What is it about?
The aim of this article is to describe an approach to deliver and largely confine cytotoxic stress to solid tumor tissues, and micro metastatic cell clusters. Past responses have focus on releasing chemo therapies within tumor tissue but completely failed to deal with its confinement therein; as a result such previous approaches will generally exhibit very little tumor selectivity due to their initial targeting.
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Why is it important?
The 1,2-bis(sulfonyl)-1-alkylhydrazine cytotoxic warhead, possesses the properties to allow the confinement of its cytotoxic actions selectively to the target site. Due to such targeting it can exhibit selective toxicity to tumors with high MGMT (O6-alkylguanine DNA alkyltransferase) levels. However, cancers lack MGMT and this deficiency can be very selectively targeted by these agents. In some tumor types the proportion lacking MGMT can be a high as 20% of the patient population, and these would be expected to have a very beneficial response to these drugs.
Perspectives
Recently there has been considerable expansion in the types of therapies available to treat cancers, ranging including the field of immuno-therapies]. However, chemotherapy is likely to remain, in the near future, a dominant therapeutic strategy for the treatment of many cancers. Chemotherapy can be greatly improved by confining its action to tumors while sparing healthy tissue. In addition, it possesses an inherently lower cost of therapy. The 1,2-bis(sulfonyl)-1- alkylhydrazines (BSH) possess a unique combination of favorable properties that make them ideal chemotherapeutic cytotoxins for selective tumor targeting.
Dr Philip Gerard Penketh
Yale University
Read the Original
This page is a summary of: Physicochemical Considerations of Tumor Selective Drug Delivery and Activity Confinement with Particular Reference to 1,2-Bis(Sulfonyl)-1- Alkylhydrazines Delivery, Current Drug Delivery, July 2020, Bentham Science Publishers,
DOI: 10.2174/1567201817666200427215044.
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