Table 1 Physicochemical guidelines for designing macrocyclic drugs (Villar et al.14).
Property | Conventional drugs | Oral macrocyclic drugs | Non-oral macrocyclic drugs |
|---|---|---|---|
MolW | \(\:\le\:\) 500 | 600–1200 | 600–1300 |
clogP | \(\:\le\:\) 5 | -2 to 6 | -7 to 2 |
PSA | \(\:\le\:\) 140 Å2 | 180–320 Å2 | 150–500 Å2 |
No. of HBDs | \(\:\le\:\) 5 | \(\:\le\:\) 12 | \(\:\le\:\) 17 |
No. of HBAs | \(\:\le\:\) 10 | 12–16 | 9–20 |
NRB value | \(\:\le\:\) 10 | \(\:\le\:\) 15 | \(\:\le\:\) 30 |
