Drug intelligence / Profile preview

LC15-0444 + ketoconazole

Development stage
Unknown
Lead developer
LG Chem
Modality
Small Molecules
Administration
Oral
01

Overview

The combination **LC15-0444 + ketoconazole** consists of gemigliptin (LC15-0444), a highly selective, reversible, and competitive inhibitor of dipeptidyl peptidase-4 (DPP-4) indicated for the treatment of type 2 diabetes mellitus, and ketoconazole, an imidazole antifungal that acts as a potent cytochrome P450 3A4 (CYP3A4) inhibitor. Gemigliptin inhibits DPP-4, thereby increasing levels of incretin hormones, which leads to reduced blood glucose levels. Ketoconazole inhibits fungal ergosterol synthesis and also CYP3A4, resulting in altered metabolism and increased gemigliptin plasma exposure when co-administered. The combination is primarily studied for pharmacokinetic interactions, highlighting the need for dose adjustment of gemigliptin when given with strong CYP3A4 inhibitors such as ketoconazole[1][2][4][8].

Brand names
gemigliptinNizoral
Other names
gemigliptin tartrateLC15-0444 tartrateLC-15-0444 tartrateLC 15-0444 tartrateNizoral
02

Targets

CYP51A1 (Sterol 14α-demethylase)CYP3A4 (Cytochrome P450 3A4)DPP-4 (Dipeptidyl Peptidase-IV)

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