Table 5.
Peptides | ||||||||
---|---|---|---|---|---|---|---|---|
LIVA | TSEP | EKAI | LKHA | EALF | VAEK | DFGAS | EPGGGG | |
Absorption | ||||||||
BBB | + | + | + | + | – | + | + | + |
HIA | – | – | – | + | + | – | – | + |
Caco-2 permeability | Caco-2- | Caco-2- | Caco-2- | Caco-2- | Caco-2- | Caco-2- | Caco-2- | Caco-2- |
PGS | Substrate | NS | Substrate | Substrate | Substrate | NS | NS | Substrate |
PGI | NI | NI | NI | NI | NI | NI | NI | NI |
ROCT | NI | NI | NI | NI | NI | NI | NI | NI |
| ||||||||
Metabolism | ||||||||
CYP3A4 substrate | Substrate | NS | Substrate | Substrate | NS | NS | NS | Substrate |
CYP2C9 substrate | NS | NS | Substrate | NS | NS | NS | NS | Substrate |
CYP2D6 substrate | NS | NS | NS | NS | NS | NS | NS | NS |
CYP3A4 inhibition | NI | NI | NI | NI | NI | NI | NI | NI |
CYP2C9 inhibition | NI | NI | NI | NI | NI | NI | NI | NI |
CYP2C19 inhibition | NI | NI | NI | NI | NI | NI | NI | NI |
CYP2D6 inhibition | NI | NI | NI | NI | NI | NI | NI | NI |
CYP1A2 inhibition | NI | NI | NI | NI | NI | NI | NI | NI |
| ||||||||
Toxicity | ||||||||
Ames toxicity | NAT | NAT | NAT | NAT | NAT | NAT | NAT | NAT |
Carcinogens | NC | NC | NC | NC | NC | NC | NC | NC |
BBB: blood-brain barrier; HIA: human intestinal absorption; PGS: P-glycoprotein substrate; PGI: P-glycoprotein inhibitor; ROCT: renal organic cation transporter; NS: nonsubstrate; NI: noninhibitor; NAT: non-Ames toxic; NC: noncarcinogenic.