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US 2026/0077066 A1Published application
Receptor-targeting conjugate with an effective pharmacokinetic profile
AssigneeFluoguide A/S
InventorsAndreas KJÆR, Morten ALBRECHTSEN
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Abstract
The present invention describes a receptor-targeting conjugate comprising a fluorophore; a molecule, e.g. a peptide, binding to the receptor; and—a linker group which covalently links the fluorophore to the molecule binding to the receptor, wherein the conjugate is adapted to be administered intravenously into a human or animal body, and provide an effective pharmacokinetic profile with reference to inter alia receptor binding affinity and removal from plasma.
Claims20
A method comprising using a receptor-targeting conjugate comprising:
- a fluorophore;
- a molecule binding to the receptor;
- and
- a linker group which covalently links the fluorophore to the molecule binding to the receptor,
- said method comprising:
- administering the receptor-targeting conjugate into a human or animal body, and thereby
- providing receptor binding at least within 4,500 minutes;
- removal from plasma making the conjugate bound to the receptor visible, measured as plasma half-life which is the time it takes for the concentration in plasma to be reduced with 50%, and wherein the plasma half-life has a maximum of 4,500 minutes;
- providing receptor binding lasting at least 30 minutes;
- proving a receptor binding affinity, being the time it takes to reach the desired receptor binding, the lasting of the receptor binding and plasma half-life translating into a TBR (tumor-to-background ratio) of at least 1.5 and reaching that level within 4,500 minutes after administration into the human or animal body;
- and
- ensuring this level of TBR of at least 1.5 at least 30 minutes after that this level has been obtained.
9 more elements
Dependencies are inferred from the claim text.