Drug intelligence / Profile preview

lodenafil carbonate

Development stage
Phase 4
Lead developer
Cristália
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral
01

Overview

Lodenafil carbonate is an orally active prodrug that delivers the active compound lodenafil in vivo. It belongs to the class of phosphodiesterase type 5 (PDE5) inhibitors, which are commonly used for the treatment of erectile dysfunction (ED). Lodenafil carbonate is a dimeric carbonate ester that breaks down in the body to release two molecules of lodenafil, resulting in higher oral bioavailability compared to its parent drug. Its mechanism of action involves inhibiting PDE5, thereby preventing cGMP breakdown and enhancing nitric oxide-mediated vasodilation in penile tissue. This leads to improved erectile function during sexual arousal but does not induce erections independently. Lodenafil carbonate has also demonstrated analgesic activity by promoting presynaptic hyperpolarization and preventing neuroplastic changes in rodent models. The drug has undergone Phase III clinical trials for ED and is marketed under the brand name Helleva in Brazil[1][3][5][6][8].

Brand names
Helleva
Other names
hydroxyhomosildenafillodenafil
02

Targets

PDE5 (Phosphodiesterase 5A)

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