On March 3, 2021 Linnaeus Therapeutics, Inc. (Linnaeus), a privately held clinical-stage biopharmaceutical company focused on the development and commercialization of novel small molecule oncology therapeutics, reported that on March 2, 2021 the U.S. Patent and Trademark Office (USPTO) issued U.S. patent 10,934,277 (‘277 patent) covering various embodiments of the pharmaceutical composition of matter for the company’s lead compound, LNS8801 (Press release, Linnaeus Therapeutics, MAR 3, 2021, View Source [SID1234576039]).
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Linnaeus’s patent disclosure is directed toward the pharmaceutical composition of matter of LNS8801 and generally embodies (1) an enantiomerically purified compound SRR G-1, or a derivative thereof, including specific crystal forms, salts, and co-crystals, that modulates G protein-coupled estrogen receptor activity; (2) pharmaceutical and cosmetic compositions comprising an enantiomerically purified SRR G-1, or a derivative thereof; and (3) methods of treating or preventing disease states and conditions and cosmetic conditions mediated through these receptors and related methods thereof in humans and animals.
"We are extremely pleased that the USPTO has issued this first patent under its expedited review format," commented Patrick Mooney, MD, CEO of Linnaeus. "We believe that the issued claims will provide critical market protection for LNS8801 through at least 2038. As we continue to collect very promising data from our clinical trials of LNS8001, we plan to prosecute the ‘277 patent, both on a worldwide basis and an on-going effort in the U.S."
Linnaeus is testing LNS8801 in its phase 1/2 adaptive-design clinical trial as a monotherapy and in combination with KEYTRUDA (pembrolizumab) in patients who had previous clinical benefit from immune checkpoint inhibitors and then subsequently progressed. This marks the first time any company has dosed a patient in a clinical trial specifically targeting the G protein-coupled estrogen receptor (GPER) in combination with pembrolizumab.
Linnaeus is currently finishing the dose-escalation portion of its phase 1/2 study assessing the safety, tolerability, pharmacokinetics, and preliminary efficacy in patients with advanced cancer, and the company has already identified the phase 2 dose for LNS8801 as a monotherapy and in combination with pembrolizumab.
About LNS8801
LNS8801 is an orally bioavailable and highly specific and potent agonist of GPER whose activity is dependent on the expression of GPER. GPER activation by LNS8801 rapidly and durably depletes c-Myc protein levels. In preclinical cancer models, LNS8801 displays potent antitumor activities across a wide range of tumor types, rapidly shrinking tumors and inducing immune memory.
In the ongoing phase 1/2 study in humans, LNS8801 monotherapy has been safe and well tolerated. Additionally, LNS8801 has demonstrated target engagement, c-Myc protein depletion, and clinical benefit in patients with advanced cancer. Data from the phase 1/2 study are anticipated to be presented in a peer-reviewed setting in 2021.