Lead and thorium compounds
The present invention relates complexes comprising a PSMA targeting compound linked to a radionuclide, such as 212 Pb or 227 Th. These compounds, and pharmaceutical compositions comprising them, can be used for medical applications. These applications include the treatment of prostate cancer, and the complexes allow for dual targeting of cancers.
1. A compound comprising a prostate specific membrane antigen (PSMA) binding unit and a chelating unit, wherein the PSMA binding unit is carbon-backbone linked to the chelating unit wherein the compound is:
2. The compound according to claim 1 , which is complexed with a radionuclide selected from the group consisting of 212 Pb, 212 Bi, 213 Bi, 225 Ac and 227 Th.
3. The compound according to claim 1 , wherein the compound is complexed with 212 Pb.
4. A pharmaceutical composition comprising the compound according to claim 2 and a diluent, carrier, surfactant, or excipient.
5. The pharmaceutical composition according to claim 4 , further comprising 224 Ra.
6. The pharmaceutical composition according to claim 5 , wherein the amount of 224 Ra and 212 Pb is in radioactive equilibrium.
7. The pharmaceutical composition according to claim 6 , wherein the activity ratio (MBq) between 212 Pb to 224 Ra is between 0.5 and 2.
8. The pharmaceutical composition according to claim 4 , wherein composition is dosaged with a radioactivity of 100 kBq to 100 MBq per dose.
9. The pharmaceutical composition according to claim 4 , which is comprised in a kit.
10. A method of inhibiting a cancer comprising administering a pharmaceutical composition according to claim 4 to an individual in need thereof.
11. The method of claim 10 , wherein the cancer is prostate cancer.
12. The method of claim 10 , wherein the cancer is selected from the group consisting of skeletal metastases from cancers to the breast, prostate, kidneys, lung, bone, and multiple myeloma.
13. The method according to claim 12 , wherein the pharmaceutical composition is administered at a dose in the range 50-150 kBq per kg of bodyweight.