Treatment of glaucoma and ocular hypertension using rho kinase inhibitors: patent evaluation of US2018244666 and US2018256595

ABSTRACT

Introduction: Glaucoma refers to a heterogeneous group of optic neuropathies characterized by an enhanced intraocular pressure (IOP). To date, there are six available different drug classes for the treatment of glaucoma and ocular hypertension: β-adrenergic antagonists, prostaglandins, carbonic anhydrase inhibitors, α2-selective adrenergic, muscarinic agonists and rho kinase inhibitors, which act by reducing the production or increasing the drainage of aqueous humor.

Areas covered: This manuscript reviews patent US2018244666A1, that describes the synthesis of novel potential rho kinase and monoamine transporters inhibitors with a benzamide or isoquinoline amide scaffolds, and patent US2018256595A1 that investigates the long-term treatment of glaucoma or ocular hypertension with ripasudil, a rho kinase inhibitor.

Expert opinion: A variety of netarsudil congeners were synthesized as rho kinases inhibitors in patent US2018244666A1. Results of patent US2018256595A1 showed that ripasudil is among the best candidates for glaucoma long-term treatment, as IOP continuously dropped over the course of the treatment.

KEYWORDS:

• Glaucoma
• ocular hypertension
• IOP
• rho kinase inhibitors
• netarsudil
• ripasudil

Article highlights

• A large subset of netarsudil congeners was synthesized and evaluated as rho kinase inhibitors.

• Rho kinase inhibitors seem to be good candidates to promote a stable IOP-lowering action without efficacy reduction in long-term treatments.

• The patients IOP continuously lowers over the course of the treatment with ripasudil.

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Reviewer disclosures

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

This paper was not funded.