Targeted therapeutics

Abstract

The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.

We claim: 
     
         1 . A pharmaceutical composition comprising a drug conjugate (SDC-TRAP) or its carboxylate derivative salt form, and at least one excipient, wherein the SDC-TRAP or its carboxylate derivative salt form is SDC-TRAP-0063 sodium. 
     
     
         2 . The pharmaceutical composition of  claim 1 , wherein the excipient is tert-butanol. 
     
     
         3 . The pharmaceutical composition of  claim 1 , further comprising water. 
     
     
         4 . The pharmaceutical composition of  claim 1 , wherein SDC-TRAP-0063 sodium has a concentration of about 100 mg/mL. 
     
     
         5 . The pharmaceutical composition of  claim 1 , wherein SDC-TRAP-0063 sodium has a concentration of about 50 mg/mL. 
     
     
         6 . The pharmaceutical composition of  claim 1 , wherein the pH of the composition is at least 9.8. 
     
     
         7 . The pharmaceutical composition of  claim 6 , further comprising sodium chloride. 
     
     
         8 . The pharmaceutical composition of  claim 7 , wherein SDC-TRAP-0063 sodium has a concentration of about 0.1 to about 2.0 mg/mL. 
     
     
         9 . The pharmaceutical composition of  claim 1 , wherein the pH of the composition is between about 8.1 to about 9.6. 
     
     
         10 . The pharmaceutical composition of  claim 1 , wherein pH of the composition is at least about 9.3. 
     
     
         11 . A method of treating tumor in a subject in need thereof comprising administering the pharmaceutical composition of  claim 1  to the subject, thereby treating the subject. 
     
     
         12 . The method of  claim 11 , wherein the tumor is colorectal cancer, breast cancer, small cell lung cancer, sarcoma, or pancreatic cancer.