Drug intelligence / Profile preview

brimonidine + dorzolamide + timolol

Development stage
Unknown
Lead developer
Kukje Pharm
Modality
Small Molecules
Administration
Ophthalmic
01

Overview

TFC-003-R2 + TFC-003-R3 is an investigational ophthalmic fixed-dose triple combination therapy developed by Kukje Pharma for the treatment of primary open-angle glaucoma and ocular hypertension. The formulation contains three active ingredients: brimonidine (an alpha-2 adrenergic agonist), dorzolamide (a carbonic anhydrase inhibitor), and timolol (a non-selective beta-blocker). These agents work synergistically to reduce intraocular pressure (IOP) by targeting different biological mechanisms: brimonidine and timolol decrease aqueous humor production, while brimonidine also increases uveoscleral outflow and dorzolamide inhibits aqueous secretion. The specific designation TFC-003-R2 + TFC-003-R3 refers to a regimen evaluated in Phase 3 clinical trials where two variants of the triple combination are administered sequentially to optimize efficacy and safety compared to standard dual-combination therapies like dorzolamide/timolol.

Other names
brimonidine tartrate + dorzolamide hydrochloride + timolol maleate
02

Targets

ADRB2 (β2)CA2 (Carbonic Anhydrase 2)ADRB1 (β1)ADRA2A (α2A)

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