GI & Hepatobiliary Library
Gastrointestinal and Hepatobiliary Drugs DMPK and Bioanalytical Services
GI drug bioanalysis splits across two distinct domains. Four PPIs — omeprazole, esomeprazole, pantoprazole, and lansoprazole — are CYP2C19 and CYP3A4 substrates requiring NADPH-supplemented microsome incubation. Among them, omeprazole and esomeprazole are also CYP2C19 inhibitors, requiring inhibitor-aware controls that pure-substrate pantoprazole and lansoprazole do not need. The remaining four compounds — famotidine, ranitidine, ursodeoxycholic acid, and obeticholic acid — are non-metabolized, excreted unchanged via renal or biliary routes, requiring no CYP or UGT incubation at all. One CYP2C19 protocol serves four PPIs but misses the inhibitor dimension for two of them, and has zero relevance to the four non-metabolized compounds.
Creative Proteomics provides CYP2C19/CYP3A4 PPI metabolism, CYP2C19 inhibitor DDI profiling for omeprazole and esomeprazole, non-metabolized GI compound disposition, and custom multi-mechanism GI drug panels.
Four PPIs: CYP2C19 + CYP3A4Omeprazole, esomeprazole, pantoprazole, lansoprazole — CYP2C19/3A4 substrates requiring NADPH incubation.
Two PPIs Are Also CYP2C19 InhibitorsOmeprazole and esomeprazole suppress CYP2C19 probe activity. Standard incubation for pantoprazole/lansoprazole does not apply.
Four Non-Metabolized CompoundsFamotidine, ranitidine, UDCA, OCA — excreted unchanged. No CYP or UGT incubation needed.
GI Drug Mechanism Divide DMPK Strategy Map
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Two-Domain ClassificationFour PPIs (CYP2C19/3A4, two of which are also CYP2C19 inhibitors) and four non-metabolized compounds — two analytical strategies, eight compounds.
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CYP2C19 PPI Metabolism + Inhibitor DDIAll four PPIs require CYP2C19/3A4 NADPH incubation. Omeprazole and esomeprazole need additional inhibitor-compensated controls for CYP2C19 probe suppression.
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Non-Metabolized GI, H2, and Bile Acid AgentsFamotidine/ranitidine (H2 antagonists) and UDCA/OCA (bile acids) — excreted unchanged via renal or biliary routes. No CYP/UGT incubation.
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CYP2C19 Polymorphism ContextCYP2C19 is polymorphic like CYP2D6 (beta-blockers). PPI metabolism varies by genotype — genotyped microsome models recommended.
GI drug mechanism audit before method development.Creative Proteomics classifies each compound as CYP2C19/3A4 PPI (with or without inhibitor status) or non-metabolized GI/bile acid agent — because omeprazole needs inhibitor compensation and famotidine needs no metabolism at all.
