Antengene Receives U.S. FDA Clearance of IND Application for Phase I Trial of Small Molecule ERK1/2 Inhibitor ATG-017 in Patients with Advanced Solid Tumors

On October 31, 2022 Antengene Corporation Limited ("Antengene" SEHK: 6996.HK), a leading innovative, commercial-stage global biopharmaceutical company dedicated to discovering, developing and commercializing first-in-class and/or best-in-class therapeutics in hematology and oncology, reported that the Investigational New Drug (IND) application for ATG-017 has received clearance from the U.S. Food and Drug Administration (FDA) (Press release, Antengene, OCT 31, 2022, View Source [SID1234622654]). The IND clearance enables Antengene to initiate the combination portion of the Phase I "ERASER" clinical trial in the United States (U.S.) to evaluate the safety, pharmacokinetics, and preliminary efficacy of ATG-017 combination therapy with nivolumab in patients with advanced solid tumors.

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ATG-017 is an oral, potent, and selective inhibitor of extracellular signal-regulated protein kinase 1 and 2 (ERK1/2). Nivolumab is a human programmed death receptor-1 (PD-1) blocking antibody that binds to the PD-1 receptor expressed on activated T-cells. The clinical collaboration between Antengene and Bristol Myers Squibb to evaluate ATG-017 in combination with nivolumab builds on Antengene’s preclinical data. The data, including studies presented at the Society for Immunotherapy of Cancer (SITC) (Free SITC Whitepaper) 36th Annual Meeting & Pre-conference Programs in November 2021, has demonstrated that the combination of an ERK1/2 inhibitor and an immune checkpoint inhibitor (ICI) worked synergistically to produce improved efficacy in preclinical ICI-resistant in vivo mice models.

"We are excited to have received IND clearance for activation of the ERASER study in the U.S. Preclinical results with ATG-017 have been very promising both as a monotherapy and in combination with ICIs in aggressive and resistant malignancies. We are very pleased that the further clinical exploration will involve multiple geographies as we attempt to define the potential role of ATG-017 as a novel cancer treatment," said Dr. Kevin Lynch, Antengene’s Chief Medical Officer."Every day, we see advanced cancer patients with limited treatment options. We intend to initiate the study in the U.S. soon, and hope that ATG-017 will eventually offer a safe and effective new treatment option to those patients in need."

"The development of new therapies for cancer patients with refractory, relapsed, or advanced diseases is a cornerstone of Antengene’s work. ATG-017 is an exciting compound because of its attractive pharmacology, impressive preclinical activity on the RAS-MAPK pathway and the potential ability to synergize with ICIs. These attributes provide the rationale for evaluating ATG-017 as a monotherapy and in combination with ICIs such as nivolumab in patients with resistant or relapsed disease," said Dr. Jay Mei, Antengene’s Founder, Chairman and CEO. "We are very encouraged by this IND clearance from the U.S. FDA as it paves the way for one of Antengene’s first studies in the U.S. and marks an important milestone in the global clinical development of ATG-017. We look forward to initiating patient enrollment of the ERASER trial in the U.S."

About ATG-017

ATG-017 is an oral, potent, and selective small molecule extracellular signal-regulated kinases 1 and 2 (ERK1/2) inhibitor. ERK1/2 are related protein-serine/threonine kinases that function as terminal kinases in the RAS-MAPK signal transduction cascade. This cascade regulates a large variety of cellular processes, including proliferation. The RAS-MAPK pathway is dysregulated in more than 30% of human cancers with the most frequent alterations being observed in RAS or BRAF genes across multiple tumor types. An ERK inhibitor enables the targeting of both RAS and BRAF mutant diseases.

Antengene presented data at the Society for Immunotherapy in Cancer (SITC) (Free SITC Whitepaper) 36th Annual Meeting & Pre-conference Programs in November 2021 detailing compelling preclinical results showing the combination of ATG-017 and an anti-PD-L1 monoclonal antibody (atezolizumab) in an aggressive immune checkpoint resistant murine cancer model rendered "cold" tumors "hot". To date, ATG-017 has been approved in Australia and the United States to enter clinical studies in patients with advanced solid tumors or hematologic malignancies.