Drug intelligence / Profile preview

fasudil + diethylenetriamine nonoate

Development stage
Preclinical
Lead developer
Vascular BioSciences
Modality
Small Molecules, Peptides, Liposomes → Lipid-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Inhalation
01

Overview

Fasudil + diethylenetriamine nonoate is an investigational combination therapy being developed by Vascular BioSciences (VBS Pharmaceuticals) for the treatment of pulmonary arterial hypertension (PAH) and COVID-19. The formulation co-delivers fasudil, a Rho-kinase (ROCK) inhibitor, and diethylenetriamine NONOate (DETA NONOate), a long-acting nitric oxide (NO) donor, within CAR peptide-modified liposomes. The CAR peptide (CARSKNKDC) is a cyclic 9-amino-acid homing peptide that selectively targets diseased pulmonary vasculature, allowing for localized delivery via inhalation. This dual-pathway approach aims to reduce vasoconstriction and vascular remodeling by inhibiting RhoA/ROCK signaling while simultaneously promoting vasodilation through nitric oxide donation. Preclinical studies have demonstrated significant reductions in pulmonary arterial pressure and amelioration of vascular remodeling features.

Other names
Fasudil + DETA NONOate liposomesCAR-targeted liposomal combination therapypeptide-modified liposomes
02

Targets

ROCK1 (Rho-associated coiled-coil containing protein kinase 1)sGC (Soluble Guanylyl Cyclase)

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