Adlai Nortye Announces First Patient Dosed in U.S. Phase 1b Trial of AN0025 in Combination with Merck’s KEYTRUDA® for Advanced Solid Tumors

On August 24, 2020, Adlai Nortye, a biopharmaceutical company dedicated to the research and development of global first-in-class innovative drugs, announced that AN0025, its oral estrogen receptor 4 antagonist with the potential to become a “first-in-class” therapy, would be combined with KEYTRUDA, Merck’s anti-PD-1 tumor immunotherapy drug.^®(Pembrolizumab, pembrolizumab) combination therapy for multiple solid tumors: First patient dosed in Phase 1b clinical trial in the United States.

This study (AN0025S0103) is an open-label, multicenter Phase 1b clinical trial conducted in the United States and Europe., including two phases: the dose-limiting toxicity (DLT) observation period and the expansion period, aimed at evaluating AN0025 in combination with KEYTRUDA^®Safety and Preliminary Efficacy of Combination Therapy in Multiple Locally Advanced/Metastatic Solid Tumors. During the dose-limiting toxicity observation period, the trial will enroll patients with urothelial carcinoma or squamous/non-squamous non-small cell lung cancer (NSCLC) to evaluate AN0025 in combination with KEYTRUDA.^®the safety and tolerability of the combination therapy, and to determine whether to proceed to the expansion phase; during the expansion phase, patient enrollment will be increased and will further include patients with urothelial carcinoma, non-small cell lung cancer, triple-negative breast cancer, cervical cancer, and colorectal cancer.In the United States, the first enrolled patient has completed dosing at the Huntsman Cancer Institute at the University of Utah, while patient recruitment is also ongoing at The University of Texas MD Anderson Cancer Center and the University of Virginia Cancer Center.

All enrolled patients will receive combination therapy with AN0025 and KEYTRUDA® until disease progression, dose-limiting toxicity, or withdrawal from the study, whichever occurs first. The maximum treatment duration shall not exceed 35 cycles (approximately 2 years). In each study cohort, for different doses of AN0025, KEYTRUDA^®A fixed dose of 200 mg/kg will be administered once every 3 weeks.

“In preclinical studies, AN0025 in combination with radiotherapy, chemoradiotherapy, and immune checkpoint inhibitors demonstrated antitumor activity across various malignant tumors. We believe that AN0025 combined with KEYTRUDA”^®“The combination therapy is expected to provide new treatment options for many cancer patients, including those with disease progression after first- or second-line therapies, as well as those who are non-responsive or resistant to PD-1 immunotherapy.”Dr. Lars Birgerson, Chief Development Officer of Adlai Nortye Biopharma, stated, “We aim to deliver innovative oncology treatments that address unmet clinical needs, enabling patients to achieve longer survival while maintaining a better quality of life.”

Regarding the AN0025S0103 Study

The AN0025S0103 study is an open-label, multicenter Phase 1b clinical trial conducted in the United States and Europe, comprising two phases: a dose-limiting toxicity (DLT) observation period and an expansion phase, designed to evaluate AN0025 in combination with KEYTRUDA^®Safety and Preliminary Efficacy of Combination Therapy in Multiple Locally Advanced/Metastatic Solid Tumors. All enrolled patients will receive AN0025 and KEYTRUDA^®combination therapy until disease progression, intolerable toxicity, or withdrawal from the study, with a maximum treatment duration of 35 cycles (approximately 2 years). In each study cohort, for different doses of AN0025, KEYTRUDA^®A fixed dose of 200 mg/kg will be administered once every 3 weeks.

About AN0025 (EP4 Antagonist)

AN0025 is a highly potent and selective oral prostaglandin E2 receptor 4 (EP4) antagonist with a globally leading research profile. It modulates the tumor microenvironment by targeting the EP4 receptor, thereby enhancing the body’s immune response. Preclinical in vitro and in vivo studies have demonstrated its robust anticancer activity and immunological benefits, and combination therapy (e.g., with radiotherapy or immune checkpoint inhibitors) has shown significant inhibition of tumor growth across multiple cancer types. At the 2019 ESMO Congress, the company presented Phase 1b clinical trial data from Europe and the United States on AN0025 as neoadjuvant therapy for locally advanced rectal cancer. Nearly 40% of patients either avoided surgery altogether or achieved pathological complete response in postoperative specimens. These encouraging results warrant further clinical investigation of AN0025 in combination with standard preoperative treatments.

About Adlai Nortye

Adlai Nortye is a clinical-stage global biopharmaceutical company focused on the global research and development of first-in-class novel drugs, positioning itself as a pioneer in “global-first” oncology therapeutics. Currently, the company has three products in mid-to-late stages of clinical development: AN2025 (buparlisib), which has received FDA Fast Track designation and is undergoing a global multicenter Phase 3 clinical trial; AN1004 (pelareorep), an intravenously administered oncolytic virus with one of the fastest global development progressions, which is also undergoing a global multicenter Phase 3 clinical trial; and AN0025 (an EP4 antagonist), a potential global first-in-class (FIC) tumor immunotherapy agent, which has completed Phase 1b clinical trials in Europe and the United States as a neoadjuvant therapy for locally advanced rectal cancer, in combination with KEYTRUDA^®Phase Ib clinical trials in Europe and the United States evaluating combination therapy for multiple solid tumors are ongoing.

KEYTRUDA^®® is a registered trademark, and the trademark rights are owned by Merck Sharp & Dohme Corp., a subsidiary of Merck & Co., Inc., located in Kenilworth, New Jersey, USA.