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. 2020 Feb 4;177(24):5467–5488. doi: 10.1111/bph.14920

TABLE 1.

PDE5I pharmacokinetic and pharmacodynamic comparison

PDE5I Pharmacokinetics Pharmacodynamics
Dose (mg) T max (hr) t ½ (hr) C max (ng·ml−1) AUC (ng × hr·ml−1) MW (g·mol−1) MF IC50 for PDE5 (nmol·L−1) PDE selectivity
Sildenafil 100 0.95 3.98 514 1,670 475 C22H30N6O4S 3.7 Low activity against PDE6; very low activity against PDE1.
Tadalafil 20 2 17.5 378 8,066 389 C22H19N3O4 1.8 Low activity against PDE11; very low activity against PDE6.
Vardenafil FCT 20 0.66 3.9 20.9 74.5 488 C23H32N6O4S 0.091 Low activity against PDE6; very low activity against PDE1.
Avanafil 200 0.75 5.1 2,920 8,490 484 C23H26CIN7O3 5.2 Highly selective for PDE5.
Udenafil 200 0.76 9.88 1,137 7,898 517 C25H36N6O4S 8.25 Comparable to sildenafil for PDE5.
Mirodenafil 100 1.4 2.5 2,989 7,907 532 C26H37N5O5S 0.33 Comparable to sildenafil for PDE5.
Lodenafil 160 1.2 2.4 157 530 1,035 C47H62N12O11S2 0.015 Low activity against PDE1 and PDE6.
PF‐00489791 20 1.1–3.5 11.9–15.7 1,570–1,630 N/A 477 C20H28N8O4S 0.71 Highly selective for PDE5.

Note. Data sourced from Clerin, Gale, & Tamimi (2014) and Hatzimouratidis, Salonia et al. (2016).

Abbreviations: AUC, area under the plasma drug concentration‐time curve; C max, maximum plasma serum concentration; FCT, film‐coated tablet; IC50, half maximal inhibitory concentration; MF, molecular formula; PDE5I, PDE type 5 inhibitor; t ½, terminal plasma half‐life; T max, time taken to reach the maximum plasma concentration.