylate cyclase (sGC), increasing intracellular cGMP and promoting smooth muscle relaxation. Furthermore, PETN induces the expression of antioxidant genes, specifically heme oxygenase-1 (HO-1) and ferritin, which contribute to its vasoprotective properties. Recent clinical research has focused on its potential to improve placental perfusion and prevent fetal growth restriction (FGR) and preeclampsia in high-risk pregnancies.

Brand names
PentalongPeritrateLentratPentrit
Other names
Pentaerythritol tetranitratePETNNitropenta
02

Targets

ALDH2 (Mitochondrial Aldehyde Dehydrogenase)sGC (Soluble Guanylyl Cyclase)HMOX1 (Heme oxygenase 1)

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