Diagnostic or therapeutic somatostatin or bombesin analog conjugates and uses thereof

Abstract

Disclosed are peptide agents and uses thereof that are analogs of biologically active peptides such as somatostatin and bombesin. The compounds of the invention have the general formula X-Y-Z-Q, where X is a cytotoxic agent, therapeutic agent, detectable label or chelating group, and Q is a biologically active peptide. In peptide agents of the invention Y is optionally a hydrophilic polymer or peptide, and Z is a linking peptide bonded to Q at the amino terminus of Q, having two, three, four, or five, amino acid residues selected to link X to Q, while retaining the biological activity of Q. Methods of using these peptide agents in the diagnosis and treatment of diseases are also disclosed.

Description

Field of Invention

[0001] The present invention relates to somatostatin and bombesin analogs and uses thereof for targeting compounds useful in the detection, diagnosis or treatment of disease. Background technique

[0002] The toxic side effects of many treatments, including standard treatments for cancer, effectively limit the amount of agents that can be administered to a patient. Additionally, many agents cause organ-specific toxicity, further limiting the dose that can be delivered to target tissues. For example, the cardiotoxicity of many members of the anthracycline family reduces the maximum therapeutic dose available for this group of chemotherapeutic agents. Targeted drug delivery of various detectable or therapeutic agents can reduce toxicity in normal tissues and increase the efficacy of treatments by providing concentrated local effects in specific tissues.

[0003] Somatostatin, bombesin, or other bioactive peptide analogs have been used to detect tumor cells...