Table 5.
SMCG | DECC | TTIT | RTTI | ARNL | TVEV | |
---|---|---|---|---|---|---|
Absorption | ||||||
Blood-brain barrier | BBB+ | BBB+ | BBB+ | BBB+ | BBB+ | BBB+ |
Human intestinal absorption | HIA- | HIA- | HIA- | HIA- | HIA+ | HIA- |
Caco-2 permeability | Caco-2- | Caco-2- | Caco-2- | Caco-2- | Caco-2- | Caco-2- |
P-Glycoprotein substrate | Substrate | Nonsubstrate | Nonsubstrate | Nonsubstrate | Substrate | Nonsubstrate |
P-Glycoprotein inhibitor | Noninhibitor | Noninhibitor | Noninhibitor | Noninhibitor | Noninhibitor | Noninhibitor |
Renal organic Cation transporter | Noninhibitor | Noninhibitor | Noninhibitor | Noninhibitor | Noninhibitor | Noninhibitor |
Metabolism | ||||||
CYP3A4 substrate | Substrate | Nonsubstrate | Nonsubstrate | Nonsubstrate | Substrate | Nonsubstrate |
CYP2C9 substrate | Nonsubstrate | Nonsubstrate | Nonsubstrate | Nonsubstrate | Substrate | Nonsubstrate |
CYP2D6 substrate | Nonsubstrate | Nonsubstrate | Nonsubstrate | Nonsubstrate | Nonsubstrate | Nonsubstrate |
CYP3A4 inhibition | Noninhibitor | Noninhibitor | Noninhibitor | Noninhibitor | Noninhibitor | Noninhibitor |
CYP2C9 inhibition | Noninhibitor | Noninhibitor | Noninhibitor | Noninhibitor | Noninhibitor | Noninhibitor |
CYP2C19 inhibition | Noninhibitor | Noninhibitor | Noninhibitor | Noninhibitor | Noninhibitor | Noninhibitor |
CYP2D6 inhibition | Noninhibitor | Noninhibitor | Noninhibitor | Noninhibitor | Noninhibitor | Noninhibitor |
CYP1A2 inhibition | Noninhibitor | Noninhibitor | Noninhibitor | Noninhibitor | Noninhibitor | Noninhibitor |
Toxicity | ||||||
AMES toxicity | Non-AMES toxic | Non-AMES toxic | Non-AMES toxic | Non-AMES toxic | Non-AMES toxic | Non-AMES toxic |
Carcinogens | Noncarcinogens | Noncarcinogens | Noncarcinogens | Noncarcinogens | Noncarcinogens | Noncarcinogens |