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SERPINB3 INHIBITOR FOR TUMOR TREATMENT

1-piperidine propionic acidAdjuvant therapycancerResistant tumorsSerpin B3 inhibitor

Introduction

This patent protects the use of the compound 1-piperidin propionic acid as a novel adjuvant drug in the treatment of different types of solid tumors resistant to chemotherapy that overexpress SerpinB3.

Technical features

The aim of the invention is to provide a novel drug for the treatment of tumors resisitant to chemotherapy expressing SerpinB3 (or SCCA-1, squamous cell carcinoma antigen-1), based on the inhibition of SerpinB3 production. Data has shown the involvement of SerpinB3 in the carcinogenesis as it determines resistance to apoptosis, induces cell proliferation and greater cell invasiveness. Furthermore, it leads to impaired immune surveillance and reduced chemosensitivity. Recent studies have documented that SerpinB3 is expressed in primary liver tumors with poor prognosis, in more advanced stage of colon and pancreatic tumors, in tumors of the lung, oesophagus, breast and ovary with poor response to chemotherapy.

In particular the invention provides the following characteristics:

  • 1-piperidine propionic acid is able to reduce the synthesis of SerpinB3 in tumor cells that express high levels of this molecule and the cell proliferation induced by it.
  • 1-piperidine propionic acid reduces the expression of genes that determine resistance to chemotherapy.
  • 1-piperidine propionic acid enhances the efficacy of antineoplastic drugs in tumor cells expressing SerpinB3.
  • 1-piperidine propionic acid significantly reduces the synthesis of inflammatory cytokines involved in tumor-typical immune deficiency.

The development is currently in the pre-clinical phase.

Possible Applications

  • treatment of tumors resistant to chemotherapy that overexpress SerpinB3 (liver, colon, pancreas, lung, oesophagus, breast, ovary).

Advantages

  • Adjuvant  to cancer therapy for solid tumors resistant to chemotherapy;
  • Readily available compound;
  • Stable compound.