Polmacoxib information

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 ;
ChEMBL	ChEMBL166863;
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]

^ "CrystalGenomics Receives MFDS Approval for Acelex (Polmacoxib)" (Press release). PR Newswire.
^ 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.
^ 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.

[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.

Polmacoxib information

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Polmacoxib

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