TABLE 2 .
Prediction of hOCT2 DDIs following FDA decision tree
| Atenolol | Metformin | MPP+ | |
|---|---|---|---|
| hOCT2 | |||
| IC50 | 9.9 | 93.5 | 146b |
| Cimetidine unbound Cmax/IC50a | 0.8 | 0.09 | 0.05 |
| Recommendation for in vivo DDI study | Yes | Yes/No | No |
| hMATE1 | |||
| IC50 | 6.7 | 1.5 | 2.7b |
| Cimetidine unbound Cmax/IC50a | 1.2 | 5.3 | 3.0 |
| Recommendation for in vivo DDI study | Yes | Yes | Yes |
| hMATE2-K | |||
| IC50 | 7.1 | 9.7 | 4.0b |
| Cimetidine unbound Cmax/IC50 a | 1.1 | 0.8 | 2.0 |
| Recommendation for in vivo DDI study | Yes | Yes | Yes |
a
Cimetidine unbound Cmax = 8 μM was used for calculation. Value is from Brunton LL, Chabner BA, Knollman BC eds (2011) Goodman & Gilman’s The Pharmacological Basis of Therapeutics, 12th ed, McGraw-Hill Medical, New York.
b
Value is from Ito et al. (2012).