HADDONFIELD, NJ, USA I April 11, 2022 I 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 laboratory of Gary Schwartz, MD at Columbia University Irving Medical Center presented new findings from his research team at the 2022 AACR Annual Meeting.

The poster was entitled, “G protein-coupled estrogen receptor-1 agonist LNS8801 induces mitotic arrest and cell death in uveal melanoma cells” and was led by Grazia Ambrosini, PhD, a research scientist in Dr. Schwartz’s lab (Abstract 1852).

Ambrosini and colleagues have demonstrated that LNS8801 has potent anti-cancer activities in models of uveal melanoma cells. Treatment with LNS8801 resulted in inhibition of proliferation and depletion of c-Myc and phospho-RB proteins. The inhibition of proliferation was associated with a G2/M cell cycle block through the disruption of microtuble dynamics and mitotic spindle formation. LNS8801 treatment also resulted in the inhibition of migration and induction of cell death. LNS8801 had potent effects in an in vivo xenograft model of uveal melanoma, resulting in the inhibiton of tumor growth.

“We are extremely pleased to showcase these data at AACR,” commented Patrick Mooney, MD, CEO of Linnaeus. “These data demonstrate that LNS8801 has activity in preclinical models of uveal melanoma in vitro and in vivo. Importantly, these data are consistent with the clinical data in our on-going studies of LNS8801 in advanced cancer patients. We look forward to sharing some of that data at ASCO in June.”

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 clinical benefit in patients with advanced cancer.

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).

SOURCE: Linnaeus Therapeutics