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    Anti-angiogenic agent, platform planned for human trial

    Take-home: Findings from preclinical studies show that a novel intravitreal depot of an anti-angiogenic drug releases the medication over a period of at least 6 months, is well-tolerated, and prevents VEGF-induced retinal vascular leakage.

    An intravitreal sustained hydrogel delivery system, releasing a tyrosine kinase inhibitor (TKI) with known anti-angiogenic properties, demonstrated positive results in preclinical studies investigating tolerability, efficacy, and pharmacokinetics.

    Planning for the first human trial to investigate the TKI depot as a treatment for retinal vascular disease is underway. Ocular Therapeutix is developing the product, OTX-TKI, and is collaborating with Regeneron to develop a 6-month depot delivery system for its aflibercept (Eylea).

    “Studies performed in Dutch Belted rabbits showed that the hydrogel platform delivered a low molecular weight TKI at zero order kinetics for a period of longer than 6 months,” said Peter Jarrett, PhD, chief scientific officer, Ocular Therapeutix. “The system had excellent tolerability, and we also obtained evidence of biological activity.”

    Dr. Jarrett pointed out that the findings of these studies indicate that the TKI delivery platform could provide patients with an alternative treatment for retinal vascular diseases. The platform would reduce the injection burden compared with used anti-VEGF agents that are administered every 4 or 8 weeks.

    The investigational product formulates micronized particles of the TKI into a bioabsorbable depot made of a synthetic hydrogel. The anti-angiogenic activity of TKIs is mediated by preventing activation of VEGFR-2 receptors, and the synthetic hydrogel has a record of excellent biocompatibility.

    “TKIs are insoluble molecules that would precipitate to create floaters in the vitreous,” said Dr. Jarrett. “(The molecules) would then be cleared quickly as they slowly dissolve. Our goal was to develop a platform that could deliver the TKI to target tissues over a period of six months,”

    The hydrogel matrix is a shape-changing device. It is formed into a long fiber that can be placed inside the lumen of a 27-gauge (or smaller) needle. Once the needle penetrates into the vitreous, a wire is used to push the depot into the eye. As the fiber gets wet, it becomes shorter and thicker, acquiring a configuration that will not obstruct the visual axis.

    Preclinical testing

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