Out-licensing

Application of Somatostatin Analogues for the Specific Delivery of Anti-tumour Drugs into Tumour Cells

Introduction/Background

Most cytotoxic anticancer drugs suffer from a common problem, ie, toxic side effects due to the lack of a selective drug delivery system. Using endocytotic ligands as carriers of the anticancer drugs to target these drugs to the cancer cells can avoid or reduce toxic side-effects and greatly improve the efficiency of these drugs' delivery.

Somatostatins function through cellular membrane receptors, known as somatostatin receptors (SSTR). These receptors are over expressed on the surfaces of certain tumour cells, such as carcinoid, islet cell of the pancreas, paragangliomas and small-cell carcinomas of lungs. Since somatostatin analogues possess such interesting properties, they may be used as a carrier system targeted to those malignant tumour cells such that the drugs can specifically act on those cells. It has been reported that somatostatin analogues labelled with chromatic or radionuclide to visualize and monitor the tumours that express SSTRs. Somatostatin analogues are particularly preferred for these applications to the original somatostatins because such analogues are known to be smaller in size, higher in affinities to the somatostatin receptors, and more metabolism stable than the original somatostatins.

Aims/Hypothesis

We are investigating the use of somatostatin analogues for the specific delivery of anti-tumour drugs into tumour cells.

Research

The present invention relates to a novel anti-cancer drug delivery system, wherein a somatostatin analogue is conjugated with an anticancer drug, such as paclitaxel, so that the anticancer drug can be delivered specifically to the targeted cancer cells.

The compound is synthesized using solid phase techniques.

Conclusion

The present invention is directed to a combination of somatostatin analogues, such as octreotide, lanreotide, and vapreotide, and a cytotoxic drug, such as paclitaxel, through a covalent bond or a physical encapsulation.

Relevance/Opportunity

We are currently seeking licensing or codevelopment partners. Please enquire if you are interested quoting reference no. 11A-880510C.

Preclinical

US6552007;