Background:

Brinzolamide is a potent and selective inhibitor of carbonic anhydrase type II (CA II) with IC50 value of 3.19nM [1].

Brinzolamide is the newest topical CAI to be successfully developed and marketed. It is a safe and efficacious glaucoma drug. In the in vitro assay, brinzolamide has its highest affinity (Ki of 0.13nM) and inhibitory potency (IC50 of 3.19 nM) for CA-II. It has much higher affinity and greater potency for CA-II than for CA-I and CAIV. In the in vivo models, administration of brinzolamide significantly reduces the intraocular pressure (IOP) both in the pigmented rabbits and cynomolgus monkeys with ocular hypertension induced by argon laser trabeculoplasty [1].

As an inhibitor of CA, brinzolamide is also used to assess cerebral blood flow reserve as it can conserve CO2 in the tissues, and the CO2 can then act on blood vessels and produce vasodilatation. Moreover, brinzolamide is proved to be safe and efficacious for reducing intraocular pressure [1].

参考文献:
[1] DeSantis L. Preclinical overview of brinzolamide. Surv Ophthalmol. 2000 Jan;44 Suppl 2:S119-29.