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Tumour vasculature targeting agents in hybrid/conjugate drugs

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Abstract

Tumour vasculature targeting has been a very active area of cancer drug discovery over the last decade. Growth of solid tumours beyond a certain point requires a sufficient blood supply in order for them to develop and metastasise. While novel anti-angiogenic and vascular disrupting agents represent an important contribution to the armoury of anti-cancer agents they nevertheless usually require combination with standard cytotoxic therapy in order to demonstrate positive clinical outcomes. In line with this consensus, a new concept has arisen, namely the design of functional hybrids where at least one component of the design targets a tumour angiogenic/vasculature pathway. This review will outline examples of such hybrid/conjugate-based approaches. Emphasis will be placed on their preclinical evaluation with particular focus on the RGD/NGR-conjugates, heparin-related hybrids and antibody-drug conjugates. In conclusion, the benefits and shortcomings of hybrids under development will be discussed in the context of future directions and applications.

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  1. School of Pharmacy and Pharmaceutical Sciences, Trinity College Dublin, Dublin 2, Ireland

    E. M. Prokopiou, S. A. Ryder & J. J. Walsh

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  1. E. M. Prokopiou
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Prokopiou, E.M., Ryder, S.A. & Walsh, J.J. Tumour vasculature targeting agents in hybrid/conjugate drugs. Angiogenesis 16, 503–524 (2013). https://doi.org/10.1007/s10456-013-9347-8

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