Polmacoxib

Polmacoxib

Clinical data
Trade names	Acelex
Other names	CG100649
ATC code	M01AH07 ( WHO )
Identifiers
IUPAC name 4-(3-(3-Fluorophenyl)-5,5-dimethyl-4-oxo-4,5-dihydrofuran-2-yl)-benzenesulfonamide
CAS Number	301692-76-2
PubChem CID	9841854
ChemSpider	8017569
UNII	IJ34D6YPAO
KEGG	D10656  Y
ChEMBL	ChEMBL166863
CompTox Dashboard (EPA)	DTXSID901029389
Chemical and physical data
Formula	C18H16FNO4S
Molar mass	361.39 g·mol−1
3D model (JSmol)	Interactive image
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

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]

References

1. "CrystalGenomics Receives MFDS Approval for Acelex (Polmacoxib)" (Press release). 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.