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. 2022 Nov 8:16:3865-3876.
doi: 10.2147/DDDT.S387508. eCollection 2022.

Comparative Pharmacokinetics and Safety of Imrecoxib, a Novel Selective Cyclooxygenase-2 Inhibitor, in Elderly Healthy Subjects

Ling Yang #  1 , Qi Shen #  1 , Chao Hu  1 , Ying Wang  1 , Xiaohong Zhu  1 , Shiqing Shu  1 , Zhu Luo  1
Affiliations

Comparative Pharmacokinetics and Safety of Imrecoxib, a Novel Selective Cyclooxygenase-2 Inhibitor, in Elderly Healthy Subjects

Ling Yang et al. Drug Des Devel Ther. .

Abstract

Background: Imrecoxib is a novel and moderately selective cyclooxygenase-2 inhibitor with properties of anti-inflammation and alleviating pain, which is widely applied in osteoarthritis patients. The pharmacokinetic data supporting imrecoxib's rational use in elderly population are not available.

Purpose: The study aims to investigate the pharmacokinetics of imrecoxib and its main metabolites and explore the safety of imrecoxib in elderly healthy subjects.

Methods: A total of 19 healthy subjects including 10 non-elderly and 9 elderly subjects received single dose of 100 mg imrecoxib under fasting condition. Pharmacokinetics, safety and tolerability profiles were assessed.

Results: After oral administration of single dose of 100 mg imrecoxib, it was absorbed into plasma with median time to reach peak concentration (Tmax) around 2 hours. The concentration-time curves of imrecoxib (M0) showed higher interindividual variability in elderly subjects compared with non-elderly subjects. Peak concentration (Cmax) of M0, its hydroxyl metabolite M1 and carboxylated metabolite M2 in plasma increased by 39%, 21% and 17%, and area under concentration-time curve from time 0 to time t (AUC0-t) of M0, M1 and M2 in plasma increased by 34%, 13% and 27%, respectively, in elderly subjects compared with non-elderly subjects. The 90% CIs of geometric mean ratios of Cmax, AUC0-t and AUC0-∞ of M0, M1 and M2 between the two groups were not located within 80-125%, indicating Cmax, AUC0-t and AUC0-∞ were not completely equivalent between non-elderly and elderly healthy subjects. However, comparison of pharmacokinetic data of M0, M1 and M2 between the two groups showed no significant difference (P>0.05). Imrecoxib was well tolerated in both non-elderly and elderly healthy subjects, especially with favorable gastrointestinal and cardiovascular safety profiles.

Conclusion: Pharmacokinetic and safety profiles of imrecoxib in elderly healthy subjects indicated that no dose adjustment should be required for elderly population.

Keywords: cyclooxygenase-2 inhibitor; elderly; imrecoxib; pharmacokinetics; safety.

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Conflict of interest statement

All authors have no conflicts of interest to declare in this work.

Figures

Figure 1
Figure 1
The major metabolic process of imrecoxib.
Figure 2
Figure 2
The flowchart of the study.
Figure 3
Figure 3
Typical chromatograms of imrecoxib (M0), M1, M2 and IS. (A–D) Chromatograms of M1 and IS in (A) blank plasma; (B) blank plasma containing IS; (C) blank plasma containing M1 and IS at their LLOQ values; and (D) the plasma sample collected 1h after an oral administration of 100 mg imrecoxib. (E–H) Chromatograms of M0, M2 and IS in (E) blank plasma; (F) blank plasma containing IS; (G) blank plasma containing M0, M2 and IS at their LLOQ values; and (H) the plasma sample collected 1h after an oral administration of 100 mg imrecoxib. Peaks I–IV shows imrecoxib (M0), M1, M2 and IS (BAP385), respectively.
Figure 4
Figure 4
Individual and mean plasma concentration-time curves of imrecoxib (M0), M1 and M2. (A) The individual plasma concentration-time curves of M0, M1 and M2 in the non-elderly group (A1–A10). (B) The individual plasma concentration–time curves of M0, M1 and M2 in the elderly group (B1–B9). (C) The mean plasma concentration–time curves of M0, M1 and M2 in the non-elderly group (A) and elderly group (B).
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