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CYP2B6 inhibitors, inducers and substrates

CYP2B6 is a liver enzyme that clears bupropion, efavirenz and ketamine, and it carries part of methadone's clearance. Its gene varies widely between people, which changes how fast these drugs are cleared.

This is the desk's mapped set for CYP2B6, 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 CYP2B6. Drugs that depend on CYP2B6 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 CYP2B6. Levels of drugs that depend on CYP2B6 can fall, and so can their effect. Induction builds over days to weeks and takes about as long to fade after the inducer stops.

Substrates marked activation pathway are ones CYP2B6 turns into an active or reactive product. For these, inhibition can mean less of that product, and induction can mean more.

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.

CYP2B6 inhibitors (3)

Moderate inhibitors (1)

≥2 to <5-fold ↑ AUC

Weak inhibitors (2)

≥1.25 to <2-fold ↑ AUC

CYP2B6 inducers (11)

Strong inducers (1)

≥80% ↓ AUC of a sensitive index substrate

Moderate inducers (5)

≥50 to <80% ↓ AUC

Weak inducers (5)

≥20 to <50% ↓ AUC

CYP2B6 substrates (14)

Sensitive substrates (1)

Exposure rises the most when CYP2B6 is blocked.

Major-pathway substrates (9)

CYP2B6 is one of the main routes for these.

Minor-pathway substrates (4)

CYP2B6 is a smaller route for these; other routes carry most of the load.

Pair pages that run through CYP2B6 (2)

Label-sourced pair pages where the desk's top finding is a CYP2B6 interaction, grouped by the desk's grade.

Serious concern (2)

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