Edison

Edison’s chemistry discovery strategy is based on developing drugs using compounds that carry electrical current and that cross couple into energy generating and supply pathways. Today, drug development is generally an exercise in systematically changing the chemical structural shape to optimize function. While shape and function are critical, non-shape variables also contribute to drug action. The company believes that one such variable, the ability to reversibly shuttle electrons, [redox] is an essential property that has been largely overlooked by medicinal chemists. The company possesses multiple redox scaffolds, however is focusing its initial attention on one particular class– quinones. Despite the observation that quinones as a class are redox active and highly represented across multiple disease indications there is a surprising absence of tools to optimize the redox parameter of quinones. Edison is deploying this library and its knowledge of redox optimization, to discover and develop quinone-based drugs

A. Edison is engineering improved CoQ10-based drugs for diseases where CoQ10 has demonstrated real, but limited clinical benefit. The Company’s strategy is to discretely alter the structure of CoQ10 to identify the optimal redox and solubility properties required for drug action.

B. Edison’s core skill is redox chemistry. Redox, short for oxidation-reduction, is a type of chemical reaction where electrons are transferred from one chemical to another. While considerable attention has been focused on altering CoQ10s solubility, minimal consideration has been given to optimizing its redox head– critical for cross coupling into redox reactions– as a means to enhance efficacy. Cyclic voltammetry is one method used to measure the redox properties of a chemical. A cyclic voltammogram of a redox-active compound is a fingerprint of its ability to reversibly or irreversibly undergo a redox transformation at a defined voltage potential.

A. Edison has assembled a library of over 5,000 individual, characterized analogs of CoQ10 that systematically differ in the redox properties of the quinone head and the cLogP properties– a measure of lipid solubility, of the lipid tail. The Company’s scientists routinely screen members of this proprietary library to identify the optimal chemical properties (redox and cLogP) it believes are required of an optimized CoQ10 drug.

B. Edison’s Redox Platform™ enables the efficient identification of optimal redox and cLogP properties required to target cellular redox defects. In this experiment, compound optimization was carried out for a typical inherited respiratory chain mitochondrial disease. 400 discrete redox and cLogP variations on the benchmark– CoQ10 were screened for biological activity and rank-ordered based on potency. A 100-fold enhancement in activity was observed for over ~100 compounds demonstrating the efficiency of the Redox Platform™.