Linnaeus Therapeutics announced the U.S. Food and Drug Administration (FDA) has cleared the company's investigational new drug application (IND) for LNS8801, a small molecule agonist of the G protein-coupled estrogen receptor (GPER). Linnaeus is developing LNS8801 for the treatment of solid and hematologic cancers.

"The FDA clearance of the IND allows Linnaeus to begin human testing of LNS8801 and represents the culmination of a tremendous effort by our research and development team," said Patrick Mooney, MD, chief executive officer of Linnaeus. "LNS8801 is a potent and highly selective small molecule agonist of GPER. Based on the epidemiological evidence and the strong preclinical data, we believe that LNS8801 has very real potential to provide meaningful and lasting clinical benefit for patients with cancer. We are excited to enroll our first patient in the coming weeks."

FDA allowance of the IND enables Linnaeus to initiate its planned phase 1/2 clinical trial in patients with advanced cancers. 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. Linnaeus expects the first patient to be enrolled in the trial in October 2019.

LNS8801 is an orally bioavailable, 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 significant antitumor activity, including complete responses that are immune to rechallenge. LNS8801 also has combinatorial effects with targeted therapies and immunotherapies. Preclinical toxicology studies have established a wide safety margin.

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