Table 2. Biochemical and Pharmacokinetic Data for Marketed Selective PDE5 Inhibitors113 a.
| compd |
|||
|---|---|---|---|
| 7 | 8 | 9 | |
| half-life (h) | 4–5 | ∼4 | 17.5 |
| bioavailability | ∼15% | ∼40% | N.D. |
| Cmax (approx, nM) | 36b | 950c | 771b |
| logBB32,151 | –1.4d | –1.3d | –1d, −0.89e |
| IC50 (nM)152 | 0.14 | 3.5 | 6.7 |
| selectivity152 f | 4-fold vs PDE6 | 10-fold vs PDE6 | 5-fold vs PDE11 |
a
The half-life, bioavailability, and Cmax data were obtained from official information provided by the relevant pharmaceutical companies (7,1488,149 and 9(150)).
b
Single oral dose (20 mg).
c
Single oral dose (100 mg).
d
Determined in rats.
e
Determined in mice.
f
Selectivity with respect to the second isoform for which the compound exerts significant inhibition.