Table 1. Table Summarizing the LipMetE, LipE, log D7.4, and log10CLint,u Ranges for the CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 Substrate datasets That Were Used for LipMetE Calculationsa.
known
drugs and model substrates data
(LipMetE 0–2.5) |
||||||||||
---|---|---|---|---|---|---|---|---|---|---|
CYP450 | LipE range | LipMetE range | log D7.4 range | log10CLint,u range | no of substrates with LipMetE between 0 and 2.5 | LipE range | average LipE | average LipMetE | average log D7.4 | average log10CLint,u |
CYP1A2 | –1.96 to 7.24 | –4.54 to 4.35 | –1.19 to 4.24 | –3.08 to 4.72 | 8 | –1.96 to 3.03 | 0.88 | 0.94 | 2.25 | 1.28 |
CYP2C9 | –1.02 to 5.01 | –3.72 to 3.63 | –0.98 to 5.92 | –0.015 to 5.18 | 6 | –0.83 to 2.73 | 1.00 | 0.69 | 2.63 | 1.94 |
CYP2C19 | –4.20 to 5.13 | –6.40 to 4.70 | –1.29 to 5.68 | –1.87 to 6.49 | 3 | –2.18 to 0.95 | –0.15 | 0.70 | 2.73 | 2.02 |
CYP2D6 | –1.18 to 4.73 | –6.35 to 2.93 | –2.01 to 5.09 | –0.53 to 6.72 | 11 | –1.14 to 2.17 | 0.50 | 1.03 | 2.48 | 1.46 |
CYP3A4 | –2.36 to 6.66 | –6.19 to 3.85 | –1.26 to 5.16 | –3.08 to 7.27 | 23 | –1.98 to 2.72 | 0.85 | 0.75 | 2.64 | 1.89 |
The average values for LipMetE, LipE, log D7.4, and log10CLint,u have been derived using drugs and model substrates from each dataset with better metabolic profiles (LipMetE 0–2.5).