Prodrugs of PKC modulators for improved formulation, therapeutic efficacy and tolerability

Researchers at Stanford have developed prodrug derivatives of protein kinase C (PKC) modulators that have lower toxicity and are more effective than the parent compound. PKC modulators are being developed to treat a variety of diseases. However, these drugs have problems that may limit their use clinically; including difficult formulations, stability and toxicity issues and non-optimal efficacy. To overcome these problems the inventors have developed this technology which provides novel prodrugs of PKC modulators as well as methods for the design and synthesis of such prodrugs. The prodrugs extend the therapeutic window and have increased efficacy and decreased toxicity as compared to the parent compounds and thus may serve as superior therapeutics.

Stage of research
The prodrugs have been shown to be effective in cells and live animals. Additional development is ongoing.