Haddonfield NJ, June 10, 2020 — Linnaeus Therapeutics, Inc. (Linnaeus), a privately held clinical-stage biopharmaceutical company focused on the development and commercialization of novel small molecule oncology therapeutics, today announced that its scientific cofounders, Christopher Natale, PhD, Vice President of Research at Linnaeus and Todd Ridky, MD, PhD, Assistant Professor of Dermatology at the Perelman School of Medicine at the University of Pennsylvania, presented their findings on a new therapeutic target for pancreatic cancer in the journal Cellular and Molecular Gastroenterology and Hepatology (https://pubmed.ncbi.nlm.nih.gov/32376419/).
The peer-reviewed article, entitled “Pharmacologic Activation of G Protein-Coupled Estrogen Receptor Inhibits Pancreatic Ductal Adenocarcinoma” was authored by Natale et al. Using a small molecule agonist of the G protein-coupled estrogen receptor (GPER), the authors demonstrated that GPER activation inhibits the growth of multiple pancreatic ductal adenocarcinoma cancer (PDAC) models and has combinatorial effects with immune checkpoint inhibitors. The authors also demonstrated that GPER protein can be detected in a large percentage of clinical specimens, suggesting that GPER may represent a new therapeutic target for PDAC.
“It’s exciting to learn that the anticancer activity we observed with GPER agonists in our first studies in melanoma models extends to pancreatic cancer and many other cancer types and that these agents have a therapeutic synergy with modern immunotherapy. We are eager to continue working to identify new cancer types that could be targeted using GPER agonists,” said Dr. Natale. “We are excited to see if these data translate to our current phase 1/2 clinical trial in patients with advanced cancer.
LNS8801 is an orally bioavailable and highly specific agonist of GPER whose activity is dependent on the expression of GPER. GPER activation suppresses well-known tumor-associated genes, such as c-Myc and PD-L1. In preclinical cancer models, LNS8801 displays potent antitumor activities across a wide range of tumor types, rapidly shrinking tumors and inducing immune memory. LNS8801 monotherapy has shown significant antitumor activity, including inducing complete responses that are immune to rechallenge. LNS8801 also has shown effects when combined with targeted therapies and immunotherapies. LNS8801 is currently in a phase 1/2 clinical trial in patients with advanced cancer at six comprehensive cancer centers in the United States.
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