Brinzolamide 1%/timolol 0.5% fixed combination (brinzolamide/timolol) is a twice-daily eyedrops suspension comprising the carbonic anhydrase-II inhibitor brinzolamide and the beta-adrenergic receptor antagonist timolol. Brinzolamide/timolol produced clinically relevant reductions in mean intraocular pressure (IOP) from baseline and was more effective than brinzolamide or timolol monotherapy in lowering IOP in a 6-month, randomized, phase III trial in patients with open-angle glaucoma or ocular hypertension (n = 523). The proportion of patients achieving a mean IOP of <18 mmHg was significantly greater in recipients of brinzolamide/timolol than in recipients of brinzolamide or timolol monotherapy. The IOP-lowering efficacy of brinzolamide/timolol was maintained for up to 12 months, and was no less effective than dorzolamide 2%/timolol 0.5% solution (dorzolamide/timolol) in a randomized, phase III, noninferiority trial (n = 437). Brinzolamide/timolol was generally well tolerated and was associated with significantly lower ocular discomfort scores than dorzolamide/timolol. Moreover, a significantly greater number of patients expressed a preference for brinzolamide/timolol over dorzolamide/timolol. The main ocular adverse event was blurred vision, and was not considered to be a safety issue.