# Phosphosulindac for dry eye

> **NIH NIH R44** · APIS THERAPEUTICS, LLC · 2020 · $377,136

## Abstract

ABSTRACT
The treatment of dry eye disease (DED) has been hampered by weak agents, significant side
effects and high cost. The pathophysiological hallmark of DED that unifies its diverse etiologies
is inflammation of the ocular surface that accounts for its clinical manifestations. The optimal
treatment of DED must provide strong efficacy; topical analgesia; safety; convenient dosing; and
low cost. None of the available treatments for DED meets these criteria.
 Phosphosulindac (PS) is a proprietary compound. We developed novel robust rabbit
models of DED encompassing its main pathophysiological subgroups (evaporative, aqueous
deficient and mixed). PS showed remarkable efficacy against DED; excellent safety; practically
instantaneous topical analgesia; superiority in terms of efficacy over cyclosporine and lifitegrast,
the two currently available drugs for the treatment of DED; and has projected low cost Additional
preliminary data include the IND-enabling development of a scaled-up synthesis of PS; and
development and validation of all the required analytical methods. We have also identified
molecular targets of PS; and developed several formulations for PS encompassing the main
physicochemical categories.
 Our goal is to develop PS as an efficacious drug for DED. In this Fast Track application,
we propose the following studies:
 Phase I studies: Aim#1: Study the effect of PS in an evaporative model of DED,
complementing our results with the aqueous deficient and mixed models. Aim #2: Develop the
lead formulation of PS.
 Phase II studies: Aim #3: Optimize the lead formulation from aim #2. Aim #4: Study the
in vitro metabolic stability and plasma protein binding of PS. Aim #5: Perform toxicity studies of
PS. And Aim # 6: Prepare the IND protocol and package for the FDA.
 The proposed work, if successful, will contribute greatly towards a successful treatment of
DED, a prevalent human disease, which represents an unmet medical need.

## Key facts

- **NIH application ID:** 9907964
- **Project number:** 1R44EY031193-01
- **Recipient organization:** APIS THERAPEUTICS, LLC
- **Principal Investigator:** Basil Rigas
- **Activity code:** R44 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $377,136
- **Award type:** 1
- **Project period:** 2020-08-01 → 2021-07-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/9907964

## Citation

> US National Institutes of Health, RePORTER application 9907964, Phosphosulindac for dry eye (1R44EY031193-01). Retrieved via AI Analytics 2026-05-24 from https://api.ai-analytics.org/grant/nih/9907964. Licensed CC0.

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