Thetis Receives Notice of Allowance for Patent Covering Pharmaceutical Compositions of Novel Mineral Amino Acid Derivatives

SOUTHPORT, CT--(Marketwired - Aug 4, 2015) - Thetis Pharmaceuticals LLC ("Thetis"), a development stage pharmaceutical company applying its expertise in amino lipid chemistry to develop innovative therapeutics, announced today receipt of a Notice of Allowance from the USPTO for its patent application covering pharmaceutical compositions of novel mineral amino-acid derivatives of docosapentaenoic acid (DPA), eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA).

The new molecular entities described by this patent are solid, stable, free flowing powders that dissociate completely in the GI tract to deliver high plasma and tissue levels of DPA, EPA and DHA in the free acid form. By "pharmaceuticalizing" omega-3 fatty acids, Thetis is enabling the development of therapeutically differentiated agents in multiple disease areas.

Frank Sciavolino, Ph.D., chief scientific officer and co-founder of Thetis, said, "This composition-of-matter patent is unique in the omega-3 arena which is dominated by formulation, method of use and process patents. It covers two of our lead product candidates: TP-252 for treatment of familial adenomatous polyposis (FAP) and TP-452 for treatment of hypercholesterolemia. We expect to advance both drugs into clinical studies in 2016."

About TP-252
TP-252 is a novel derivative of eicosapentaenoic acid (EPA) with prospects to reduce polyp burden in FAP patients and delay the need for surgery. FAP is a dominantly inherited condition resulting in formation of numerous large bowel adenomas (polyps) in late childhood or adolescence. If left untreated, patients inevitably develop colorectal cancer by middle age. There are no drugs currently marketed for the treatment of this condition. Due to the increasing number of adenomas in this young population, prophylactic cancer preventive colorectal surgery during the late teenage years or early twenties is the advocated management paradigm for this disease.

Investigators at Leeds (UK) have shown in a Phase II study that EPA free fatty acid (EPA FFA) significantly reduces polyp burden in FAP patients (cf., Gut (2010) 59, 918-925). The active agent in TP-252 is EPA FFA. Demonstrated efficacy of EPA-FFA in reducing polyp burden coupled with its favorable safety profile suggests TP-252 has good prospects to improve clinical practice in treating FAP patients. Due to the profound physical and emotional trauma of surgery and the resulting impact on quality of life in this youthful population, the prospect of delaying surgery with a safe drug that could be used chronically in young patients may be highly desirable.

About TP-452
TP-452, a novel derivative of docosapentaenoic acid (DPA), has potential as adjunct therapy to statins for oral treatment of elevated LDL cholesterol (LDL-C). Nearly 79 million adults in the United States have high LDL-C, and approximately 27 million are treated with statins, the standard of care for this condition. Despite treatment, nine million statin users still have uncontrolled LDL-C. 

Laboratory findings suggest that DPA could exert unique synergistic anti-hyperlipidemic effects in combination with statins (cf., PLEFA (2011) 85, 155-161). Further, preclinical and clinical observations indicate that DPA down-regulates both HMGCoA reductase and PCSK-9. Through these dual pharmacological actions, DPA has prospects for reducing cholesterol biosynthesis and increasing LDL receptor levels. Based on these data, we believe TP-452 may be a highly differentiated therapeutic agent for reduction of LDL-C in patients not at treatment goal.

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 cardiometabolic and other 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 and rare diseases.