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    Topical drug delivery via mucus-penetrating particles blocks VEGF signaling

    Animal models explore receptor tyrosine kinase inhibitor as noninvasive retinal disease therapy

    Take-home message: A topical receptor tyrosine kinase inhibitor may be a potential noninvasive inhibitor of vascular endothelial growth factor signaling.


    Waltham, MA—A topical receptor tyrosine kinase inhibitor candidate (K106, Kala Pharmaceuticals) is designed to potently and selectively block vascular endothelial growth factor (VEGF) signaling.

    When applied topically as mucus-penetrating particles (MPPs) in animals, the drug reaches the back of the eye—implying potential relevance in retinal disease therapy, according to Lisa Schopf, PhD.

    Mucus is an innate defense mechanism comprising a heterogeneous mesh of mucin that defends against pathogens and other particles by excluding particles larger than its pore sizes. In this situation, glycosylated macromolecules bind to foreign particles to facilitate clearance.

    MPPs should be able to overcome both steric exclusion and binding to allow for more efficient delivery of drugs in mucus-protected tissues.

    “The MPPs rapidly and uniformly coat and penetrate mucosal barriers, and have the potential to increase drug exposure to underlying tissues and improve topical ocular drug delivery,” Dr. Schopf said.

    Research goals

    The goals of Dr. Schopf and colleagues in this research were to design a small molecular inhibitor of the VEGF signaling pathway that was highly potent against VEGF receptors and against the platelet-derived growth factor receptor with good selectivity against particular growth factor, cell cycle, and other detrimental receptors. The K106 affinity for KDR over the other targets—i.e., EGFR, FGFR1 and RET—were 680, 188, and 28-fold, respectively.

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