UNM Rainforest Innovations

A drug discovered more than a decade ago at UNM and NMSU by Dr. Eric Prossnitz (UNM) and Dr. Jeffrey Arterburn (NMSU) and combined with a drug discovered at the University of Pennsylvania in 2017 has received FDA clearance as an Investigational New Drug (IND).  The new drug will now advance to human clinical trials for patients with advanced cancers.  The co-inventors on the team effort that discovered the compound included  researchers Tudor I. Oprea, Cristian-George Bologa, Larry A. Sklar, Chetana M. Revankar, Alexander Kiselyov, Sergey Tkatchenko, Susan M. Young, Daniel Cimino, and Bruce S. Edwards.

In 2005, the UNM team characterized a new estrogen-binding receptor, named GPER (G protein-coupled estrogen receptor).  Estrogen and its receptors regulate many physiological and pathological processes in the human body. Since GPER specifically modulates responses to estrogen in many different cell types, finding small molecules that activate or inhibit GPER could potentially treat many diseases.  The UNM team in collaboration with the UNM Center for Molecular Discovery identified G-1, a small molecule that specifically activates GPER, without acting on other estrogen receptors. The team discovered in mouse models that G-1 had beneficial effect on multiple diseases such as cancer, diabetes, obesity, and cardiovascular disease.

The University of Pennsylvania team, led by Dr. Todd Ridky, discovered in mouse models that G-1 had potent activity against melanoma.  By combining G-1 with an anti-PD-1 antibody, the Penn team discovered that the combo decreased proliferation of melanoma cells by inhibiting the c-Myc protein, a driver of melanoma and other cancers.  The new combinational therapeutic made the melanoma cells more susceptible to elimination by the immune system.

These discoveries led to the formation of startup Linnaeus Therapeutics.  The company licenses G-1 and related compounds from STC.  To read more about the company’s progress and IND approval, see the press release below.

Linnaeus Therapeutics Announces FDA Clearance of Investigational New Drug Application for LNS8801

Company Set to Commence Phase 1/2 Clinical Trial in Patients with Advanced Cancer

NEWS PROVIDED BY Linnaeus Therapeutics, Inc. 

Sep 24, 2019, 09:00 ET

HADDONFIELD, N.J., Sept. 24, 2019 /PRNewswire/ — 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 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,” commented 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.

About LNS8801
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.

About Linnaeus
Linnaeus Therapeutics, Inc. is a privately held, clinical-stage biopharmaceutical company focused on the development and commercialization of novel, small molecule oncology therapeutics that target G protein-coupled receptors. The company was formed and launched in partnership with the UPstart incubator at the University of Pennsylvania’s Penn Center for Innovation (PCI). The company expects to begin its first phase 1 clinical trial in patients with advanced cancer imminently.

SOURCE Linnaeus Therapeutics, Inc.

Related Links


Skip to content