Abstract: 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.

Abstract: 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—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.

Abstract: The present invention harnesses the differential expression of membrane-type matrix metalloproteinases (MT-MMPs) between human solid tumours and normal tissues to provide a systemically inactive prodrug which is selectively activated at the tumour micro-environment. The present invention provides a prodrug which is a conjugate of a taxane and a selective MT-MMP cleavable delivery vehicle.

Abstract: 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.

Abstract: The present inventors have harnessed the targeting of nanoparticles to tumour sites, combined with the tumour site specific elevated MMP-14 activity within one conjugate to simultaneously deliver a vascular disrupting agent (VDA) and a MRI contrast agent to a tumour site. The MMP activatable conjugate of the present invention provides both therapeutic and diagnostic functions—and is referred to as a “theranostic”. The theranostic conjugate of the present invention achieves the benefits of tumour 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 whilst simultaneously reducing dose-limiting systemic toxicities and provides a tool for rapidly and non-invasively identifying tumour location, monitoring drug delivery and pharmacodynamics.

Abstract: 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.

Abstract: The invention relates to compounds which are useful in the delivery of a wide variety of therapeutically useful molecules. In particular, the invention relates to compounds which are able to act as carriers for therapeutically useful molecules, and to pharmaceutical agents comprising these carriers. The compounds of the invention comprise a mono- or oligosaccharide, a lipidic moiety, and optionally a linker and/or a spacer. The pharmaceutical agents of the invention are particularly useful for oral administration.

Abstract: The invention relates to compounds which are useful in the delivery of a wide variety of therapeutically useful molecules. In particular, the invention relates to compounds which are able to act as carriers for therapeutically useful molecules, and to pharmaceutical agents comprising these carriers. The compounds of the invention comprise a mono- or oligosaccharide, a lipidic moiety, and optionally a linker and/or a spacer. The pharmaceutical agents of the invention are particularly useful for oral administration.