— TP-113 designed to address insulin resistance, hepatic glucose output and elevated lipids —
— Study supports potential of Thetis HEALER™ Platform to transform known agents into new molecular entities with prospects for enhanced efficacy, tolerability and convenience —

SOUTHPORT, CT, USA I April 29, 2015 I Thetis Pharmaceuticals, LLC (“Thetis”) today announced the presentation of new data on a novel oral anti-diabetes drug candidate, TP-113, with the potential to reduce insulin resistance, decrease hepatic glucose output, and reduce plasma triglycerides. Thetis and its collaborators presented data on TP-113 and its mechanistic effects on the myokine-hepatic glucoregulatory axis at the Annual GTC Diabetes Summit and the 8th Diabetes Drug Discovery & Development Conference in Boston.

“Today’s oral anti-diabetic drugs do not adequately address insulin resistance and elevated lipid levels, two critical needs in the treatment of type 2 diabetes”

“Today’s oral anti-diabetic drugs do not adequately address insulin resistance and elevated lipid levels, two critical needs in the treatment of type 2 diabetes,” said Frank C. Sciavolino, Ph.D., Thetis co-founder and CSO, in an oral presentation entitled TP-113: A Novel Oral Anti-Diabetic Drug Candidate for Reduction of Insulin Resistance in Type 2 Diabetes. “TP-113 is an innovative small molecule that delivers both metformin and DHA from a single new chemical entity, which enables a product profile that includes HbA1c lowering, insulin resistance reduction, beneficial modulation of serum triglyceride levels, and multiple mechanistic effects on hepatic gluconeogenesis that offer prospects for enhanced glycemic control.”

Thetis collaborator and scientific advisor, Andre Marette, Ph.D., Professor of Medicine, Laval University, Quebec, Canada, further elaborated TP-113’s prospects as a potential diabetes drug. In an oral presentation, he described the previously unrecognized glucoregulatory activity of DHA and discussed how DHA metabolite protectin DX acts as a critical signaling molecule that enables glucose uptake in skeletal muscle and the down-regulation of hepatic glucose output.

“TP-113 is bis-metformin glutamate docosahexaenoate, an ionic compound created with our HEALER platform,” Dr. Sciavolino noted. “However, TP-113 is just one of the innovative compounds for cardio-metabolic diseases that we are developing with HEALER. Our other product candidates include TP-252, an EPA-only agent with prospects as best-in-class for treatment for reduction of triglycerides, and TP-452, a DPA-only agent for treatment of heterozygous familial hypercholesterolemia.”

About HEALER™ Platform

The HEALER (High Efficiency Amino Lipid Enabled Release) platform is a proprietary platform that uses ionic chemistry via an amino acid scaffold to efficiently design, evaluate and develop patentable new molecular entities (NMEs). Potential advantages of HEALER-created compounds include improved bioavailability and formulation options for known agents, and the ability to combine such agents with other drugs (statins, SGLT2s, DPP4s), creating novel therapeutic agents with important patient benefits. As ionic NMEs, HEALER compounds completely dissociate into their component entities in gastric fluids, precluding exposure of systemic tissues to the NME and providing the foundation for clinical development and regulatory efficiencies.

About Thetis Pharmaceuticals

Thetis Pharmaceuticals is a privately held biopharmaceutical company applying its expertise in amino-lipid chemistry to discover and develop innovative drugs for the treatment of cardio-metabolic diseases. Thetis uses its proprietary HEALER platform to transform approved drugs or previously studied biologically active agents into new chemical entities with better pharmacokinetic, pharmacodynamic or physico-chemical properties, thereby enhancing their efficacy, tolerability and patient convenience. This approach enables the development of known agents for new, previously unattainable indications and offers an approach to drug discovery and clinical development that is potentially more efficient and less expensive than conventional small molecule drug research and development. Thetis is implementing this approach to develop a robust pipeline of potential new medicines targeting major diseases including dyslipidemia and type 2 diabetes. www.thetispharma.com  

SOURCE: Thetis Pharmaceuticals