On April 2, 2024 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 6, 2024, the European Patent Office (EPO) issued EP patent 3,823,617 (‘617 patent) covering the pharmaceutical composition of matter for the company’s lead compound, LNS8801 (Press release, Linnaeus Therapeutics, APR 2, 2024, View Source [SID1234641712]).
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Linnaeus’s patent disclosure is directed toward the pharmaceutical composition of matter of LNS8801 and 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 EPO has issued this composition of matter patent," commented Patrick Mooney, MD, CEO of Linnaeus. "We are thrilled to have these issued claims in both the US and Europe, and we believe that they will provide critical market protection for LNS8801 into the 2040s. As we continue to collect very promising data from our clinical trials with LNS8001, we will continue to prosecute the claims in this patent worldwide."
Linnaeus is currently conducting an open-label phase 1/2 study assessing the safety, tolerability, pharmacokinetics, and preliminary efficacy in patients with advanced cancer, including cutaneous melanoma.
Based on promising data from the phase 1/2 study, Linnaeus plans to initiate a potentially pivotal, randomized controlled trial in patients with metastatic cutaneous melanoma who have had confirmed progression on immune checkpoint inhibitors. The study will enroll 135 patients who will be selected based on a predictive biomarker and then randomized to receive LNS8801 alone, LNS8801 and pembrolizumab, or physician’s choice therapy. Key endpoints will include an analysis of progression-free survival and overall survival between the treatment groups. Over 25 comprehensive cancer centers in the United States are eager to participate in this study.
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 clinical study in humans, LNS8801 monotherapy has been safe and well tolerated. Additionally, LNS8801 has demonstrated target engagement, c-Myc protein depletion, and durable clinical benefit in patients with advanced cancers, and a predictive biomarker has been identified.
About Metastatic Cutaneous Melanoma
Although there has been progress in the treatment of metastatic cutaneous melanoma, most patients will progress on standard-of-care therapies and need further treatment. According to the American Cancer Society, almost 8000 patients die each year in the United States, highlighting the need for safe and effective therapies in the treatment-refractory setting.