InSite Vision Introduces DuraSite 2® Ophthalmic Drug Delivery System

Topline Data from Comparative Study Demonstrates Superior Drug Retention and Tissue Penetration

ALAMEDA, Calif.--(BUSINESS WIRE)--InSite Vision Incorporated (OTCBB: INSV) today introduced DuraSite 2^®, its next-generation enhanced drug delivery system which provides a broad platform for developing superior ophthalmic therapeutics. DuraSite 2 increases the tissue penetration for topically delivered ocular drugs with the aim of improved efficacy and dosing convenience. The company also announced topline data from a large-scale comparative study that demonstrates superior drug retention and tissue penetration for DuraSite 2 as compared to DuraSite^®.

“With DuraSite 2, we have developed a powerful new ophthalmic drug delivery platform that improves upon our well-established DuraSite technology and has surpassed our expectations, achieving multifold tissue penetration and positive safety results in a well-designed, large-scale preclinical study”

DuraSite 2 is based on InSite’s proven original DuraSite technology, and incorporates a cationic polymer to achieve sustained and enhanced ocular delivery of drugs. InSite scientists formulated both DuraSite 2 and DuraSite with the commonly used cataract surgery drug, ketorolac, a non-steroidal anti-inflammatory drug (NSAID), and conducted experiments to evaluate the difference between the two delivery systems and the commercially available ketorolac solution. InSite recently completed a three-arm preclinical pharmacokinetic study comparing DuraSite 2 versus DuraSite versus ketorolac in an industry-standard animal model. Results of this study show that the DuraSite 2 formulations of ketorolac demonstrated significantly higher drug levels than DuraSite plus ketorolac, or ketorolac alone, achieving more than 2x and 4x concentrations in the aqueous humor of the eye, respectively. Further, there was no indication of eye irritation using the DuraSite 2 formulation. InSite plans to submit detailed data from this study for presentation at the Association for Research in Vision and Ophthalmology (ARVO) 2013 Annual Meeting.

“With DuraSite 2, we have developed a powerful new ophthalmic drug delivery platform that improves upon our well-established DuraSite technology and has surpassed our expectations, achieving multifold tissue penetration and positive safety results in a well-designed, large-scale preclinical study,” said Lyle Bowman, Ph.D., Vice President of Development of InSite Vision. “InSite scientists have unique expertise in formulating novel ophthalmic therapeutics, and we believe DuraSite 2 could be critical in optimizing the profile of approved and future ocular drugs, extending the drug retention on the eye and reducing dosing frequency and the amount of drug needed to achieve efficacious results. In addition to these potential clinical advantages, the intellectual property surrounding DuraSite 2 was filed in early 2009, providing potential patent life into 2029 for this new drug delivery system, as well as increased protection for all drugs formulated with DuraSite 2.”

DuraSite 2 patent applications were submitted in 2009 in the United States and Europe and published in 2010. Both patents are pending issuance.

InSite Vision plans to utilize the DuraSite 2 platform in all future pipeline product candidates. Additionally, InSite will be finalizing and announcing a broad and novel licensing program with the intent of making DuraSite 2 a standard drug delivery technology in the ophthalmology industry, and provide access to industry partners through both exclusive and non-exclusive licensing and/or commercialization agreements.

About DuraSite^® and DuraSite 2^®

While eye drops are a proven delivery mechanism for numerous ocular drugs, efficacy of these agents is impeded by tears and blinking, which rinse the drug from the surface of the eye and limit retention and absorption. InSite’s DuraSite and DuraSite 2 platforms are sustained delivery technologies using a synthetic polymer-based formulation designed to extend the residence time of a drug relative to conventional topical therapies. DuraSite and DuraSite 2 enable topical delivery of a solution, gel or suspension and can be customized for delivering a wide variety of potential drug candidates. The DuraSite platform is currently leveraged in two commercial products for the treatment of bacterial eye infections, AzaSite^® and Besivance^®. InSite Vision is advancing a portfolio of novel preclinical- to clinical-stage ophthalmic products based on the DuraSite platform and anticipates advancing future ophthalmic product candidates using the DuraSite 2 platform.

About InSite Vision

InSite Vision is advancing new ophthalmologic products for unmet eye care needs. The company’s product portfolio utilizes InSite Vision’s proven DuraSite^® bioadhesive polymer core technology, an innovative platform that extends the duration of drug retention on the surface of the eye, thereby reducing frequency of treatment and improving the efficacy of topically delivered drugs. The DuraSite platform is currently leveraged in two commercial products for the treatment of bacterial eye infections, AzaSite^® (azithromycin ophthalmic solution) 1%, marketed in the U.S. by Merck, and Besivance^® (besifloxacin ophthalmic suspension) 0.6%, marketed by Bausch + Lomb. InSite Vision’s clinical-stage ophthalmic product pipeline includes AzaSite Plus^™ and DexaSite^™ for the treatment of eye infections, BromSite^™ for pain and inflammation associated with ocular surgery, and ISV-101 for the treatment of dry eye disease. InSite Vision is actively advancing additional front-of-eye technologies to expand its portfolio and for industry use. For further information on InSite Vision, please visit www.insitevision.com.

Forward-looking Statements

This news release contains certain statements of a forward looking nature relating to future events, including InSite's planned use of DuraSite 2 to formulate future drug candidates, the expected patent protection for DuraSite 2, InSite’s plans to license DuraSite 2 to third-parties, and the expected benefits of the DuraSite 2 drug delivery system. Such statements entail a number of risks and uncertainties, including but not limited to: the ability to formulate DuraSite 2 with existing drugs; the results of future clinical trials for product candidates formulated in DuraSite 2; InSite’s ability to obtain FDA approval of DuraSite 2 enabled drugs; InSite’s ability to successfully license DuraSite 2 to third parties; the risk that DuraSite 2 may not be commercially accepted; InSite's reliance on third parties for the commercialization of its products; the ability of InSite to enter into corporate collaborations for its product candidates; InSite's ability to expand its product platform to include additional indications; InSite's ability to compete effectively, either alone or through its partners, with other companies offering competing products or treatments; InSite's ability to maintain and develop additional collaborations and commercial agreements with corporate partners, its ability to adequately protect its intellectual property and to be free to operate with regard to the intellectual property of others; and determinations by the FDA. Reference is made to the discussion of these and other risk factors detailed in InSite Vision's filings with the Securities and Exchange Commission, including its annual report on Form 10-K and its quarterly reports on Form 10-Q, under the caption "Risk Factors" and elsewhere in such reports. Any forward-looking statements or projections are based on the limited information currently available to InSite Vision, which is subject to change. Although any such forward-looking statements or projections and the factors influencing them will likely change, InSite Vision undertakes no obligation to update the information. Such information speaks only as of the date of its release. Actual events or results could differ materially and one should not assume that the information provided in this release is still valid at any later date.

AzaSite^®, DuraSite 2^® and DuraSite^® are registered trademarks of InSite Vision Incorporated. BESIVANCE^® is a registered trademark of Bausch + Lomb Incorporated.