Polmacoxib

Polmacoxib (trade name Acelex) is a nonsteroidal anti-inflammatory drug (NSAID) used to treat osteoarthritis. It was developed as CG100649 and approved for use in South Korea in February 2015.[1] It inhibits the enzymes carbonic anhydrase and COX-2. A study in healthy volunteers showed drug effects on urinary prostaglandin metabolites for both polmacoxib and celecoxib that suggest a similar cardiovascular risk profile.[2] Further work by this group developed dose-exposure relationships of polmacoxib to guide clinical development strategies.[3]

Polmacoxib
Clinical data
Trade namesAcelex
Other namesCG100649
ATC code
Identifiers
IUPAC name
  • 4-(3-(3-Fluorophenyl)-5,5-dimethyl-4-oxo-4,5-dihydrofuran-2-yl)-benzenesulfonamide
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC18H16FNO4S
Molar mass361.39 g·mol−1
3D model (JSmol)
SMILES
  • CC1(C(=O)C(=C(O1)C2=CC=C(C=C2)S(=O)(=O)N)C3=CC(=CC=C3)F)C
InChI
  • InChI=1S/C18H16FNO4S/c1-18(2)17(21)15(12-4-3-5-13(19)10-12)16(24-18)11-6-8-14(9-7-11)25(20,22)23/h3-10H,1-2H3,(H2,20,22,23)
  • Key:IJWPAFMIFNSIGD-UHFFFAOYSA-N

References
  1. "CrystalGenomics Receives MFDS Approval for Acelex (Polmacoxib)". PR Newswire.
  2. Skarke C, Alamuddin N, Lawson JA, Cen L, Propert KJ, Fitzgerald GA (June 2012). "Comparative impact on prostanoid biosynthesis of celecoxib and the novel nonsteroidal anti-inflammatory drug CG100649". Clinical Pharmacology and Therapeutics. 91 (6): 986–93. doi:10.1038/clpt.2012.3. PMC 3740579. PMID 22278334.
  3. Hirankarn S, Barrett JS, Alamuddin N, FitzGerald GA, Skarke C (October 2013). "GCG100649, A Novel Cyclooxygenase-2 Inhibitor, Exhibits a Drug Disposition Profile in Healthy Volunteers Compatible With High Affinity to Carbonic Anhydrase-I/II: Preliminary Dose-Exposure Relationships to Define Clinical Development Strategies". Clinical Pharmacology in Drug Development. 2 (4): 379–86. doi:10.1002/cpdd.47. PMID 27121942. S2CID 35992507.
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