February 12, 2014
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Squalamine eye drops reach therapeutic concentrations in choroid

MIAMI — Squalamine eye drops achieve trough concentrations in the choroid well in excess of its threshold level to inhibit angiogenesis, a speaker said here.

“Squalamine has some very promising properties,” Lawrence J. Singerman, MD, FACS, FICS, said at the Angiogenesis, Exudation, and Degeneration 2014 meeting. “One is long retention time in the posterior ocular tissues. Another is high potency, and it has ability to inhibit multiple angiogenic growth factors.”

Lawrence J. Singerman

Squalamine has a novel intracellular anti-angiogenic mechanism of action that inhibits VEGF, PDGF and bFGF signaling through chaperoning of the modulatory protein calmodulin, Singerman said. In May 2012, the U.S. Food and Drug Administration fast tracked the agent for use in wet age-related macular degeneration.

There is precedence for topical delivery of drops to the posterior segment, for example, in clinical practice for treating macular edema after ocular surgery, Singerman said.

Safety and efficacy of squalamine eye drops in neovascular AMD are being studied in a multicenter phase 2 trial whose final data are due at the end of the year, Singerman said. Further study of its use in diabetic retinopathy and retinal vein occlusion is also planned.

Disclosure: Singerman is a consultant and on the advisory board for Ohr Pharmaceutical.