Evaluation of a pantoprazole and 4-desmethylpantoprazole-sulfate metabolic ratio as a novel CYP2C19 phenotyping method

Single-center randomized crossover pharmacokinetic study, 20 healthy volunteers, omeprazole (10 mg) vs pantoprazole (20 mg), validation of pantoprazole metabolic ratio as functional biomarker of CYP2C19 activity

This study validates the pantoprazole/4-desmethylpantoprazole-sulfate ratio as a new functional phenotyping probe for CYP2C19 activity, in a crossover pharmacokinetic study in 20 healthy volunteers receiving omeprazole (10 mg) or pantoprazole (20 mg). The pantoprazole metabolic ratio correlates with CYP2C19 metabolizer status (PM, IM, EM, UM) and could serve to detect in vivo phenoconversion, particularly during polypharmacy with CYP2C19 inhibitors or inducers.

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Functional CYP2C19 phenotyping by endogenous biomarkers or exogenous probes is a complementary approach to genotyping, particularly for detecting phenoconversion. This study provides a phenotyping probe based on a widely prescribed drug (pantoprazole), facilitating CYP2C19 activity measurement without additional sampling in polypharmacized populations.

Clinical impact: 2/3 · Evidence strength: 2/3 · Novelty: 2/2 · Sample size: 0/1 · Publication status: 1/1 → Total: 7/10