GSK Acquires Sitari Pharmaceuticals to Advance TG2 Inhibitor for Celiac Disease Treatment

On September 17, 2019, VCBeat (WeChat ID: vcbeat) learned from foreign media reports that pharmaceutical giant GlaxoSmithKline (GSK) announced the acquisition of biopharmaceutical company Sitari Pharmaceuticals (Sitari). No financial terms of the acquisition were disclosed.

Upon completion of this acquisition, GSK will incorporate Sitari’s development program for a transglutaminase 2 (TG2) inhibitor for the treatment of celiac disease, thereby expanding its portfolio of therapies for autoimmune diseases.

TG2 is a monomeric protein that catalyzes intramolecular and intermolecular covalent cross-linking of protein polypeptides, thereby enhancing their structure and function. This enzyme imparts foaming, emulsifying, stabilizing, and water-retaining properties to proteins, making it suitable for individuals with compromised immune systems.

Celiac disease, also known as gluten-sensitive enteropathy or non-tropical sprue, is an autoimmune disorder with a higher incidence in North America, Northern Europe, and Australia. The disease primarily affects the intestines and is more prevalent in women than in men. Studies have shown that celiac disease may result from the interplay of genetic predisposition, immune response, and dietary gluten intake. Patients commonly present with symptoms such as diarrhea, abdominal pain, nausea, vomiting, and fatigue.

TG2 is considered one of the pathogenic factors in celiac disease, and its abnormal levels can trigger autoimmune disorders. Studies have shown that this enzyme catalyzes the conformational change of dietary gluten peptides, thereby driving disease progression. Sitari has been dedicated to developing TG2-targeted inhibitors to provide new therapeutic options for patients with celiac disease.

Sitari, a biotechnology and pharmaceutical company founded in 2013 and headquartered in San Diego, California, USA, was established as a joint venture between GSK and Avalon Venture, a life sciences-focused venture capital firm. In November 2013, the company completed a $10 million Series A financing round led by these two founding entities.

Sitari is dedicated to the research and development of TG2 inhibitors, aiming to develop novel therapies for autoimmune diseases involving the human digestive system. The company believes that targeted inhibition of TG2 can mitigate protein-triggered autoimmune responses, thereby treating intestinal inflammation, celiac disease, and their complications. Additionally, Sitari is developing therapeutic agents for a variety of other disease indications.

GSK, established in 1929 and headquartered in the United Kingdom, is a globally leading pharmaceutical company. The company is a pioneer in the treatment of central nervous system, respiratory, gastrointestinal, metabolic, and infectious diseases, and ranks at the forefront of the industry in vaccine and oncology drug research and development. Additionally, GSK manufactures over-the-counter medications, oral care products, and nutritional supplements.

In addition to GSK and Sitari, companies such as Amgen, ImmunogenX, and Celimmune are all developing therapeutics for celiac disease. Recently, biopharmaceutical company ActoBio Therapeutics submitted an Investigational New Drug (IND) application for AG017, an oral investigational candidate for the treatment of this condition. In May of this year, Genentech and Parvus Therapeutics reached an agreement to jointly develop novel therapies for celiac disease.

John Lepore, Senior Vice President of Drug Development at GSK, stated: “Sitari’s TG2 inhibitor development program complements GSK’s research portfolio in genetic and immune-mediated diseases. Currently, patients with celiac disease must strictly adhere to a gluten-free diet as prescribed, yet many still experience gastrointestinal discomfort and disease progression. TG2 inhibitors will bring new hope to millions of patients with celiac disease.”

(Compiled by Xu Xiaoxue)