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The following term was not found in PubMed: CG1-00649
Page 1
An update on drug interaction considerations in the therapeutic use of carbonic anhydrase inhibitors.
Supuran CT. Supuran CT. Expert Opin Drug Metab Toxicol. 2020 Apr;16(4):297-307. doi: 10.1080/17425255.2020.1743679. Epub 2020 Mar 21. Expert Opin Drug Metab Toxicol. 2020. PMID: 32172611 Review.
An update on their drug-drug interactions is presented here considering these main therapeutic areas and drugs: glaucoma (acetazolamide, methazolamide, dichlorophenamide, dorzolamide, and brinzolamide); epilepsy/obesity (sulthiame, topiramate, and zonisamide); arthritis/inflammat …
An update on their drug-drug interactions is presented here considering these main therapeutic areas and drugs: glaucoma (acetazolamide, met …
Drug interaction considerations in the therapeutic use of carbonic anhydrase inhibitors.
Supuran CT. Supuran CT. Expert Opin Drug Metab Toxicol. 2016;12(4):423-31. doi: 10.1517/17425255.2016.1154534. Epub 2016 Mar 3. Expert Opin Drug Metab Toxicol. 2016. PMID: 26878088 Review.
Acetazolamide, methazolamide, dichlorophenamide, dorzolamide and brinzolamide are mainly used as antiglaucoma drugs, sulthiame, topiramate and zonisamide as antiepileptic/antiobesity agents, celecoxib and polmacoxib are dual carbonic anhydrase/cycloxygenase inhibitors. Gir …
Acetazolamide, methazolamide, dichlorophenamide, dorzolamide and brinzolamide are mainly used as antiglaucoma drugs, sulthiame, topiramate a …
Population Pharmacokinetic and Pharmacodynamic Analysis of Polmacoxib in Healthy Volunteers and Patients With Osteoarthritis.
Cho YS, Bae KS, Choi SC, Cho JM, Lim HS. Cho YS, et al. Clin Ther. 2022 Jan;44(1):67-80.e1. doi: 10.1016/j.clinthera.2021.11.008. Epub 2021 Dec 31. Clin Ther. 2022. PMID: 34974943
PURPOSE: Polmacoxib, a new coxib dually inhibiting cyclooxygenase-2 and carbonic anhydrase I/II, was recently approved for osteoarthritis treatment in South Korea. ...Iron concentration was the significant covariate associated with clearance of polmacoxib. The relat …
PURPOSE: Polmacoxib, a new coxib dually inhibiting cyclooxygenase-2 and carbonic anhydrase I/II, was recently approved for osteoarthr …
Structural insight into the inhibition of carbonic anhydrase by the COX-2-selective inhibitor polmacoxib (CG100649).
Kim HT, Cha H, Hwang KY. Kim HT, et al. Biochem Biophys Res Commun. 2016 Sep 9;478(1):1-6. doi: 10.1016/j.bbrc.2016.07.114. Epub 2016 Jul 27. Biochem Biophys Res Commun. 2016. PMID: 27475498
Polmacoxib is not only a selective COX-2 inhibitor but also a potent inhibitor of carbonic anhydrases (CAs). ...To understand, at the molecular level, how polmacoxib interacts with CA I and II, we solved the first crystal structures of CA I and CA II in complex with …
Polmacoxib is not only a selective COX-2 inhibitor but also a potent inhibitor of carbonic anhydrases (CAs). ...To understand, at the …
A Randomized, Multicenter, Phase III Trial to Evaluate the Efficacy and Safety of Polmacoxib Compared with Celecoxib and Placebo for Patients with Osteoarthritis.
Lee M, Yoo J, Kim JG, Kyung HS, Bin SI, Kang SB, Choi CH, Moon YW, Kim YM, Han SB, In Y, Choi CH, Kim J, Lee BK, Cho S. Lee M, et al. Clin Orthop Surg. 2017 Dec;9(4):439-457. doi: 10.4055/cios.2017.9.4.439. Epub 2017 Nov 10. Clin Orthop Surg. 2017. PMID: 29201297 Free PMC article. Clinical Trial.
According to Physician's Global Assessments, more subjects were "much improved" at week 3 with polmacoxib than with celecoxib or placebo. Gastrointestinal and general disorder AEs occurred with a greater frequency with polmacoxib or celecoxib than with placebo. ...T …
According to Physician's Global Assessments, more subjects were "much improved" at week 3 with polmacoxib than with celecoxib or plac …
Benzylic Aroylation of Toluenes Mediated by a LiN(SiMe3)2/Cs+ System.
Gu Y, Zhang Z, Wang YE, Dai Z, Yuan Y, Xiong D, Li J, Walsh PJ, Mao J. Gu Y, et al. J Org Chem. 2022 Jan 7;87(1):406-418. doi: 10.1021/acs.joc.1c02446. Epub 2021 Dec 27. J Org Chem. 2022. PMID: 34958592
The value of benzylic deprotonation of 3-fluorotoluene is demonstrated by the synthesis of a key intermediate in the preparation of Polmacoxib....
The value of benzylic deprotonation of 3-fluorotoluene is demonstrated by the synthesis of a key intermediate in the preparation of Polma …
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.
Hirankarn S, Barrett JS, Alamuddin N, FitzGerald GA, Skarke C. Hirankarn S, et al. Clin Pharmacol Drug Dev. 2013 Oct;2(4):379-86. doi: 10.1002/cpdd.47. Epub 2013 Jul 25. Clin Pharmacol Drug Dev. 2013. PMID: 27121942
CG100649, proposed as a dual inhibitor of cyclooxygenase (COX)-2 and carbonic anhydrase (CA)-I/-II, is long-lived in plasma and whole blood. ...The extent to which these unique PK characteristics of CG100649 discriminate it from other COX-2 inhibitors will be the su …
CG100649, proposed as a dual inhibitor of cyclooxygenase (COX)-2 and carbonic anhydrase (CA)-I/-II, is long-lived in plasma and whole …
Effects of ketoconazole on the pharmacokinetic properties of CG100649, a novel NSAID: a randomized, open-label crossover study in healthy Korean male volunteers.
Youn Choi H, Jin SJ, Jung JA, Kim UJ, Ko YJ, Noh YH, Bae KS, Lim HS. Youn Choi H, et al. Clin Ther. 2014 Jan 1;36(1):115-25. doi: 10.1016/j.clinthera.2013.12.004. Clin Ther. 2014. PMID: 24417786 Clinical Trial.
No serious AEs were reported. Six subjects receiving the single dose of CG100649 had 9 AEs, and 7 subjects receiving the combination of ketoconazole and CG100649 had 8 AEs. The Cmax of CG100649 with CG100649 only and with concurrent administration of …
No serious AEs were reported. Six subjects receiving the single dose of CG100649 had 9 AEs, and 7 subjects receiving the combination …
Comparative impact on prostanoid biosynthesis of celecoxib and the novel nonsteroidal anti-inflammatory drug CG100649.
Skarke C, Alamuddin N, Lawson JA, Cen L, Propert KJ, Fitzgerald GA. Skarke C, et al. Clin Pharmacol Ther. 2012 Jun;91(6):986-93. doi: 10.1038/clpt.2012.3. Epub 2012 Jan 25. Clin Pharmacol Ther. 2012. PMID: 22278334 Free PMC article. Clinical Trial.
Both CG100649 and celecoxib had the effect of depressing urinary excretion of 2,3-dinor-6-keto-PGF(1alpha) (PGI-M); the effect of CG100649 was dose-dependent and more sustained (up to 240 h after the dose) than that of celecoxib. Neither CG100649 nor celecoxi …
Both CG100649 and celecoxib had the effect of depressing urinary excretion of 2,3-dinor-6-keto-PGF(1alpha) (PGI-M); the effect of …
CG100649, a novel COX-2 inhibitor, inhibits colorectal adenoma and carcinoma growth in mouse models.
Kim SH, Margalit O, Katoh H, Wang D, Wu H, Xia D, Holla VR, Yang P, DuBois RN. Kim SH, et al. Invest New Drugs. 2014 Dec;32(6):1105-1112. doi: 10.1007/s10637-014-0144-z. Epub 2014 Aug 3. Invest New Drugs. 2014. PMID: 25085205 Free PMC article.
Using mouse models, we show here that CG100649 inhibits premalignant and malignant colorectal lesions in mouse models, partly through inhibiting tumor cell proliferation. These pre-clinical findings suggest a need for further exploration of CG100649 for CRC preventi …
Using mouse models, we show here that CG100649 inhibits premalignant and malignant colorectal lesions in mouse models, partly through …
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