UPAR TARGETING PEPTIDE FOR USE IN PEROPERATIVE OPTICAL IMAGING OF INVASIVE CANCER
There is provided a novel conjugate that binds to the cell surface receptor uPA (uPAR). The conjugate is based on a fluorescence-labeled peptide useful as a diagnostic probe to the surfaces of cells expressing uPAR. The conjugate is capable of carrying a suitable detectable and imageable label that will allow qualitative detection and also quantitation of uPAR levels in vitro and in vivo. This renders the surgical resection of tumors more optimal.
1 . A fluorophor labelled u PAR-targeting peptide conjugate having the formula:
X-Y-(D-Asp)-([beta]-cyclohexyl-L-alanine)-(Phe)-(D-Ser)-(D-Arg)-(Tyr)-(Leu)-(Trp)-(Ser)
wherein,
X represents imageable moiety capable of detection either directly or indirectly in a optical imaging procedure, and
Y represents a spacer, a biomodifier or is absent
2 . A fluorophor labelled uPAR-targeting peptide conjugate as claimed in claim 1 of the formula:
and pharmaceutically acceptable salts thereof.
3 . The compound of claim 1 for use in fluorescence guided surgical resection of tumours.
4 . The compound of claim for use according to claim 3 , wherein the compound is administered to a subject in a dose of 0.1-1000 mg per person.
5 . The compound of claim 1 for peroperative optical imaging of cancer.
6 . A pharmaceutical composition for optical imaging of cancer, wherein the composition comprises a compound of claim 1 together with at least one pharmaceutically acceptable carrier or excipient.
7 . The pharmaceutical composition of claim 6 , wherein the concentration of the compound is 0.1-1000 mg per dosage unit.
8 . Use of a compound of claim 1 for the manufacture of a diagnostic agent for use in a method of optical imaging of cancer involving administration of said compound to a subject and generation of an image of at least part of said subject.
9 . Use according to claim 8 , wherein the compound is administered to the subject in a dose of 0.1-1000 mg per subject.
10 . A method of optical imaging of cancer of a subject involving administering a compound of claim 1 to the subject and generating an optical image of at least a part of the subject to which said compound has distributed.
11 . Method of claim 10 , wherein the compound of claim 1 is administered to the subject in a dose of 0.1-1000 mg per subject.