# Development of a Selective Inhibitor of NaV1.7 for the Treatment of Ocular Pain

> **NIH NIH R44** · SITEONE THERAPEUTICS, INC. · 2021 · $1,081,115

## Abstract

PROJECT SUMMARY
The absence of safe and effective strategies for the management of ocular pain is motivating the development
of a novel topical drug suitable for patient self-administration. Conventional local anesthetics, such as
proparacaine, inhibit voltage-gated sodium channels (NaV) and are highly effective for the management of
ocular pain in acute, in-office settings. However, these anesthetic agents block protective ocular reflexes and
are toxic to the corneal surface, which limits their use to a few in-office administrations. Other agents, such as
topical NSAIDs, are relatively ineffective at relieving ocular discomfort, or have side effects that limit their use.
SiteOne Therapeutics has discovered a novel chemical series of exquisitely selective inhibitors of human
NaV1.7, a voltage-gated sodium channel subtype implicated in the transmission of pain signals by human
genetics. These compounds exhibit excellent dose-dependent analgesic effects in multiple animal models of
acute and chronic pain including a rat dry eye model. In preclinical safety and efficacy studies, topical ocular
administration is effective, safe, well tolerated, and leads to good intraocular exposure. The goal of this Phase
2 SBIR proposal is to advance IND-enabling development of a topical ocular analgesic product. The Specific
Aims are to complete GLP nonclinical safety studies, drug product development, and to prepare the first GMP
batch in order to initiate clinical studies to determine if the new topical drug has an adequate safety and
efficacy profile to justify further clinical development for the treatment of ocular pain.

## Key facts

- **NIH application ID:** 10326026
- **Project number:** 1R44EY033267-01
- **Recipient organization:** SITEONE THERAPEUTICS, INC.
- **Principal Investigator:** Sheri Denet Klas
- **Activity code:** R44 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2021
- **Award amount:** $1,081,115
- **Award type:** 1
- **Project period:** 2021-09-01 → 2023-08-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10326026

## Citation

> US National Institutes of Health, RePORTER application 10326026, Development of a Selective Inhibitor of NaV1.7 for the Treatment of Ocular Pain (1R44EY033267-01). Retrieved via AI Analytics 2026-05-25 from https://api.ai-analytics.org/grant/nih/10326026. Licensed CC0.

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