IC351 (tadalafil, Cialis): update on clinical experience

• Published in: International journal of impotence research Vol. 14 Suppl 1; no. S1; pp. S57 - S64
• Main Author: Porst, H
• Format: Journal Article
• Language: English
• Published: England Nature Publishing Group 01-02-2002
• Subjects: Carbolines; Clinical Trials as Topic; Drug dosages; Erectile dysfunction; Erectile Dysfunction - drug therapy; Humans; Male; Phosphodiesterase Inhibitors - administration & dosage; Tadalafil
• ISSN: 0955-9930; 1476-5489
• DOI: 10.1038/sj.ijir.3900807

IC351 (tadalafil, trade name Cialis) is a new representative compound of the second generation of selective phosphodiesterase 5 (PDE-5) inhibitors. The selectivity ratio vs PDE-5 is more than 10 000 for PDE-1 through PDE-4 and PDE-7 through PDE-10 and 780 for PDE-6. In the European daily-dosing trial, the efficacy rates were up to 93% for successful intercourses with completion in the 50-mg dose in patients with mild to moderate erectile dysfunction (ED). In two different dose-ranging studies with 2-25 mg taken as needed, efficacy rates of up to 88% improvement in erections and up to 73% successful intercourses with completion were achieved. In a placebo-controlled, fixed-dose (10- and 20-mg) trial in diabetic patients, improved erections of 56% and 64% were reported compared with 25% after placebo. Drug-related adverse effects, with headache in up to 23% of patients (placebo, up to 17%), dyspepsia in up to 11% (placebo, up to 7%), back pain in up to 4.7% (placebo, 0%), and myalgia in up to 4.1% (placebo, up to 2.4%), were mostly mild to moderate. Neither drug-related serious cardiovascular adverse events nor color vision disturbances were encountered. The long half-life (>17 h), with a comfortably long window of opportunity, releases couples from the need to plan sexual activities and therefore provides the highest amount of spontaneity for sexual activities.