Inventors:
Ravindra K. Pandey - Williamsville NY, US
Suresh Pandey - Buffalo NY, US
Lalit Goswami - Columbia MO, US
Allan Oseroff - Buffalo NY, US
Shipra Dubey - Williamsville NY, US
Munawwar Sajjad - Clarence Center NY, US
Stephanie Pincus - Buffalo NY, US
Assignee:
HEALTH RESEARCH, INC. - Buffalo NY
THE RESEARCH FOUNDATION OF STATE UNIVERSITY OF NEW YORK - Amherst NY
International Classification:
A61K 51/04, A61K 49/00, A61K 31/30, A61K 31/409, A61K 38/12, A61K 31/437, A61K 31/506, A61P 35/00, A61P 43/00
US Classification:
424 111, 424 91, 514499, 514410, 514 199, 514279, 514275
Abstract:
A compound that is a conjugate of an antagonist to an integrin expressed by a tumor cell and at least one of a tumor avid tetrapyrollic photosensitizer, a fluorescent dye, and a radioisotope labeled moiety wherein the radioisotope is C, F, Cu, I, Tc, In or GdIII and its method of use for diagnosing, imaging and/or treating hyperproliferative tissue such as tumors. Preferably the photosensitizer is a tumor avid tetrapyrollic photosensitizer, e.g. a porphyrin, chlorin or bacteriochlorin, e.g. pheophorbides and pyropheophorbides. Such conjugates have extreme tumor avidity and can be used to inhibit or completely destroy the tumor by light absoption. The integrin is usually αvβ3, α5β1, αvβ5, α4β1, or α2β1. Preferably, the antagonist is an RGD peptide or another antagonist that may be synthetic such as a 4-{2-(3,4,5,6-tetra-hydropyrimidin-2-ylamino)ethyloxy}-benzoyl]amino-2-(S)-amino-ethyl-sulfonylamino group. Such compounds provide tumor avidity and imaging ability thus permitting selective and clear tumor imaging.