Park SR, et al. Transl Clin Pharmacol. 2024 Mar;32(1):63-72. https://doi.org/10.12793/tcp.2024.32.e6

Envlo (enavogliflozin) 0.3 mg, an SGLT2 inhibitor, was approved in Korea in 2022 for glycemic control in type 2 diabetes (T2DM). This study evaluates its safety, pharmacokinetics, and food effects. Healthy subjects (age ≥ 19, weight ≥ 50.0 kg, body mass index (BMI) 18.0–30.0 kg/m ² ) were enrolled. Study I was a randomized, two‐way crossover study with an 8‐day washout, where subjects received either a separate or a fixed‐dose combination (FDC) of enavogliflozin 0.3 mg/gemigliptin 50 mg. Study II, a randomized, open‐label, two‐way crossover design with a 7‐day washout, compared the food effect of a single dose of enavogliflozin in fed versus fasted after a high‐fat meal. In study I, enavogliflozin reached peak plasma concentration at 1.25 h (median) in both groups. The mean half‐life ( t _1/2 ) was also comparable, recorded as 12.56 ± 4.04 h for the separate combination and 12.23 ± 3.46 h for the FDC. Gemigliptin peaked at 2.00 h in the separate combination and at 3.00 h in the FDC. The mean t _1/2 was 18.04 ± 1.75 h for the separate combination and 18.67 ± 2.54 h for the FDC. In study II, the plasma concentration of enavogliflozin 0.3 mg peaked at 1.25 and 2.00 h (median), indicating a delayed T _max in the fed group. The average t _1/2 was similar at 12.49 ± 2.12 h and 12.30 ± 2.81 h, respectively. The FDC of enavogliflozin and gemigliptin demonstrated pharmacokinetic equivalence and comparable safety to their co‐administration as separate agents. Furthermore, the systemic exposure of enavogliflozin was not affected by food intake, supporting its potential for flexible, meal‐independent use in clinical settings.

Compared to pelubiprofen, a cyclooxygenase-2-selective inhibitor, pelubiprofen tromethamine has been reported to exhibit improved solubility and absorption. Pelubiprofen tromethamine combines the anti-inflammatory effect of pelubiprofen with the gastric protective function of tromethamine salt, making it a relatively safe class of non-steroidal anti-inflammatory drugs with low levels of gastrointestinal side effects in addition to its original analgesic, anti-inflammatory, and antipyretic effects. This study assessed the pharmacokinetic and pharmacodynamic characteristics of pelubiprofen and pelubiprofen tromethamine in healthy subjects. Two independent clinical trials were performed in healthy subjects using a randomized, open-label, oral, single-dose, two-sequence, four-period, crossover design. In Study I and Study II, subjects received 25 mg of pelubiprofen tromethamine and 30 mg of pelubiprofen tromethamine, respectively, with 30 mg of pelubiprofen being the reference. Study I fell within the bioequivalence study criteria. A trend of increased absorption and exposure for 30 mg of pelubiprofen tromethamine vs. the reference in Study II was observed. The maximum cyclooxygenase-2 inhibitory effect of 25 mg of pelubiprofen tromethamine was approximately 98% compared to the reference, showing no significant pharmacodynamic variation. It is thus predicted that 25 mg of pelubiprofen tromethamine would show no clinically significant discrepancies in clinical analgesic and antipyretic effects from 30 mg of pelubiprofen.