Radiopharmaceuticals and methods of use thereof

2:

• The compound of claim 1, wherein said targeting moiety is a peptide.

3:

• The compound of claim 1, wherein said peptide is less than 20 amino acids in length.

4:

• The compound of claim 1, wherein said targeting moiety is an agonist of said receptor.

5:

• The compound of claim 1, wherein said receptor is selected from the group consisting of neurotensin receptors, gastrin-releasing peptide receptors, folate receptors, somatostatin receptors, prostate specific membrane antigen, vasoactive intestinal peptide receptors, cholecystokinin receptors, calcitonin receptors, vitronectin receptors, integrin receptors, asialoglycoprotein receptors, vascular endothelia growth factor receptors, transferrin receptors, luteinizing hormone-releasing hormone receptor, melanocortin receptors, glucagon-like peptide receptors, neurokinin receptors, sigma receptors, tropomyosin receptor kinase, aminopeptidase n (CD13) receptor, and epidermal growth factor receptor.

6:

• The compound of claim 5, wherein said receptor is selected from the group consisting of neurotensin receptors, gastrin-releasing peptide receptors, folate receptors, and somatostatin receptor.

7:

• The compound of claim 6, wherein said receptor is neurotensin receptor 1.

8:

• The compound of claim 1, wherein said CCTA is an acyloxymethyl ketone or an epoxide.

9:

• The compound of claim 8, wherein said CCTA is a peptidyl acyloxymethyl ketone or a dipeptidyl acyloxymethyl ketone.

10:

• The compound of claim 8, wherein said CCTA is an epoxysuccinyl peptide.

11:

• The compound of claim 1, wherein said cytotoxic or radioactive moiety is a radionuclide.

12:

• The compound of claim 11, wherein said radionuclide is contained within 1,4,7,10-tetraaza-1,4,7,10-tetra(2-carbamoylmethyl)cyclododecane (TCMC) or 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA).

13:

• The compound of claim 11, wherein said radionuclide is 177Lu.

14:

• The compound of claim 1, wherein said cysteine cathepsin trapping agent and said cytotoxic or radioactive moiety are each linked to said targeting moiety via a linker.

15:

• The compound of claim 1, wherein at least one of said linkers comprises a peptide linker.

16:

• The compound of claim 1, wherein at least one of said linkers comprises poly(ethylene glycol).

17:

• The compound of claim 1, wherein the log D7.4 of the compound is −2.5 to −4.0.

18:

• The compound of claim 17, wherein the log D7.4 of the compound is −3.0 to −4.0.

19:

• The compound of claim 1 selected from the group consisting of 2a, 2b, 2c, 2d, 2e, 2f, 4a, Ea, NE2a, NE2b, NE2c, NE2d, A-AG, A-ANT, NE1c, OE1a, FE1, and RE1, or a derivative thereof.

20:

• A composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier.

21:

• The composition of claim 20, further comprising a chemotherapeutic agent.

22:

• A method of treating a disease or disorder in a subject in need thereof, said method comprising administering a compound of claim 1 to said subject.

23:

• The method of claim 22, wherein said compound is administered as a composition further comprising a pharmaceutically acceptable carrier.

24:

• The method of claim 22, wherein said disease or disorder is cancer.

25:

• The method of claim 24, wherein said compound or composition is administered intravenously or to the tumor site.