VTI-1002

VTI-1002 is a first-in-class, highly potent, selective small-molecule inhibitor of human granzyme B (GzmB), developed primarily for topical administration to treat inflammatory and impaired-wound-healing skin conditions.[1][3] It inhibits human GzmB with a Ki of approximately 4.4 nM and shows strong selectivity over related proteases including caspases 3–10, cathepsin G, and neutrophil elastase, as well as potent activity against mouse GzmB, enabling translational studies in murine models.[1][3] In preclinical models, VTI-1002 formulated as a topical gel penetrates the stratum corneum, is retained in skin for at least 24 hours with minimal systemic absorption, and accelerates wound closure, improves collagen organization, reduces inflammation, and restores structural proteins in models of diabetic burn wound healing, autoimmune pemphigoid diseases, and atopic dermatitis–like inflammation.[1][2][4] These data support development of VTI-1002 as a targeted GzmB-pathway modulator for cutaneous diseases associated with extracellular matrix degradation, skin barrier disruption, and chronic inflammation.[1][2][4][7][9]