Pharmaceutical Breaking

Aug 14, 2024

Not to be confused with the newly minted Olympic sport of breaking, which featured the instantly memeable routine of Australian University lecturer, Rachael Gunn aka “Raygun,” shown above, is pharmaceutical breaking. The indubitable champion of pharmaceutical breaking is lead EpicentRx therapy, RRx-001 (nibrozetone), which twists and folds on itself to dissociate or break apart and release therapeutic molecules like nitric oxide (NO) in the vicinity of diseased tissues, as illustrated below.

Well-defined therapeutic effects of NO are protection against ischemia-reperfusion (IR) injury, dilation of coronary blood vessels, scavenging of free radicals, and inhibition of clotting. NO deficiency is a central feature of several conditions including essential hypertension (high blood pressure), heart failure, angina, glaucoma, asthma, erectile dysfunction, pulmonary hypertension, type II diabetes, chronic kidney disease, mitochondrial disorders, and prostate hyperplasia etc., which makes the NO donor, RRx-001, a broadly active therapeutic.

The problem with other so-called NO donors like the FDA-approved nitroglycerin is that they release nitric oxide everywhere whereas RRx-001 only releases it in and around diseased tissues, which increases the concentration of nitric oxide locally and prevents systemic side effects.

Now, breaking is reportedly not on the program for the Los Angeles Olympics in 2028, which means that Raygun’s inimitable performance was likely a one-and-done, much to the disappointment of TikTokers everywhere who put Raygun at the center of their memes. But, hopefully for patients around the world with diseases and conditions of unmet medical need like severe oral mucositis, cancer, endometriosis, Parkinson’s, ALS/MND, and general CNS toxicity, RRx-001 aka “NOgun” will continue its well-choreographed breaking routine for years and years to come.