Pharmacokinetics and bioequivalence of 0.5 mg lobeglitazone tablets in healthy male subjects

Abstract

This study suggests that the two lobeglitazone tablet formulations have similar exposure and absorption rates. Therefore, the newly-developed formulation of the 0.5-mg DuvieTM tablet is expected to contribute to the treatment of patients with type 2 diabetes. .

Effects of Hepatic Impairment on the Pharmacokinetic Profile and Safety of Lobeglitazone

“…12 Lobeglitazone is transformed by liver enzymes mainly to M7 (O-demethylated from), which is further metabolized to M5 (di-demethylated form) partially in humans. 14,15 The PK properties of lobeglitazone are proportional for the range from 1 to 4 mg orally when given once a day. 13 In healthy men and women, orally administered 2 mg of lobeglitazone is well-tolerable and no sex difference for systemic exposure.…”

“…The primary metabolic pathways are demethylation and hydroxylation by cytochrome P450 (CYP) isozymes, such as 2D6, 2C19, and 3A4 12 . Lobeglitazone is transformed by liver enzymes mainly to M7 ( O ‐demethylated from), which is further metabolized to M5 (di‐demethylated form) partially in humans 14,15 …”