Patent Evaluation: Somatostatin Analogues as Tyrosine Kinase Inhibitors

Summary

Novelty: Novel octa or heptapeptide derivatives which inhibit tyrosine kinase activity are disclosed. They are potentially useful in regulating the release of growth hormone (GH), insulin, glucagon and prolactin, and for inhibiting tumour growth. The compounds can also be used to inhibit psoriasis, elicited by the pathological proliferation of skin cells.

Biology: Inhibition of GH was measured on rat hypophysis; the specified compound showed a 46% inhibition of cell division in MCF7 cells at 10 μg. The antimetastatic effect on Lewis lung tumour (LLT) count of metastases was 43%. Its tyrokinase activity in HT29 cell line at 10 μg showed an inhibition of 44%.

Chemistry: Detailed preparation of twenty-one peptides are described using known methods. The specified compound is aspartyl-(indolinyl)-Cys-Tyr-D-Trp-Lys-Val-Cys-Thr-NH₂ and is one of nine specifically claimed compounds.