Netarsudil Mesylate
Class: Rho Kinase Inhibitors
Chemical Name: [4-[(2S)-3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl]phenyl]methyl 2,4-dimethylbenzoate;methanesulfonic acid
Molecular Formula: C30H35N3O9S2
CAS Number: 1422144-42-0
Brands: Rhopressa
Introduction
Ocular hypotensive agent; rho kinase (ROCK) inhibitor and norepinephrine transporter (NET) inhibitor.
Uses for Netarsudil Mesylate
Ocular Hypertension and Glaucoma
Netarsudil 0.02%: Reduction of elevated IOP in patients with open-angle glaucoma or ocular hypertension. Once-daily administration of netarsudil 0.02% appears to be noninferior to twice-daily administration of timolol 0.5% in reducing IOP.
Fixed-combination netarsudil 0.02% and latanoprost 0.005%: Reduction of elevated IOP in patients with open-angle glaucoma or ocular hypertension. When administered once daily, mean IOP reduction was approximately 1–3 mm Hg greater than that achieved with once-daily administration of either drug alone.
When selecting an initial ocular hypotensive agent, consider extent of the required IOP reduction, coexisting medical conditions, and drug characteristics (e.g., dosing frequency, adverse effects, cost). With single-agent regimens, the reduction in IOP is approximately 25–33% with topical prostaglandin analogs; 20–25% with topical β-adrenergic blocking agents, α-adrenergic agonists, or miotic (parasympathomimetic) agents; 20–30% with oral carbonic anhydrase inhibitors; 18% with topical rho kinase inhibitors; and 15–20% with topical carbonic anhydrase inhibitors.
A prostaglandin analog frequently is considered for initial therapy in the absence of other considerations (e.g., contraindications, cost considerations, intolerance, adverse effects, patient refusal) because of relatively greater activity, once-daily administration, and low frequency of systemic adverse effects; however, ocular adverse effects can occur.
Goal is to maintain an IOP at which visual field loss is unlikely to substantially reduce quality of life during the patient's lifetime.
Reduction of pretreatment IOP by ≥25% shown to slow progression of primary open-angle glaucoma. Set an initial target IOP (based on extent of optic nerve damage and/or visual field loss, baseline IOP at which damage occurred, rate of progression, life expectancy, and other considerations) and reduce IOP toward this goal. Adjust target IOP up or down as needed over course of disease.
Combination therapy with drugs from different therapeutic classes often required to control IOP.
Netarsudil Mesylate Dosage and Administration
Administration
Ophthalmic Administration
Apply topically to the eye(s) as an ophthalmic solution containing netarsudil alone or in fixed combination with latanoprost.
Avoid contaminating the solution container. (See Bacterial Keratitis under Cautions.)
Remove soft contact lenses prior to administration of each dose; may reinsert contact lenses 15 minutes after the dose. (See Use with Contact Lenses und...
