ReviewClinical pharmacokinetics2026
Clinical Pharmacokinetics of Polmacoxib (CG100649): A Tissue-Selective Dual COX-2 and Carbonic Anhydrase I/II Inhibitor.
Review in Clinical pharmacokinetics, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
0 citing papers in PubMed.
No citing paper in PubMed yet.
Corrections and comments
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Authors and funding
6 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Polmacoxib (CG100649; Acelex) is a first-in-class non-steroidal anti-inflammatory drug that combines selective cyclooxygenase-2 (COX-2) inhibition with high-affinity binding to carbonic anhydrase I/II (CA-I/II). Approved for osteoarthritis in South Korea (2015) and India (2023), it exhibits pharmacokinetic (PK) properties distinct from other coxibs. The objective of this review is to review the clinical PK and pharmacokinetic-pharmacodynamic (PK-PD) profile of polmacoxib, compare it with other coxibs, and identify key evidence gaps. PubMed, Embase, Scopus, Web of Science, Google Scholar, and ClinicalTrials.gov were searched through June 2026, supplemented by reference lists and regulatory, patent, and Protein Data Bank records. The clinical PK profile of polmacoxib is dominated by erythrocyte sequestration via high-affinity binding to CA-I/II. After oral dosing, whole-blood concentrations exceed plasma concentrations by approximately 50-78 on average, with individual values approaching 120-fold, and terminal half-lives are approximately 121-203 h in blood and 100-167 h in plasma. A 2-compartment whole-blood model with mixed zero- and first-order absorption best describes the data, with serum iron, white-cell count, and age identified as covariates of clearance. The 2-mg once-daily dose substantially inhibits thromboxane B2 and ex vivo PGE2, with only modest, dose-dependent inhibition of urinary prostacyclin metabolite (PGI-M) that is of comparable magnitude, although less sustained, to celecoxib 200 mg after single dosing; the 2-mg dose is noninferior to celecoxib 200 mg on WOMAC pain endpoints in osteoarthritis. Ketoconazole produces only modest changes in plasma exposure, and PK data in hepatic impairment, renal impairment, older people, and non-Korean populations remain limited. Polmacoxib has a unique PK profile among coxibs, driven by erythrocyte carbonic anhydrase binding, which supports its proposed tissue-selective pharmacology. Further studies in special populations, drug-drug interactions, and post-marketing settings are needed to support broader global use.
Identifiers
42879101What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.