Selectivity of avanafil, a PDE5 inhibitor for the treatment of erectile dysfunction: implications for clinical safety and improved tolerability.

摘要: ABSTRACT Introduction Phosphodiesterase type 5 (PDE5) inhibitors are indicated for the treatment of erectile dysfunction (ED); however, they can also inhibit other PDE isozymes, affecting their target tissues (e.g., PDE1: heart; PDE6: retina; and PDE11: skeletal muscle), which in some cases cause unwanted side effects therapy discontinuation. Data from vitro studies showed that avanafil, a PDE5 inhibitor ED, exhibited strong selectivity toward against all isozymes. Aim To review inhibitory avanafil isozymes compared with those sildenafil, tadalafil, vardenafil to discuss these results within context clinical trial safety observations. Methods Review data (published primary peer‐reviewed journal scientific congress abstracts); PubMed search pertinent publications on data; published articles abstracts phase 1, 2, 3 trials. Main Outcome Measures A low incidence PDE‐related adverse events may be reflected by high non‐PDE5 Results Avanafil is highly selective tested. Lower PDE1, PDE6, PDE11 consistent randomized, placebo‐controlled, trials musculoskeletal hemodynamic were reported Conclusions suggest confer benefit, terms lower specific events, virtue its specificity overall Wang R, Burnett AL, Heller WH, Omori K, Kotera J, Kikkawa Yee S, Day WW, DiDonato Peterson CA. Selectivity dysfunction: Implications improved tolerability. J Sex Med 2012;9:2122–2129.