Drug intelligence / Profile preview

linagliptin + rifampicin

Development stage
Unknown
Lead developer
Boehringer Ingelheim
Modality
Small Molecules
Administration
Oral
01

Overview

**Linagliptin + rifampicin** refers to the concurrent use of linagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor for type 2 diabetes mellitus, and rifampicin, a broad-spectrum antibiotic primarily used for tuberculosis and other bacterial infections. Linagliptin acts by inhibiting DPP-4, thereby increasing levels of incretin hormones, which improves insulin secretion and decreases glucagon concentrations in a glucose-dependent manner. Rifampicin is a potent inducer of cytochrome P450 3A4 and P-glycoprotein, markedly affecting the pharmacokinetics of many drugs, including linagliptin. Co-administration leads to a significant reduction in plasma concentrations and efficacy of linagliptin (AUC and Cmax reduced by about 40–44%). Therefore, this particular drug combination is not recommended or is considered contraindicated due to the risk of poor glycemic control from reduced linagliptin exposure[1][2][3].

Other names
linagliptin and rifampicin
02

Targets

CYP3A4 (Cytochrome P450 3A4)DPP-4 (Dipeptidyl Peptidase-IV)ABCB1 (P-glycoprotein)rpoB (DNA-directed RNA polymerase subunit beta)

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