Linnaeus Therapeutics Announces Expanded Clinical Collaboration with Merck to Include Multiple Additional Cohorts to Evaluate LNS8801 in Combination with KEYTRUDA® in Patients with Advanced Cancer

Studies Will be Conducted at Multiple NCI-Designated Comprehensive Cancer Centers

Haddonfield NJ, June 15, 2021–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 expansion of its ongoing clinical collaboration with Merck to include multiple additional phase 2 cohorts. Based on promising preliminary safety, pharmacodynamic and efficacy data, this expanded agreement will allow the companies to further evaluate the combination of LNS8801 and Merck’s anti-PD-1 therapy, KEYTRUDA^®(pembrolizumab) in patients with selected advanced solid tumors.

LNS8801 is a first-in-class, orally bioavailable small molecule that is a highly specific and potent agonist of the G-protein estrogen receptor (GPER). GPER is widely expressed on cancers.  Stimulating GPER rapidly and durably depletes the c-Myc oncoprotein, stops cancers from proliferating, and makes them more visible to the immune system.

Linnaeus and Merck are currently evaluating the combination of LNS8801 and KEYTRUDA in patients who had previously responded to PD-1/L1 therapy but have subsequently  progressed on PD-1/L1 inhibitors. Additionally, Linnaeus is currently evaluating LNS8801 as a monotherapy in patients that cannot tolerate PD-1/L1 therapy due to serious immune-related adverse events.

Under the terms of the agreement, Linnaeus will conduct six additional Phase 2 cohorts evaluating the combination of LNS8801 and KEYTRUDA in several indications including NSCLC, head and neck cancer, cutaneous and uveal melanoma, among others.

“We are very pleased to expand our collaboration with Merck, the established leader in cancer immunotherapy, as we advance LNS8801 into Phase 2 clinical trials,” said Patrick Mooney, MD, Chief Executive Officer of Linnaeus. “Based on the encouraging signals we have seen so far in the advanced cancer patients treated with the combination of LNS8801 and KEYTRUDA as well as LNS8801 as monotherapy, we are optimistic that the combination of LNS8801 and KEYTRUDA will provide meaningful benefit to this patient population.”

KEYTRUDA is a registered trademark of Merck Sharp & Dohme Corp, a subsidiary of Merck & Co., Inc., Kenilworth, NJ, USA.

About LNS8801

LNS8801 is an orally bioavailable and highly specific, potent agonist of GPER whose activity is dependent on the expression of GPER. GPER activation by LNS8801 rapidly and durably depletes c-Myc oncoprotein 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 human 1/2a study, LNS8801 monotherapy has been safe and well tolerated. Additionally, LNS8801 has demonstrated target engagement, c-Myc oncoprotein depletion, and durable clinical benefit in patients with advanced cancer.