Drug intelligence / Profile preview

FR900359

Development stage
Preclinical
Lead developer
Novartis
Modality
Small Molecules, Peptides
Administration
Inhalation
01

Overview

FR900359 is a cyclic depsipeptide natural product isolated from the plant *Ardisia crenata*. It acts as a potent and selective pan-Gq protein inhibitor, specifically targeting the Gαq, Gα11, and Gα14 subunits of heterotrimeric G proteins. By blocking Gq-mediated signaling, FR900359 inhibits the downstream activation of phospholipase C and subsequent calcium mobilization. Research has demonstrated its potential in treating conditions characterized by pathological Gq signaling, such as pulmonary hypertension, where it prevents and reverses both vasoconstriction and vascular remodeling. It has shown superior vasodilatory effects compared to standard-of-care treatments like bosentan and sildenafil in preclinical models.

Other names
UBO-QIC
02

Targets

GNA11 (Guanine nucleotide-binding protein subunit alpha-11)GNAQ (G protein subunit alpha q)

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