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    RG7716 molecule shows promise as DME treatment

    A bi-specific molecule that simultaneously inhibits angiopoietin-2 (Ang2) and vascular endothelial growth factor A (VEGF-A) has shown clinically meaningful and statistically significant improvements in visual acuity gains compared with ranibizumab alone for diabetic macular edema (DME).

    RG7716 (Genentech/Roche) has a high potency and specificity, said Pravin U. Dugel, MD, managing partner, Retinal Consultants of Arizona, Phoenix; clinical professor, Department of Ophthalmology, Keck School of Medicine, University of Southern California, Los Angeles. In DME, Ang-2 works synergistically with VEGF-A to drive biological pathways that cause vessel permeability and inflammation.

    Figure 1. Computer-generated modeling of RG7716 (Image courtesy of Roche)

    A bi-specific compound is a single molecule that has two different arms that inhibit two different ligands, Dr. Dugel said, noting these look like the letter “Y” (See Figure 1). Each of the top “arms” binds to either VEGF-A or Ang2, while the “base” has been specifically engineered to decrease inflammation and systemic VEGF-A exposure.

    “But it’s one molecule, and that’s what differentiates this compound,” Dr. Dugel said. “There’s a single clearance rate, and that’s really a key point.”

    Clinicians, who believe both ligands need to be inhibited at the same time for the best result, would also agree to the benefit of using a bi-specific compound because of that single clearance rate.

     

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