Drug intelligence / Profile preview

vigafirstat

Development stage
Unknown
Lead developer
Topfond Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

Vigafirstat (TPN729) is a potent and highly selective small-molecule inhibitor of cGMP-specific phosphodiesterase type 5 (PDE5), developed by Henan Topfond Pharmaceutical in collaboration with Topharman Shanghai. It is specifically designed for the treatment of erectile dysfunction (ED). The mechanism of action involves the inhibition of the PDE5 enzyme, which prevents the degradation of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the corpus cavernosum. By maintaining elevated levels of cGMP, vigafirstat enhances the nitric oxide-mediated relaxation of smooth muscles and increases blood flow to the penis during sexual stimulation. Clinical development in China has reached Phase 3, where the drug has demonstrated efficacy and a safety profile comparable to established PDE5 inhibitors like sildenafil and tadalafil, potentially offering improved selectivity and reduced side effects.

Other names
vigafirstat maleatevigafirstat hydrochloride
02

Targets

PDE5 (Phosphodiesterase 5A)

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