Drug intelligence / Profile preview

bimatoprost + brimonidine + timolol

Development stage
Phase 4
Lead developer
Allergan
Modality
Small Molecules
Administration
Ophthalmic
01

Overview

Triplenex is a fixed-dose triple combination ophthalmic solution developed by Allergan (now an AbbVie company) for the treatment of open-angle glaucoma and ocular hypertension. The formulation contains bimatoprost (0.01%), brimonidine tartrate (0.15%), and timolol maleate (0.5%). Bimatoprost is a prostaglandin analog (prostamide) that lowers intraocular pressure (IOP) by increasing aqueous humor outflow through both the trabecular meshwork and uveoscleral pathways. Brimonidine is a selective alpha-2 adrenergic agonist that reduces aqueous humor production and enhances uveoscleral outflow. Timolol is a non-selective beta-adrenergic antagonist that reduces IOP by decreasing aqueous humor secretion from the ciliary epithelium. By combining three agents with distinct and complementary mechanisms of action, Triplenex provides superior IOP reduction compared to dual combinations or monotherapies, particularly for patients who are insufficiently responsive to less intensive regimens. It is administered twice daily and has been approved in several international markets, including Mexico and India.

Brand names
Triplenex
Other names
Bimatoprost/brimonidine/timolol fixed-dose combinationTriple fixed-combination ophthalmic solution
02

Targets

ADRA2C (α2C)ADRB1 (β1)ADRA2A (α2A)ADRB2 (β2)PTGER3 (Prostaglandin E2 receptor EP3 subtype)PTGFR (Prostaglandin F2 alpha receptor)ADRA1B (α1B)PTGER1 (Prostaglandin E Receptor 1)ADRA2B (α2B)

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