Linagliptin is a substrate for CYP 3A4, and in vitro studies have shown that it is a weak competitive and mechanism-based inhibitor of CYP 3A4. The week inhibitory effect is not expected or found to have clinical relevance, and it is also regarded as insignificant in relevance of having any porphyrinogenic potential.

Linagliptin is a dipeptidyl peptidase-4 inhibitor.

Linagliptin is indicated in the treatment of type 2 diabetes mellitus to improve glycaemic control in adults. It is administered orally.

Linagliptin is a substrate of CYP 3A4, but most of the drug is excreted unchanged. Linagliptin does not induce any CYP enzymes (Sheen 2010, SPC, Tornio 2012). In an in vitro study linagliptin was identified as a weak competitive and a moderate to poor mechanism-based inhibitor of CYP3A4. Linagliptin is not expected to cause clinically significant CYP related drug-drug interactions (Blech 2010, Golightly 2012), and is not listed as a perpetrator drug in interaction databases. Linagliptin had no clinically relevant effects on the pharmacokinetics of the CYP3A4 substrate simvastatin (Graefe-Mody 2010). Concomitant administration of linagliptin and warfarin had no clinically relevant effect on the pharmacokinetics and pharmacodynamics of warfarin (Graefe-Mody 2011a). Coadministration of linagliptin and glyburide showed no clinically relevant inhibition CYP2C9 or CYP3A4 (Graefe-Mody 2011b).