Drug intelligence / Profile preview

aflibercept + dorzolamide + timolol

Development stage
Preclinical
Lead developer
Regeneron Pharmaceuticals
Modality
Small Molecules
Administration
Intravitreal, Topical
01

Overview

Aflibercept + dorzolamide + timolol is a combination regimen involving the intravitreal injection of aflibercept, an anti-vascular endothelial growth factor (anti-VEGF) biologic, together with topical administration of dorzolamide and timolol, both small molecule drugs used as eye drops. Aflibercept acts by binding VEGF-A and placental growth factor (PlGF), inhibiting angiogenesis and vascular permeability in the retina. Dorzolamide is a carbonic anhydrase inhibitor that reduces aqueous humor production, while timolol is a non-selective beta-adrenergic blocker that also decreases aqueous humor formation. This combination has been studied primarily for persistent exudation in neovascular age-related macular degeneration (nAMD) not fully responsive to anti-VEGF monotherapy; evidence suggests that adding dorzolamide-timolol may reduce central subfield thickness and subretinal fluid, potentially by prolonging intraocular residence time of aflibercept[1][3][4]. The components are individually approved for other indications but are used together off-label in this context.

02

Targets

ADRB2 (β2)CA2 (Carbonic Anhydrase 2)VEGFA (Vascular endothelial growth factor A)PGF (Placental Growth Factor)ADRB1 (β1)VEGFB (Vascular endothelial growth factor B)

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