Tolerability and pharmacokinetics of avanafil, a phosphodiesterase type 5 inhibitor: A single- and multiple-dose, double-blind, randomized, placebo-controlled, dose-escalation study in healthy Korean male volunteers

Avanafil, a Potent and Highly Selective Phosphodiesterase-5 Inhibitor for Erectile Dysfunction

“…More recently clinical studies of avanafil revealed that avanafil has good tolerability and pharmacokinetic properties, 20 and its time to maximum plasma concentration in humans is shorter than that of sildenafil, tadalafil and vardenafil. 20,21 This indicates that avanafil has more rapid onset of action in humans as well as in animals. Drugs were administered 5 minutes before stimulation.…”

Mechanisms of Penile Erection and Basis for Pharmacological Treatment of Erectile Dysfunction

“…Avanafil is a pyrimidine derivative rapidly absorbed and quickly eliminated after oral administration. A mean T max was reached at 0.33 to 0.52 h after oral dosing and then declined with a mean apparent t 1/2 of 5.36 to 10.66 h. AUC and C max were proportional to dose, and the mean accumulation index on day 7 after a single daily dose was 0.98; concomitant food intake decreased the C max by 24% (Jung et al, 2010;Limin et al, 2010). Two phase III studies have been completed, both with a positive outcome (Limin et al, 2010).…”

A review of analytical methods for the determination of four new phosphodiesterase type 5 inhibitors in biological samples and pharmaceutical preparations

“…Avanafil oral tablets will be available in 50, 100, and 200 mg (Traynor, 2012). A mean Tmax was reached at 0.33 to 0.52 h after oral dosing and then declined with a mean apparent T1/2 of 5.36 to 10.66 h. AUC and Cmax in a single-dose were 2217 ng h/mL and 1206 ng/mL, respectively (Jung et al, 2010). A randomized, double-blind, placebo-controlled Phase III study evaluating two doses of avanafil (100 and 200 mg) in 390 men with both diabetes and ED, showed satisfactory results.…”

“…Avanafil (Figure 4) is a selective PDE5 inhibitor developed by Mitsubishi Tanabe Pharma Corporation (Osaka, Japan) (Jung et al, 2010;Alwaal et al, 2011).…”

“…Mirodenafil (Mvix ® ), recently marketed in South Korea (Choi et al, 2009), is reported to have an excellent profile of efficacy for erectile dysfunction Kim et al, 2010). One of the recently developed PDE5i, avanafil is a promising medication for ED due to its favorable pharmacokinetics, safety, and efficacy (Jung et al, 2010;Alwaal et al, 2011). FDA approved avanafil (Stendra ® ) in April 27 (Traynor, 2012).…”