ZYDENA Tablet Ref.[51199] Active ingredients: Udenafil

ZYDENA, an oral therapy for the treatment of erectile dysfunction (ED), is a pyrazolopyrimidinone class and a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5) of the corpus cavernosum, which induce potent penile erection.

ZYDENA demonstrated 88.5% improvement in patients with ED. Based on the results from the phase III trial performed in 13 Korean centers, involving 270 ED patients, ZYDENA showed 81.5% and 88.5% improvement in Global Assessment Questionnaire (GAQ) scores at doses of 100 and 200 mg, respectively, compared to placebo.

ZYDENA has an optimal duration of action of up to 8-12 hours. Clinical pharmacodynamic study showed that the time to maximum concentration (T_max) and half-life (T_I/2) of ZYDENA are approximately 1 hour and 10-12 hours, respectively. The ability to maintain an erection sufficient for a successful intercourse (SEP3) at 8-12 hours after taking ZYDENA (100 mg) was significantly superior to placebo in phase III study.

The efficacy and safety of ZYDENA are satisfactory in all the phase I, II, and III studies. ZYDENA is an oral therapy for the treatment of ED, which completed the clinical trial processes in Korea. The major adverse events are flushing, nasal congestion, headache, and dyspepsia. However, most adverse events were temporal and mild in severity.

Moreover, these adverse events soon resolved without treatment.

ZYDENA does not inhibit phosphodiesterase type 11 (PDE11) (>3,000-fold selectivity) and adverse effects such as myalgia, back pain have not been reported.

Geriatric Use

When udenafil (100 mg) was given to 12 healthy elderly volunteers (65-80 years) and 12 healthy younger volunteers (19-45 years), AUC and C_max of udenafil (l00 mg) in the elderly group were lower by 0.73-fold and 0.88-fold, respectively, compared to that of the younger group. Therefore, as the possibility of increased udenafil exposure in the elderly patients is rare, dose control is not required with elderly patients.

Administration experience in patients with renal impairment

The pharmacokinetic characteristics and safety was compared and evaluated in a clinical trial where ZYDENA 100mg was administered for single therapy in 9 healthy male subjects, 9 patients with mild renal impairment (creatinine clearance rate 50~80mL/min), 6 patients with moderate renal impairment (creatinine clearance rate 30~50mL/min), and 7 patients with severe renal impairment (creatinine clearance rate <30mL/min). The exposure of ZYDENA (AUC) was increased compared to healthy male subjects by 1.3 times in case of mild renal impairment and approximately 1.6 times in case of moderate or severe renal impairment. Information on terminal stage renal failure patients undergoing dialysis is unknown.

Administration experience in patients with hepatic impairment

The pharmacokinetic characteristics and safety was compared and evaluated in a clinical trial where ZYDENA 100mg was administered for single therapy in 6 healthy male subjects, 6 patients with mild hepatic impairment (Child-Pugh Class A) and 6 patients with moderate hepatic impairment (Child-Pugh Class B). The exposure of ZYDENA (AUC) was increased compared to healthy male subjects by 1.05 times in case of mild hepatic impairment and 1.49 times in case of moderate hepatic impairment. There is no information on administering more than ZYDENA 100mg in patients with hepatic impairment.