Linnaeus Therapeutics Announces Presentation of Positive Clinical Data of LNS8801 at 2022 ASCO Annual Meeting

Haddonfield NJ, June 6, 2022 — 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 the presentation of clinical data from its phase 1/2 clinical trial of LNS8801 in combination with pembrolizumab in patients who have developed secondary resistance to anti–PD-1/L1 therapy at the 2022 ASCO Annual Meeting. 

The poster is entitled, “Phase 1b study of the novel first-in-class G protein-coupled estrogen receptor (GPER) agonist, LNS8801, in combination with pembrolizumab in patients with immune checkpoint inhibitor (ICI)-relapsed and refractory solid malignancies.” 

In the dose-escalation portion of the study, LNS8801 demonstrated exceptional safety and tolerability. With monotherapy, no dose-limiting toxicities (DLTs) or treatment-related serious adverse events were observed, and the combination of LNS8801 and pembrolizumab was confirmed to be safe and tolerable with no DLTs observed. The recommended phase 2 dose of LNS8801 was identified as 125 mg daily as a monotherapy and in combination with  pembrolizumab (200 mg every 3 weeks). Predictive, prognostic, and confirmatory biomarkers have been shown to correlate well with anticancer activity and clinical benefit. These biomarkers are being further validated and will aid in the selection of patients in future clinical studies. 

The combination  of LNS8801 with pembrolizumab has demonstrated strong signals of activity in patients with metastatic cancer who had previously benefited from and then developed secondary resistance to ICI therapy.  An objective response rate of 15.4% was achieved, with 2 of 13 evaluable patients achieving confirmed partial responses. A disease control rate of 69.2% was observed, with 9 of 13 evaluable patients achieving partial responses or stable disease. Four patients have already remained on study longer than 6 months with ongoing benefit for the duration of therapy. The combination of LNS8801 and pembrolizumab is tolerable without unanticipated toxicities. 

“We are very pleased to showcase these data at ASCO,” commented Patrick Mooney, MD, CEO of Linnaeus. “LNS8801 continues to be extremely safe and well tolerated and shows very promising activity in combination with pembrolizumab. It is important to note that the disease control rate of ICI therapy alone in this patient population is expected to be very low, so it is exciting to see that the addition of LNS8801 to pembrolizumab is stopping progression in almost 70% of patients without any additional toxicity. We look forward to further exploration of LNS8801 alone and in combination, and we are encouraged by the continuing data we are seeing from these open cohorts.”

About LNS8801

LNS8801 is an orally bioavailable, 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 1/2a 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 some 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).


Patrick Mooney
Chief Executive Officer
(856) 433-1300