Vardenafil (hydrochloride hydrate)

Vardenafil is a potent inhibitor of phosphodiesterase 5 (PDE5; IC50s = 0.2-1.2 nM) and PDE6 (IC50 = 2 nM). It is selective for PDE5 and PDE6 over PDE1 and PDE11 (IC50s = 230 and 130 nM, respectively). Vardenafil (4 mg/kg per day for three weeks) improves erectile function in a rat model of acute arteriogenic erectile dysfunction by increasing intracavernous pressure and mean arterial pressure, and this effect persists for at least two weeks following the end of treatment. Chronic vardenafil administration at a dose of 2 mg/kg for five weeks in subordinate mice reduces the latency to mount and increases the frequency of mounting behavior. Formulations containing vardenafil have been used in the treatment of erectile dysfunction.