Near-infrared dyes and conjugates for targeting tumors
Inventors
Small, Lyle D. • Wang, Ruizheng • Crippen, Shane M.
Assignees
Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-12599682-B2
Publication Date
2026-04-14
Expiration Date
Abstract
The design, synthesis, and functionalization of a conjugate including a tumor-targeting near-infrared (NIR) dye and a therapeutic agent and/or a diagnostic agent, whereby the NIR dye can function to target the therapeutic agent and/or diagnostic agent to tumor cells.
Core Innovation
A composition is provided comprising a tumor-targeting near-infrared dye and a chemotherapeutic agent bound to the dye via a linker. The dye targets the chemotherapeutic agent to tumor cells, and the composition is configured such that the near-infrared dye serves as a tumor-targeting component to deliver the bound chemotherapeutic agent to tumor cells.
The disclosure includes linker concepts that support attachment of a near-infrared dye to a nanoparticle-associated structure, including heterobifunctional linkers with anchors for nanoparticle association and reactive groups for near-infrared dye attachment. Cleavable and self-destruct linker concepts are described to address differences between tumor and normal cells, including enzyme-cleavable and pH-cleavable mechanisms.
The document further describes near-infrared therapeutic conjugates extending beyond chemotherapeutics to oxidative-stress therapy and photodynamic and photothermal therapy agent conjugates. Illustrative embodiments also include near-infrared dye conjugates using nanoparticle cores and characterization and biological testing readouts, including TEM, UV-visible near-infrared peak, organoid uptake comparisons, and hyperthermia temperature versus concentration and versus frequency.
Claims Coverage
The provided independent claim defines a tumor-targeting near-infrared dye composition with a chemotherapeutic agent bound via a linker that targets tumor cells, supported by dependent claims that refine the dye absorption wavelength range and the linker behavior, including cleavability and self-destruction mechanisms that exploit differences between tumor cells and normal cells such as enzymes or pH, and further refine a conjugate architecture using a cyanine dye. Across the claim set, six inventive-feature refinements are specified.
Tumor-targeting near-infrared dye bound chemotherapeutic delivery
A composition comprising a tumor-targeting near-infrared dye and a chemotherapeutic agent bound to said dye via a linker, wherein said dye targets said chemotherapeutic agent to tumor cells.
Near-infrared dye absorption wavelength range
The composition wherein the near-infrared dye has an absorption wavelength in the range of about 650 nm to about 1200 nm.
Tumor-cell cleavable linker after entering tumor cells
The composition wherein the linker is cleavable after entering tumor cells.
Linker cleavage exploited by differences between tumor cells and normal cells
The composition wherein the linker is cleaved near tumor cells by exploiting differences between tumor cells and normal cells.
pH difference driven linker cleavage near tumor cells
The composition wherein the linker cleaves near tumor cells by exploiting pH differences between tumor cells and normal cells.
Cyanine-dye tumor-targeting component conjugate
The composition wherein the cyanine dye and the chemotherapeutic agent form a conjugate, where the tumor-targeting component of the conjugate is the cyanine dye.
Overall, the claim set centers on a tumor-targeting near-infrared dye bound to a chemotherapeutic agent via a linker that delivers to tumor cells, with refinements that constrain the near-infrared absorption wavelength and require tumor-environment-triggered linker cleavage mechanisms, including cleavage driven by differences between tumor and normal cells and specifically pH-dependent cleavage, and further specifying a cyanine dye-based conjugate architecture.
Stated Advantages
Conjugate targeting aims to reduce toxicity to healthy tissue.
Deep-penetrating irradiation enables hyperthermia and phototherapies.
NIR-IONP conjugates are associated with MRI contrast material and hyperthermia roles.
Documented Applications
Cancer-targeting platform using tumor-targeting near-infrared (NIR) dyes conjugated to therapeutic and/or diagnostic agents.
Hyperthermia and phototherapies enabled by deep-penetrating irradiation of the conjugates.
MRI contrast material and hyperthermia roles associated with NIR dye-IONP conjugates.
Interested in licensing this patent?