Glipten Drug Interactions

CYP3A4 and flavin monooxygenase 3 (FMO3) are the major and CYP2D6 and flavin monooxygenase 1 (FMO1) are the minor hepatic enzymes responsible for the metabolism of Teneligliptin. Teneligliptin is a weak inhibitor of CYP2D6, CYP3A4, and FMP (IC50 values; 489.4, 197.5, and 467.2 µmol/L, respectively) but shows no inhibitory effect on CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C8/9, CYP2C19, and CYP2E1. Teneligliptin does not induce CYP3A4 or CYP1A2.
Ketoconazole (400 mg) a potent inhibitor of CYP3A4 increased C_max and AUC of Teneligliptin by 1.37-fold and 1.49-fold, respectively which was less than 2-fold and not considered clinically significant (see Tables 8 and 9). The half-life (t_1/2) of Teneligliptin was unchanged with ketoconazole coadministration. The combination of Teneligliptin with drugs and food that inhibit CYP3A4 are not expected to cause marked, clinically significant increases in the exposure to Teneligliptin. No dose adjustments are required.
The pharmacokinetics of Teneligliptin is not significantly affected by coadministration with pioglitazone or metformin. Teneligliptin does increase the exposure to metformin by a non-clinically relevant 20.5% (see Tables 8 and 9). No dosage adjustment is needed when Teneligliptin is combined with either pioglitazone or metformin.
When coadministered, neither Teneligliptin nor glimepiride affect each other's pharmacokinetic profile in any clinically meaningful way (see Tables 8 and 9). The risk of hypoglycemia may be increased when Teneligliptin is used concomitantly with insulin and insulin secretagogues such as sulfonylureas and glinides. The dosage of insulin or the insulin secretagogue should be adjusted.

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