Michelle SladeAssociate Editor

InSite Vision Inc. will begin a Phase I safety trial for an ocularapplication of Synergen's IL-1ra (interleukin-1 receptorantagonist) in early December, the companies announcedThursday.

The trial will be the first use of IL-1ra in the eye. It is expectedto be completed by year end, and data should be available byFebruary 1993, according to InSite spokeswoman ChristaNicholas.

Assuming the trial produces favorable results, an efficacystudy will start in March to study allergic inflammation,Nicholas said.

Synergen is supplying IL-1ra to InSite for the studies, Nicholastold BioWorld, and a more elaborate joint venture agreement isbeing negotiated.

Jon Saxe, Synergen's president and chief executive officer, toldBioWorld that the development of IL-1ra as an ocular anti-inflammatory, particularly for allergic conjunctivitis, will be animprovement over current treatments.

"One of the widely used approaches is steroidal eye drops,which over time can be damaging to the eye tissue andsystem," Saxe said. "IL-1ra mediates inflammation without theside-effects of a steroid."

Synergen (NASDAQ:SYGN) of Boulder, Colo., declined to predictwhen an ocular product resulting from the collaboration wouldreach the market.

InSite Vision of Alameda, Calif., is also working on aformulation of IL-1ra in its proprietary delivery vehicle,DuraSite 1, for further Phase II/III clinical trials. DuraSite is across-linked polymer vehicle that delivers the drug over anextended period to provide enhanced duration of activity forhigh-molecular weight proteins, such as IL-1ra, which presenta major hurdle when they come in contact with the eye.

"As the proteins are too large to penetrate the ocular surfacereadily, they need to be held on the surface of the eye for sometime to maximize penetration and be useful," Nicholas said.

Using the DuraSite approach, the drug enters the tear fluid,forms a gel and settles into the bottom of the lower eyelid,where it releases the drug.

InSite, founded in 1986, is developing novel drug deliverysystems for ophthalmics.

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