Acid Labile Linker for Cancer-Targeted Drug-Conjugates

Abstract

Controlled chemical release is an increasingly critical characteristic in targeted therapy. Controlling chemical release via selective drug delivery has been the focus of significant research efforts to reduce off target effects associated with therapy, especially with regards to cancer chemotherapy. In many controlled release applications, it is desirable for a chemical structure to allow little or no chemical release at normal physiological conditions but, allow for the release of the active compound from the carrier only in the presence of a disease state. The ideal characteristics of such a chemical structure would be that the rate of chemical release could be tailored to release the active compound once it had encountered the disease state that was being targeted. There are a number of applications for such a technology, but the most prominent trends tend to be in the field of targeted drug delivery via antibody-drug conjugates and drug eluting stents. But, it is reasonable to consider that the technology could be applied to prodrug design, intracellular probes, and degradable polymers just to name a few applications.

The most promising and impacting embodiments of the invention relates to a tunable functional group that will trigger the release of a drug or other molecule given a targeted set of conditions. More specifically, one embodiment relate to a prodrug functional group, which will allow for a rapidly releases of the drug once introduced to a select cancer. But, this platform technology can be modified to be adaptable to a variety of applications.

Applications and Advantages

• This method is a cell-specific delivery system that utilizes a patented functional group to deliver a desired therapeutics to a specific tumor cell.

• This technology is a platform technology that can be adapted to a number of applications

• Attachment of drug conjugates are done via click chemistry

IP Status

PCT Application