Though physicians continue to advocate the benefits of balanced eating and exercise, pharmaceutical companies have spent billions of dollars and decades of research trying to develop weight loss drugs that meet FDA’s standards for efficacy and safety. But safety has historically been the downfall for so many pharmaceutical weight loss drugs—Fen-phen, Meridia and more recently, Qnexa, to name a few. That’s why San Diego, CA-based Elcelyx Therapeutics Inc. took a different route when it began the development its own unique approach to weight loss: a product that would have “drug-like efficacy and food-like safety in a supplement form.” That product, Lovidia, is based on a proprietary Generally Recognized As Safe (GRAS) mix of non-nutritive sweet, bitter and umami dietary ingredients, and delivers a satiating effect that the company said provides “a distinct safety advantage over conventional pharmaceutical approaches for treating metabolic disorders.”
Alain Baron, MD, Elcelyx’s president and CEO, explained to Nutraceuticals World that Lovidia’s weight loss benefits happen as a result of stimulation of sensory receptors in the gut, which magnify important hormones that trigger the sensation of satiety. Elcelyx named its proprietary approach Gut Sensory Modulation (GSM).
“In response to nutrient ingestion, specialized cells called enteroendocrine cells located in the lining of the gut release several hormones into the circulation,” Dr. Baron said. “These hormones include peptide YY (PYY), which signals satiety to the brain, and glucagon-like peptide-1 (GLP-1), which plays an important role in glucose regulation. We hypothesized that the nutrient-driven release of these important hormones could be amplified by delivering potent compounds to activate chemosensory receptors located on these cells.”
Dr. Baron went on to add that Elcelyx conducted a randomized, placebo-controlled, double-blinded trial designed to assess the effect of a prototype of Lovidia on weight loss in overweight and obese subjects. “In a 16-week study evaluating 121 obese subjects who were not directed to alter their diet or exercise, Lovidia demonstrated statistically significant progressive and sustained weight loss, with a threefold higher proportion of subjects losing 3-5% of their body weight compared to placebo,” he said. “The prototype was also shown to increase the body’s production of natural satiety and gluco-regulatory gut hormones twofold; with the same number of calories, subjects had twice the satiety signal. The prototype’s tolerability and safety profile was similar to placebo.”
And because Elcelyx’s GSMs work primarily in the lower gut, there is minimal absorption into the bloodstream. In addition to Lovidia, which is in development for use as an over-the-counter weight loss product for food and beverage applications, the company’s GSM platform also produced NewMet, a pharmaceutical delayed-release generic formulation of Metformin for patients with type 2 diabetes.
The low bioavailability premise, Dr. Baron said, is the primary safety advantage over conventional pharmaceutical approaches. “Our goal is to develop a product that can achieve clinically meaningful weight loss without side effects,” Dr. Baron said. “Drug safety issues are generally due to systemic absorption of the drug—a higher level of the drug in the bloodstream is believed to be necessary to achieve efficacy. However, we determined that by targeting the specialized cells in the lower gut responsible for the release of hormones that regulate glucose and satiety, both Lovidia and NewMet do not need to enter the bloodstream and therefore avoid side effects often seen with systemic therapies, including those that limit the use of two recently FDA-approved therapies for obesity.
"Because Lovidia is composed of GRAS-designated dietary ingredients that have been safely consumed for decades, it will be regulated by the FDA as a supplement,” he continued. “This allows Elcelyx to offer consumers a product that safely addresses the tremendous unmet need in obesity.”
Lovidia is still being subjected to additional clinical trials that Dr. Baron expected would provide additional scientific support. At the end of last summer, Elcelyx extended series B private equity financing ($4 million of a $7 million extension) earmarked to support clinical trials on Lovidia and NewMet. He said Lovidia should be ready for commercialization as a supplement in late 2013 or early 2014.
Though the Elcelyx team has a rich pharmaceutical background, the current entity is a largely virtual, venture-backed company (with just seven employees). Dr. Baron said he hoped the future would bring the strength and reach of a much larger healthcare company to maximize the potential of NewMet. “Within the next five years, our business plan is to either partner our products with global healthcare companies or participate in a strategic transaction,” he concluded.