Strengths and weaknesses of the recommended probe compounds
| In Vitro | In Vivo | |||||
|---|---|---|---|---|---|---|
| Probe | Strengths | Weaknesses | Probe | Strengths | Weaknesses | |
| Substrate | Amodiaquine | Selectivity, high turnover | Repaglinide | Sensitivity, short half-life | Reduces blood glucose levels, also a substrate of OATP1B1 and CYP3A4 | |
| Paclitaxel | Selectivity, extensive documentation | Low/intermediate turnover, solubility issues | Montelukast | Relative sensitivity, safety | Medium long half-life | |
| Montelukast | Selectivity | Contribution by CYP2C9, requirement for very low substrate concentration, issues with protein binding | Pioglitazone | Relative sensitivity, safety, not a substrate of OATP1B1 | Long half-life | |
| Cerivastatin (acid) | Selectivity | Availability of reference compounds | ||||
| Repaglinide | Selectivity | Lack of metabolite standards, contribution by CYP3A4, requirement for low substrate concentration | Rosiglitazone | Safety, not a substrate of OATP1B1 | Only moderate sensitivity, long half-life, not easily available in all countries | |
| Pioglitazone | Selectivity | Low/intermediate turnover | Dasabuvir | Sensitive | Lack of documentation | |
| Rosiglitazone | Selectivity | Low/intermediate turnover | ||||
| Inhibitor | Gemfibrozil 1-O-β glucuronide | Potency | Selectivity not well documented, requires a preincubation | Gemfibrozil | Strength, selectivity | Moderate inhibitor of OATP1B1 and OAT3 |
| Clopidogrel acyl 1-β-D-glucuronide | Selectivity not documented, requires a preincubation | Clopidogrel | Strength, not an inhibitor of OATP1B1 or CYP3A4 | Also CYP2B6 inhibitor | ||
| Montelukast | Potency, selectivity | Also a substrate of CYP2C8, microsomal protein binding | Trimethoprim | Selectivity | Weak inhibitor | |
| Inducer | Rifampin (Rifampicin) | Potency, well-documented inducer | Nonselective | Rifampin (Rifampicin) | Strong, well-documented inducer | Nonselective |