gemfibrozil and glibenclamide: label evidence and limits

The gemfibrozil label names glyburide, also called glibenclamide, among OATP1B1 substrates whose exposure may increase when this transporter is inhibited.

Which products this evidence covers

Oral gemfibrozil tablets; glyburide/glibenclamide identity.

What this finding does and does not establish

The label discusses possible clinician-directed dose reduction. CDI’s severity category is not an FDA-assigned rating.

Supporting label passage

Gemfibrozil is an inhibitor of OATP1B1 transporter and may increase exposure of drugs that are substrates of OATP1B1 (e.g., atrasentan, atorvastatin, bosentan, ezetimibe, fluvastatin, glyburide, SN-38 [active metabolite of irinotecan], rosuvastatin, pitavastatin, pravastatin, rifampin, valsartan, olmesartan). Therefore, dosing reductions of drugs that are substrates of OATP1B1 may be required when gemfibrozil is used concomitantly (see WARNINGS ). Combination therapy of gemfibrozil with simvastatin or with repaglinide, which are OATP1B1 substrates, is contraindicated (see CONTRAINDICATIONS ).

Read the product label on DailyMed. Section: Drug Interactions — OATP1B1 substrates. Compared label version 102, dated 2023-10-24.

How this brief was prepared

This brief uses an AI-assisted source comparison dated 2026-10-16. The label version and supporting passage were checked again on 2026-10-25. Independent clinical review has not been recorded. The comparison does not validate CDI's severity category or determine individual treatment.

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