Brinzolamide

Brinzolamide (AL-4862) is a selective carbonic anhydrase II inhibitor with anIC₅₀ value of 3.2 nM. Brinzolamide hydrochloride reduces intraocular pressure (IOP) by inhibiting ciliary CA-II and decreasing atrial fluid secretion. Brinzolamide can be used in glaucoma disease research^[1][2]. IC50 & Target: IC50: 3.2 nM (carbonic anhydrase II) ^[2]. In Vivo: Brinzolamide (7.5 mg or 12 mg) implanted in a silicone matrix is extremely well tolerated and provides sustained release of brinzolamide and significant reduction in intraocular pressure (IOP) for up to 28 days with no adverse effects or signs of toxicity in normotensive NZW rabbits^[2].
The pharmacokinetic parameters of Brinzolamide in rabbits^[1].

	Intracameral Administration (4.5 mg)	Intracameral Administration (4.5 mg)	Topical Administration (500 mg)	Topical Administration (500 mg)
PK Parameters	Aqueous Humor	Iris-Ciliary Body	Aqueous Humor	Iris-Ciliary Body
Tmax (h)	0.08	0.5	1	0.25
Cmax (ng/mL, ng/g)	11,050	1964	408	1245
Terminal t1/2 (h)	3.4	13	2	13.6
AUC0-24h (h*ng/mL, h*ng/g)	17,780	7725	1896	11414
AUC0-∞ (h*ng/mL, h*ng/g)	17,836	8839	1955	16628
Dose-normalized AUC0-∞ (h*/mL, h*/g)	4	2	0.004	0.03