On March 20, 2025 Linnaeus Therapeutics, Inc. ("Linnaeus"), a privately held biopharmaceutical company focused on the development and commercialization of novel, small molecule oncology therapeutics, reported that seminal data describing Linnaeus’s clinical candidate, LNS8801, was published in Cancer Research Communications (Press release, Linnaeus Therapeutics, MAR 20, 2025, View Source [SID1234651326]). This paper characterizes LNS8801 as a developable pharmaceutical drug candidate, demonstrating its activity in cancer and highlighting a predictive biomarker.
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The manuscript, entitled "LNS8801: An enantiomerically pure agonist of the G protein-coupled estrogen receptor suitable for clinical development," was authored by Natale et al. The publication can be viewed at: View Source
This new study highlights the potential of LNS8801, a first-in-class, oral compound targeting the G protein estrogen receptor (GPER), to be used as a novel cancer therapy. Linnaeus researchers and collaborators discovered that LNS8801 is the active component of the widely studied GPER agonist, G-1. In preclinical models, LNS8801 demonstrated potent, oral, GPER-dependent anticancer effects. This study also demonstrates that a common genetic variant of GPER may influence patient response, offering a potential mechanism-linked biomarker for patient selection and personalized therapy. These findings complement the data generated in ongoing clinical trials of LNS8801 for cancer.
"The validation of our science by the acceptance of this paper in Cancer Research Communications underscores the importance of GPER as a therapeutic target," said Patrick Mooney, MD, Chief Executive Officer of Linnaeus. "This data demonstrates that using LNS8801 to target GPER has therapeutic effects in melanoma and other GPER-positive cancers and is the appropriate molecule for clinical development. We are excited by the data we have seen in our clinical phase 1/2 study, and we are poised to open enrollment in a randomized, controlled study in the near future."
Linnaeus anticipates initiating a randomized controlled clinical trial testing LNS8801 in unresectable, treatment-refractory, cutaneous melanoma patients this year. This study will randomize 135 biomarker-positive patients to receive either LNS8801 monotherapy, LNS8801 in combination with pembrolizumab, or physician’s choice therapy. The study will assess progression-free survival and overall survival between the groups.
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 has been safe and well tolerated. Additionally, LNS8801 has demonstrated target engagement, c-Myc protein depletion, and clinical benefit in patients with advanced cancers, and a predictive biomarker has been identified.