CYP2C8 inhibitors, inducers and substrates

CYP2C8 is a liver enzyme that clears repaglinide, pioglitazone and montelukast. Gemfibrozil is a strong inhibitor, and clopidogrel inhibits it too.

This is the desk's mapped set for CYP2C8, taken from the same catalog the desk uses to grade pairs. It is not a complete list. A drug that isn't listed here hasn't been cleared as safe; it just isn't on this list.

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What inhibition and induction mean

Inhibition. An inhibitor slows CYP2C8. Drugs that depend on CYP2C8 can build up, so their levels and effects can rise. Reversible inhibition starts as the inhibitor builds up and fades as it clears. Some inhibitors destroy the enzyme, and the effect lasts until the body makes more.

Induction. An inducer makes the body produce more CYP2C8. Levels of drugs that depend on CYP2C8 can fall, and so can their effect. Induction builds over days to weeks and takes about as long to fade after the inducer stops.

Strong, moderate and weak are the desk's grades for how much a perpetrator changes a sensitive substrate's exposure, in FDA's fold-change bins. FDA table of substrates, inhibitors and inducers.

Names with a solid underline open that drug's page of label-sourced pairs. Names with a dotted underline open the desk with that drug.

CYP2C8 inhibitors (15)

Strong inhibitors (1)

≥5-fold ↑ AUC of a sensitive index substrate

Gemfibrozil

Moderate inhibitors (8)

≥2 to <5-fold ↑ AUC

Weak inhibitors (6)

≥1.25 to <2-fold ↑ AUC

CYP2C8 inducers (3)

Moderate inducers (1)

≥50 to <80% ↓ AUC

Rifampin

Weak inducers (2)

≥20 to <50% ↓ AUC

CYP2C8 substrates (15)

Sensitive substrates (2)

Exposure rises the most when CYP2C8 is blocked.

Major-pathway substrates (10)

CYP2C8 is one of the main routes for these.

Minor-pathway substrates (3)

CYP2C8 is a smaller route for these; other routes carry most of the load.

Educational reference only. Not FDA-cleared. The Prescribing Information governs.