Incanthera Limited

Leland Stanford Junior University

Ellipses Pharma Limited

Robert Falconer

Jason Gill

Paul Loadman

Laurence Patterson

Michael Bibby

Jennifer Xavier

Jianghong Rao

Heike E Daldrup-Link

Jennifer Atkinson

The present invention relates to prodrugs of vascular disrupting agents comprising a vascular disrupting agent (VDA) associated with a MMP proteolytic cleavage site and to the use of such prodrugs in the targeted treatment of cancer.

Methods of treating cancer using compounds containing a vascular disrupting agent

The present inventors have harnessed the targeting of nanoparticles to tumor sites, combined with the tumor site specific elevated MMP-14 activity within one conjugate to simultaneously deliver a vascular disrupting agent (VDA) and a MRI contrast agent to a tumor site. The MMP activatable conjugate of the present invention provides both therapeutic and diagnostic functions&#x2014;and is referred to as a 'theranostic'. The theranostic conjugate of the present invention achieves the benefits of tumor site specificity, VDA delivery and MRI contrast agent delivery in a single theranostic conjugate. Consequently, the present invention provides a cancer 'theranostic' which improves therapeutic efficacy while simultaneously reducing dose-limiting systemic toxicities and provides a tool for rapidly and non-invasively identifying tumor location, monitoring drug delivery and pharmacodynamics.

Tumour-targeted theranostic

The present invention relates to prodrugs of vascular disrupting agents comprising a vascular disrupting agent (VDA) associated with a matrix metalloproteinase (MMP) proteolytic cleavage site and to the use of such prodrugs in the targeted treatment of cancer.

Compounds

Growing community of inventors

West Yorkshire, United Kingdom

Robert Falconer