Radiosensitizer compounds for use in combination with radiation
View Patent ↗Disclosed herein are radiosensitizer compounds useful in combination with radiation therapy, e.g., a synergistic combination therapy for the treatment of cancer and other disorders. The radiosensitizer compounds have the general formula I: wherein A represents an aromatic core; at least one of R a and R b is an electron transfer promoter as defined herein, e.g., NH 2 ; and at least one of R c is a leaving group as defined herein, e.g., halogen; and the remainder of the molecule is as defined herein. Pharmaceutical compositions, methods, uses, kits and commercial packages comprising the radiosensitizer compounds are also disclosed.
1. A method of treating cancer in a patient comprising administering to said patient a biocompatible radiosensitizer compound in combination with ionizing radiation, wherein the compound is selected from the group consisting of:
and a pharmaceutically acceptable salt thereof.
2. The method of claim 1 , wherein the compound and the ionizing radiation are administered sequentially or simultaneously.
3. The method of claim 1 , wherein the compound is radiolabelled.
4. The method of claim 3 , wherein compound is radiolabelled with one or more atoms selected from the group consisting of 3 H, 14 C, 32 P, 35 S, 43 F and 36 Cl.
5. The method of claim 1 , wherein the compound is formulated for enteral administration.
6. The method of claim 5 , wherein the compound is formulated for oral administration.
7. The method of claim 1 , wherein the compound is administered parenterally.
8. The method of claim 7 , wherein the compound is formulated for intravenous, intramuscular, or subcutaneous administration.
9. The method of claim 7 , wherein the compound is administered intravenously.
10. The method of claim 7 , wherein the compound is administered systemically.
11. The method of claim 7 , wherein the compound is administered regionally.
12. The method of claim 1 , wherein the subject is administered a pharmaceutical formulation comprising an effective amount of the compound and one or more pharmaceutically acceptable carriers or diluents.
13. The method of claim 1 , wherein the ionizing radiation is external source radiation.
14. The method of claim 13 , wherein the ionizing radiation is X-ray radiation.
15. The method of claim 13 , wherein the ionizing radiation is gamma (γ)-ray radiation.
16. The method of claim 13 , wherein the radiation is neutral or charged particle radiation.
17. The method of claim 16 , wherein the ionizing radiation is β-ray radiation.
18. The method of claim 1 , wherein the ionizing radiation is internal radiation sources.
19. The method of claim 1 , wherein the ionizing radiation is radioisotope sources.
20. The method of claim 1 , wherein the combination therapy of the compound with ionizing radiation further includes one or more additional cancer therapies.