Biospherics’ lead clinical candidate is D-Tagatose, a naturally occurring simple sugar being developed as an oral treatment for glycemic control in patients with Type 2 diabetes and other indications. D-Tagatose has been recognized by the U.S. Food and Drug Administration (FDA) as a GRAS (Generally Recognized as Safe) substance for use in food and beverages since 2001.
Structurally,
D-Tagatose is a naturally occurring stereoisomer of D-fructose, and
resulted from the application of Biospherics’ expertise in chiral
carbohydrate chemistry to create L-sugars that would retain their
sweetness characteristics without being metabolized. Originally
developed as a reduced-calorie sugar substitute, D-Tagatose is poorly
absorbed in the small intestine, thus preventing the stimulation of
insulin secretion and lowering blood glucose levels. D-Tagatose passes
directly to the lower intestine, where it is fermented by bacteria to
produce short-chain fatty acids and carbon dioxide. It is considered a
prebiotic, promoting more favorable microbial flora in the colon.
Biospherics is running a Phase 2 clinical trial studying the dose-response effect of minimal doses of D-Tagatose on glycemic control in subjects with Type 2 diabetes under diet control and exercise. It is a six-month, multi-center, single-blinded, randomized parallel study. Preliminary results of the trial were encouraging, with the group receiving 7.5 grams of D-Tagatose averaging a 0.3% reduction in HbA1c (blood glucose level) versus the group receiving 2.5 grams, and the group receiving 5.0 grams of D-Tagatose averaging a reduction in HbA1c of 0.05% versus the 2.5 gram group. In addition, triglycerides (a measurement of fat in the bloodstream) were reduced by 59 mg/dl, low-density lipoproteins (LDL, or “bad” cholesterol) were lowered an average of 13 mg/dl and high-density lipoproteins (HDL or “good” cholesterol) were raised an average of 0.9 mg/dl. The overall LDL:HDL ratio of the subjects in the trial improved by 0.3.
D-Tagatose is currently being studied as an adjunct to diet
and exercise to improve glycemic control in patients with Type 2
diabetes in a double-blind, randomized Phase 3 study at 62 sites in the
U.S. and India. The study is powered to detect a 0.5% reduction in
HbA1c as its primary endpoint, with secondary endpoints establishing
glucose, insulin and lipid profiles and measuring changes in body
weight.
Spherix has intellectual property protecting D-Tagatose, with 2 issued U.S. patents and one patent pending. In addition, if approved, D-Tagatose is likely to receive at least five years of market exclusivity as a result of the Hatch-Waxman extension for new chemical entities.