Homosildenafil
Homosildenafil
Chemical compound
Homosildenafil (also known as methyl-sildenafil) is a synthetic drug which acts as a phosphodiesterase inhibitor.[1] It is an analog of sildenafil and vardenafil. Homosildenafil was first identified as an adulterant in sex enhancement products in 2003 and was more recently detected in dietary supplements.[2][3][4][5]
Homosildenafil has 35% the PDE5 inhibition activity of sildenafil itself with similar selectivity.[1]
Sildenafil is mainly metabolized by the microsomal isozymes CYP3A4 with secondary metabolism by CYP2C9. The major active metabolite is N-desmethylsildenafil. The plasma level of the equivalent homosildenafil metabolite reaches 40% of sildenafil's bioavailability. The N-desmethyl metabolite is further metabolized, with a half-life of 4 hours.[6][7][8][9]