Company Commences First-in-Human Study at Multiple Academic Sites in United States
Haddonfield NJ,October 29, 2019–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 it has dosed the first patient in its phase 1/2 clinical trial of LNS8801 in patients with advanced solid and hematologic cancers. This marks the first time any company has dosed a patient in a clinical trial specifically targeting the G protein-coupled estrogen receptor (GPER). The initiation of the study follows U.S. Food and Drug Administration (FDA) clearance of the company’s investigational new drug application (IND) for LNS8801 in late September.
LNS8801 is an orally bioavailable small molecule that is a highly specific and potent agonist of the GPER.
“We are thrilled to begin testing LNS8801 in patients with advanced cancer. We will have six outstanding academic comprehensive cancer centers all enthusiastically recruiting patients for this promising study,” commented Patrick Mooney, MD, chief executive officer of Linnaeus. “LNS8801 has very real potential to provide meaningful and lasting clinical benefit for patients with cancer, and we look forward to providing updates over the course of the study.”
The study entitled, “A Multicenter Study to Assess the Safety, Tolerability, Pharmacokinetics, and Antitumor Activity of LNS8801 in Patients with Advanced Cancer,” is designed in two parts. The phase 1 dose-escalation portion of the trial will assess the safety, tolerability, pharmacokinetics, and preliminary antitumor activity of LNS8801. After a recommended phase 2 dose is established, dose expansion cohorts are anticipated.
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. Preclinical toxicology studies have established a wide safety margin.
Linnaeus Therapeutics, Inc. is a privately held biopharmaceutical company focused on the development and commercialization of novel, small molecule oncology therapeutics that target a novel G protein-coupled receptor, known as GPER, or GPR30. The company was launched through the UPstart incubator at the University of Pennsylvania’s Penn Center for Innovation (PCI) Ventures. Its lead molecule, LNS8801, is in the final stages of preclinical development. The Company expects to begin its phase 1 clinical program in the summer of 2019. In addition to developing GPER agonists, Linnaeus is also currently focusing on developing small molecules that activate other G protein-coupled receptors to engage tumor-suppressive cellular signaling pathways.
Chief Executive Officer