Polmacoxib

Polmacoxib is an inhibitor of cyclooxygenase 2 (COX-2) and the carbonic anhydrase subtypes I (CAI) and CAII.¹ It inhibits COX-2 in the absence of carbonic anhydrase II with an IC₅₀ value of 40 nM, which increases by approximately 4- and 17-fold in the presence of a CAII at a molar ratio of 1:1 and 1:5, respectively.² It also inhibits CAI and CAII (IC₅₀s = 210 and 95 nM, respectively). Polmacoxib prevents >95 and 90% of prostaglandin E₂ (PGE₂) production in HCA-7 and HT-29 human colon cancer cells, respectively, using concentrations of 0.01 and 0.001 µg/ml.³ It inhibits polyp formation in a transgenic mouse model of intestinal polyp formation and tumor growth in human colorectal carcinoma mouse xenograft models when used at a dose of 7 mg/kg. The inhibition of COX-2 and CAII by polmacoxib has the potential for fewer serious systemic adverse effects, including cardiovascular events associated with COX-2 selective inhibitors such as celecoxib (Item No. 10008672).^1,2 Formulations containing polmacoxib have been used in the treatment of osteoarthritis.

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1. Singh, O., Kakularam, K.R., Reddanna, P., et al. Understanding the dual inhibition of COX-2 and carbonic anhydrase-II by celecoxib and CG100649 using density functional theory calculations and other molecular modelling approaches. Protein Pept. Lett. 22(10), 903-912 (2015).

2. Kim, H.T., Cha, H., and Hwang, K.Y. Structural insight into the inhibition of carbonic anhydrase by the COX-2-selective inhibitor polmacoxib (CG100649). Biochem. Biophys. Res. Commun. 478(1), 1-6 (2016).

3. Kimg, S.-H., Margalit, O., Katoh, H., et al. CG100649, a novel COX-2 inhibitor, inhibits colorectal adenoma and carcinoma growth in mouse models. Invest New Drugs 32(6), 1105-1112 (2014).