Technologies
This technology is a set of ferrostatin-1 (Fer-1) derivatives optimized for enhanced stability and solubility to serve as therapeutic candidates against pathologies driven by ferroptosis.
Ferroptosis is a form of iron-dependent programmed cell death characterized by the accumulation of lipid reactive oxygen species (ROS). While the small molecule ferrostatin-1 (Fer-1) has been discovered as a inhibitor of ferroptosis, it lacks metabolic and microsomal stability which limits its efficacy in physiological settings. There is currently a lack of stable ferroptosis inhibitors in development that have the drug-like properties, such as high bioavailability and water solubility, required to effectively protect tissues and organs in in vivo models of degenerative diseases.
This technology consists of a series of ferrostatin-1 (Fer-1) derivatives designed through structure-activity relationship (SAR) analysis to improve the drug-like properties of the original Fer-1 molecule. The synthesized lead analog, SRS 15-72, demonstrates significantly improved microsomal stability and calculated solubility (cLogP) while maintaining potent inhibition of oxidative cell death. By overcoming the metabolic limitations of earlier probes, these optimized derivatives offer a viable pathway for in vivo testing and potential therapeutic development to protect neural and somatic cells from ferroptosis-induced injury.
This technology has been validated in vitro through potency, stability, and bioavailability testing of the synthesized analogs in multiple disease and tissue models.
Patent Issued (US10,259,775)
IR CU14077, CU17132
Licensing Contact: Joan Martinez